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(4E)-4-(hydroxyimino)-5-methyl-2-(propan-2-yl)cyclohexa-2,5-dien-1-one
(4E)-5-methyl-4-{[(2-methylbenzoyl)oxy]imino}-2-(propan-2-yl)cyclohexa-2,5-dien-1-one
(7R)-2-[5-(2,4-difluorophenyl)-1H-pyrazol-4-yl]-7-ethyl-5-methyl-8-(1-methyl-1H-pyrazol-4-yl)-7,8-dihydropteridin-6(5H)-one
-
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(1-methyl-1H-pyrazol-3-yl)-7,8-dihydropteridin-6(5H)-one
-
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(1-methyl-1H-pyrazol-4-yl)-7,8-dihydropteridin-6(5H)-one
-
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(1-methyl-1H-pyrazol-5-yl)-7,8-dihydropteridin-6(5H)-one
-
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(1H-pyrazol-4-yl)-7,8-dihydropteridin-6(5H)-one
-
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(3,3,3-trifluoropropyl)-7,8-dihydropteridin-6(5H)-one
-
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(oxetan-3-yl)-7,8-dihydropteridin-6(5H)-one
-
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-[(3S)-tetrahydrofuran-3-yl]-7,8-dihydropteridin-6(5H)-one
-
(7R)-7-ethyl-5-methyl-2-(2-phenyl-1H-imidazol-1-yl)-8-(3,3,3-trifluoropropyl)-7,8-dihydropteridin-6(5H)-one
-
(7R)-7-ethyl-5-methyl-2-(2-phenyl-1H-imidazol-1-yl)-8-(propan-2-yl)-7,8-dihydropteridin-6(5H)-one
-
(7R)-7-ethyl-5-methyl-2-(2-phenyl-1H-imidazol-1-yl)-8-(pyrimidin-5-yl)-7,8-dihydropteridin-6(5H)-one
-
(7R)-7-ethyl-5-methyl-2-(2-phenyl-1H-imidazol-1-yl)-8-[(3R)-tetrahydrofuran-3-yl]-7,8-dihydropteridin-6(5H)-one
-
(7R)-7-ethyl-5-methyl-2-(2-phenyl-1H-imidazol-1-yl)-8-[(3S)-tetrahydrofuran-3-yl]-7,8-dihydropteridin-6(5H)-one
-
(7R)-7-ethyl-5-methyl-8-(1H-pyrazol-4-yl)-2-[5-(1,3-thiazol-2-yl)-1H-pyrazol-4-yl]-7,8-dihydropteridin-6(5H)-one
-
(7R)-7-ethyl-5-methyl-8-(tetrahydro-2H-pyran-4-yl)-2-[5-(1,3-thiazol-2-yl)-1H-pyrazol-4-yl]-7,8-dihydropteridin-6(5H)-one
-
(7R)-7-ethyl-5-methyl-8-(tetrahydrofuran-3-yl)-2-[5-(1,3-thiazol-2-yl)-1H-pyrazol-4-yl]-7,8-dihydropteridin-6(5H)-one
-
(7R)-8-(3,3-difluorocyclobutyl)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-7,8-dihydropteridin-6(5H)-one
-
(R)-4-[(8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl)amino]-3-methoxy-N-(1-methyl-4-piperidinyl)benzamide
i.e. BI2536
1-(1-methylpiperidin-4-yl)-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
1-(2-hydroxyethyl)-2-(2-[[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridin-4-one
-
1-(2-hydroxyethyl)-5-(2-[[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-1H-pyrrole-3-carboxamide
-
1-acetyl-L-prolyl-L-leucyl-3-(5-[[(Z)-([2-[acetyl(phenyl)amino]-1,3-thiazol-4-yl]methylidene)amino]oxy]pentyl)-L-histidyl-L-seryl-O-phosphono-L-threoninamide
-
1-acetyl-L-prolyl-L-leucyl-3-(5-[[(Z)-([2-[benzyl(methyl)amino]-1,3-thiazol-5-yl]methylidene)amino]oxy]pentyl)-L-histidyl-L-seryl-O-phosphono-L-threoninamide
-
1-acetyl-L-prolyl-L-leucyl-3-(5-[[(Z)-benzylideneamino]oxy]pentyl)-L-histidyl-L-seryl-O-phosphono-L-threoninamide
-
1-acetyl-L-prolyl-L-leucyl-3-(6-[[(Z)-([1-[4-(thiophen-2-yl)pyrimidin-2-yl]-1H-pyrrol-2-yl]methylidene)amino]oxy]hexyl)-L-histidyl-L-seryl-O-phosphono-L-threoninamide
-
1-acetyl-L-prolyl-L-leucyl-3-(6-[[(Z)-([2-[acetyl(phenyl)amino]-1,3-thiazol-4-yl]methylidene)amino]oxy]hexyl)-L-histidyl-L-seryl-O-phosphono-L-threoninamide
-
1-acetyl-L-prolyl-L-leucyl-3-(6-[[(Z)-([2-[benzyl(methyl)amino]-1,3-thiazol-5-yl]methylidene)amino]oxy]hexyl)-L-histidyl-L-seryl-O-phosphono-L-threoninamide
-
1-acetyl-L-prolyl-L-leucyl-3-(6-[[(Z)-([5-chloro-2-[(pyridin-2-yl)methoxy]phenyl]methylidene)amino]oxy]hexyl)-L-histidyl-L-seryl-O-phosphono-L-threoninamide
-
1-acetyl-L-prolyl-L-leucyl-3-(6-[[(Z)-benzylideneamino]oxy]hexyl)-L-histidyl-L-seryl-O-phosphono-L-threoninamide
-
1-acetyl-L-prolyl-L-leucyl-3-(8-phenyloctyl)-L-histidyl-L-seryl-O-phosphono-L-threoninamide
-
1-acetyl-L-prolyl-L-leucyl-3-[5-([(Z)-[(2-fluoro-6-phenoxyphenyl)methylidene]amino]oxy)pentyl]-L-histidyl-L-seryl-O-phosphono-L-threoninamide
-
1-acetyl-L-prolyl-L-leucyl-3-[6-(2-phenoxyphenyl)hexyl]-L-histidyl-L-seryl-O-phosphono-L-threoninamide
-
1-acetyl-L-prolyl-L-leucyl-3-[6-([(Z)-[(2-fluoro-6-phenoxyphenyl)methylidene]amino]oxy)hexyl]-L-histidyl-L-seryl-O-phosphono-L-threoninamide
-
1-acetyl-L-prolyl-L-leucyl-3-[6-([(Z)-[(4'-fluoro[1,1'-biphenyl]-2-yl)methylidene]amino]oxy)hexyl]-L-histidyl-L-seryl-O-phosphono-L-threoninamide
-
1-acetyl-L-prolyl-L-leucyl-3-[8-(2-fluoro-6-phenoxyphenyl)octyl]-L-histidyl-L-seryl-O-phosphono-L-threoninamide
-
1-acetyl-L-prolyl-L-leucyl-3-[8-(2-phenoxyphenyl)octyl]-L-histidyl-L-seryl-O-phosphono-L-threoninamide
-
1-acetyl-L-prolyl-L-leucyl-3-[8-([1,1'-biphenyl]-2-yl)octyl]-L-histidyl-L-seryl-O-phosphono-L-threoninamide
-
1-acetyl-L-prolyl-L-leucyl-3-[8-[2-(benzyloxy)phenyl]octyl]-L-histidyl-L-seryl-O-phosphono-L-threoninamide
-
1-acetyl-L-prolyl-L-leucyl-3-[9-(2-fluoro-6-phenoxyphenyl)nonyl]-L-histidyl-L-seryl-O-phosphono-L-threoninamide
-
1-acetyl-L-prolyl-L-leucyl-L-histidyl-L-seryl-O-phosphono-L-threoninamide
-
1-cyclohexyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
1-methyl-2-(2-[[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridin-4-one
high levels of selectivity on a panel of unrelated kinases, as well as against PLK2 and PLK3 isoforms, acceptable oral bioavailability in mice making this inhibitor a suitable candidate for further in vivo activity studies
1-methyl-5-(2-[[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-1H-pyrrole-3-carboxamide
high levels of selectivity on a panel of unrelated kinases, as well as against PLK2 and PLK3 isoforms, acceptable oral bioavailability in mice making this inhibitor a suitable candidate for further in vivo activity studies
1-methyl-5-(2-[[5-(piperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-1H-pyrrole-3-carboxamide
-
1-methyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
1-methyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxylic acid
-
1-methyl-8-[(2-methylphenyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
1-methyl-8-[(2-nitrophenyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
1-methyl-8-[(2-phenoxyphenyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
1-methyl-8-[(2-sulfamoylphenyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
1-methyl-8-[(3-nitrophenyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
1-methyl-8-[(4-nitrophenyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
1-methyl-8-[[2-(methylamino)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
1-methyl-8-[[2-(methylsulfanyl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
1-methyl-8-[[2-(phenylamino)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
1-methyl-8-[[2-(phenylcarbonyl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
1-methyl-8-[[2-(phenylsulfanyl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
1-methyl-8-[[2-(propan-2-yl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
1-methyl-8-[[2-(trifluoromethyl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
1-methyl-8-[[3-(trifluoromethyl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
1-methyl-8-[[4-(trifluoromethyl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
1-methyl-N-phenyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
1-phenyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
1-[2-hydroxy-3-(4-methylpiperazin-1-yl)propyl]-1H-indole-3-carboxylic acid
-
1-[2-hydroxy-3-(piperidin-1-yl)propyl]-1H-indole-3-carboxylic acid
-
1-[2-hydroxy-3-(pyrrolidin-1-yl)propyl]-1H-indole-3-carboxylic acid
-
1-[3-(diethylamino)-2-hydroxypropyl]-1H-indole-3-carboxylic acid
-
2'-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5'-methyl-8'-(propan-2-yl)-5',8'-dihydro-6'H-spiro[cyclobutane-1,7'-pteridin]-6'-one
-
2-(2-[[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-1-(2,2,2-trifluoroethyl)-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridin-4-one
-
2-cyano-3-hydroxy-3-methyl-N-[4-(trifluoromethoxy)phenyl]-propenamide
LFM-A12
2-methyl-5-(propan-2-yl)cyclohexa-2,5-diene-1,4-dione
2-[(3-cyano-6-methoxyquinolin-2-yl)sulfanyl]-N-(2-methoxy-5-methylphenyl)acetamide
i.e. I2
2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5,7,7-trimethyl-8-(propan-2-yl)-7,8-dihydropteridin-6(5H)-one
-
2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-7-(2,2,2-trifluoroethyl)-8-(3,3,3-trifluoropropyl)-7,8-dihydropteridin-6(5H)-one
-
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-methoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(2R)-2,3-dihydroxypropyl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(2R)-2-hydroxy-3-pyrrolidin-1-ylpropyl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(4R)-1-methylazepan-4-yl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(4S)-1-methylazepan-4-yl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)methoxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
-
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
-
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[3-(dimethylamino)propoxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
-
3-[(1S)-1-(2-chlorophenyl)ethoxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
3-[(2-chlorobenzyl)oxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
3-[1-[2-hydroxy-3-(piperidin-1-yl)propyl]-1H-indol-3-yl]propanoic acid
-
3-[1-[2-hydroxy-3-(pyrrolidin-1-yl)propyl]-1H-indol-3-yl]propanoic acid
-
4-((R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydro-pteridin-2-ylamino)-3-methoxy-N-(1-methyl-piperidin-4-yl)-benzamide
BI 2536
4-[7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-6-oxo-6,7-dihydropteridin-8(5H)-yl]benzonitrile
-
5-(2-[[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-1-(2,2,2-trifluoroethyl)-1H-pyrrole-3-carboxamide
-
5-(2-[[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-1-[2-(tetrahydro-2H-pyran-4-yloxy)ethyl]-1H-pyrrole-3-carboxamide
-
5-(5,6-dimethoxy-1H-benzimidazol-1-yl)-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide
-
5-(6-methoxy-1H-benzimidazol-1-yl)-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
-
5-[6-(piperidin-4-yloxy)-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
-
5-[6-[(1-methylpiperidin-4-yl)methoxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
-
5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
-
7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5,7-dimethyl-8-(3,3,3-trifluoropropyl)-7,8-dihydropteridin-6(5H)-one
-
7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(1H-pyrazol-3-yl)-7,8-dihydropteridin-6(5H)-one
-
7-ethyl-5-methyl-8-(1-methyl-1H-pyrazol-4-yl)-2-[5-(1,3-thiazol-2-yl)-1H-pyrazol-4-yl]-7,8-dihydropteridin-6(5H)-one
-
7-ethyl-5-methyl-8-(1-methyl-1H-pyrazol-4-yl)-2-[5-(pyridin-2-yl)-1H-pyrazol-4-yl]-7,8-dihydropteridin-6(5H)-one
-
7-ethyl-5-methyl-8-phenyl-2-(2-phenyl-1H-imidazol-1-yl)-7,8-dihydropteridin-6(5H)-one
-
7-ethyl-8-(4-fluorophenyl)-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-7,8-dihydropteridin-6(5H)-one
-
8-(3,3-difluorocyclopentyl)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-7,8-dihydropteridin-6(5H)-one
-
8-(biphenyl-2-ylamino)-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
8-(phenylamino)-1-(2,2,2-trifluoroethyl)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
8-(phenylamino)-1-(propan-2-yl)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
8-(phenylamino)-1-[2-(piperidin-1-yl)ethyl]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
8-[(2-acetylphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
8-[(2-aminophenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
8-[(2-benzylphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
8-[(2-carbamoylphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
8-[(2-fluorophenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
8-[(2-methoxyphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
8-[(3-acetylphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
8-[(3-methoxyphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
8-[(4-acetylphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
8-[(4-methoxyphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
8-[[2-(acetylamino)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
8-[[2-acetyl-3-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
8-[[2-acetyl-4-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
8-[[2-acetyl-5-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
8-[[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
8-[[2-methoxy-5-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
CHIR-258
selectivity profile of PLK2/4 over PLK1/3
cyclic (-CH2-CO-Pro-Leu-His-Ser-pThr-Cys-S-)
-
cyclic [-CH2-CO-N[2-(1H-indol-3-yl)ethyl]-CH2-CO-Leu-His-Ser-pThr-NH-CH[CONH2]-CH2-S-]
-
cyclic [-CH2-CO-N[3-[[2-(1H-indol-3-yl)ethyl]amino]-3-oxopropyl]-CH2-CO-Leu-His-Ser-p-Thr-NH-CH[CONH2]-CH2-S-]
-
cyclic [-CH2-CO-N[6-[[2-(1-acetyl-1H-indol-3-yl)ethyl]amino]-6-oxohexyl]-CH2-CO-Leu-His-Ser-pThr-NH-CH[CONH2]-CH2-S-]
-
cyclic [-CH2-CO-N[6-[[2-(1-acetyl-1H-indol-3-yl)ethyl]amino]-6-oxohexyl]-CH2-CO-Leu-His[N3-(8-phenyloctyl)]-Ser-pThr-NH-CH[CONH2]-CH2-S-]
-
ethyl 1-methyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxylate
-
GO 6976
loses PLK1 activity by at least an order of magnitude, relative to staurosporine
GW843682X
potent inhibitor
hesperadin
almost complete inhibition
methyl 2-[(3-carbamoyl-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazolin-8-yl)amino]benzoate
-
N,1-dimethyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-2-methylbenzamide
-
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-2-nitrobenzamide
-
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-chlorobenzylaniline
-
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-methoxybenzamide
-
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-methoxybenzylaniline
-
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-methylbenzamide
-
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-methylbenzylaniline
-
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-nitrobenzamide
-
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-nitrobenzylaniline
-
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-acetamide
-
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-benzamide
-
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-benzylaniline
-
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)-2-methylbenzamide
-
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)-2-nitrobenzamide
-
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)-4-methoxybenzamide
a highly selective inhibitor of Plk1, in vitro kinase inhibitory profile of 5i, overview
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)-4-nitrobenzamide
-
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)acetamide
-
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)benzamide
-
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)benzylaniline
-
N-cyclopentyl-1-methyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
N-cyclopropyl-1-methyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
N-[2-methoxy-5-({[(E)-2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonyl}methyl)phenyl]glycine
N-[4-[(6-chloropyridin-3-yl)methoxy]-3-methoxybenzyl]-2-(3,4-dimethoxyphenyl)ethanamine
SBE13
ONO1910
inhibits Plk1 activity without significantly impacting Plk3 activity in vitro
PHA-680626
selective against Plk1
RNA
RNA interference abrogates centrosome maturation, spindle bipolarization, and silencing of the spindle assembly checkpoint
RNAi
down-regulation of Plk1 protein level by ca. 90%, abolishes the mobility-shifted, hyperphosphorylated form of BubR1 in the prometaphase-arrested cells
-
tert-butyl 1-methyl-2-(2-[[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-4-oxo-1,4,6,7-tetrahydro-5H-pyrrolo[3,2-c]pyridine-5-carboxylate
-
Wortmannin
time-dependent irreversible inhibition with PLK1
[1-[2-hydroxy-3-(4-methylpiperazin-1-yl)propyl]-1H-indol-3-yl]acetic acid
a highly selective inhibitor of Plk1, poor inhibition of Plk2 and Plk3
[1-[2-hydroxy-3-(morpholin-4-yl)propyl]-1H-indol-3-yl]acetic acid
-
[1-[2-hydroxy-3-(piperidin-1-yl)propyl]-1H-indol-3-yl]acetic acid
-
[1-[2-hydroxy-3-(pyrrolidin-1-yl)propyl]-1H-indol-3-yl]acetic acid
-
[1-[3-(diethylamino)-2-hydroxypropyl]-1H-indol-3-yl]acetic acid
-
(1R)-1-[(3S,6S,9S,12S,15S)-19-(6-[[2-(1-acetyl-1H-indol-3-yl)ethyl]amino]-6-oxohexyl)-3-carbamoyl-9-(hydroxymethyl)-12-(1H-imidazol-5-ylmethyl)-15-(2-methylpropyl)-5,8,11,14,17,20-hexaoxo-1-thia-4,7,10,13,16,19-hexaazacyclohenicosan-6-yl]ethyl phosphate
PL-116
-
(1R)-1-[(3S,6S,9S,12S,15S)-19-(6-[[2-(1-acetyl-1H-indol-3-yl)ethyl]amino]-6-oxohexyl)-3-carbamoyl-9-(hydroxymethyl)-15-(2-methylpropyl)-5,8,11,14,17,20-hexaoxo-12-[[1-(9-phenylnonyl)-1H-imidazol-5-yl]methyl]-1-thia-4,7,10,13,16,19-hexaazacyclohenicosan-6-yl]ethyl phosphate
PL-120
(2Z)-2-(5-bromo-2-methoxybenzylidene)-6-methyl-7H-[1,3]thiazolo[3,2-b][1,2,4]triazine-3,7(2H)-dione
-
(3S)-4-amino-4-oxo-3-([[2-(4-phenylbutyl)-1-(2-phenylethyl)-1H-benzimidazol-5-yl]carbonyl]amino)butan-2-yl phosphate
-
(4E)-5-methyl-4-[[(2-methylbenzoyl)oxy]imino]-2-(propan-2-yl)cyclohexa-2,5-dien-1-one
-
(4R)-1-acetyl-4-(4-phenylbutoxy)prolyl-L-leucyl-L-histidyl-L-seryl-O-phosphono-L-threoninamide
-
(4R)-1-acetyl-4-[[(E)-(3-phenylpropylidene)amino]oxy]prolyl-L-leucyl-L-histidyl-L-seryl-O-phosphono-L-threoninamide
-
(7R)-2-[5-(2,4-difluorophenyl)-1H-pyrazol-4-yl]-7-ethyl-5-methyl-8-(1-methyl-1H-pyrazol-4-yl)-7,8-dihydropteridin-6(5H)-one
-
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(1-methyl-1H-pyrazol-3-yl)-7,8-dihydropteridin-6(5H)-one
good selectivity over Plk-1 (193-fold), good permeability and moderate microsomal stability. When dosed orally in rats, the inhibitor demonstrates a 41-45% reduction of pS129-a-synuclein levels in the cerebral cortex
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(1-methyl-1H-pyrazol-4-yl)-7,8-dihydropteridin-6(5H)-one
-
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(1-methyl-1H-pyrazol-5-yl)-7,8-dihydropteridin-6(5H)-one
-
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(1H-pyrazol-4-yl)-7,8-dihydropteridin-6(5H)-one
-
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(3,3,3-trifluoropropyl)-7,8-dihydropteridin-6(5H)-one
-
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(oxetan-3-yl)-7,8-dihydropteridin-6(5H)-one
-
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-[(3S)-tetrahydrofuran-3-yl]-7,8-dihydropteridin-6(5H)-one
-
(7R)-7-ethyl-5-methyl-2-(2-phenyl-1H-imidazol-1-yl)-8-(3,3,3-trifluoropropyl)-7,8-dihydropteridin-6(5H)-one
-
(7R)-7-ethyl-5-methyl-2-(2-phenyl-1H-imidazol-1-yl)-8-(propan-2-yl)-7,8-dihydropteridin-6(5H)-one
-
(7R)-7-ethyl-5-methyl-2-(2-phenyl-1H-imidazol-1-yl)-8-(pyrimidin-5-yl)-7,8-dihydropteridin-6(5H)-one
-
(7R)-7-ethyl-5-methyl-2-(2-phenyl-1H-imidazol-1-yl)-8-[(3R)-tetrahydrofuran-3-yl]-7,8-dihydropteridin-6(5H)-one
-
(7R)-7-ethyl-5-methyl-2-(2-phenyl-1H-imidazol-1-yl)-8-[(3S)-tetrahydrofuran-3-yl]-7,8-dihydropteridin-6(5H)-one
-
(7R)-7-ethyl-5-methyl-8-(1H-pyrazol-4-yl)-2-[5-(1,3-thiazol-2-yl)-1H-pyrazol-4-yl]-7,8-dihydropteridin-6(5H)-one
-
(7R)-7-ethyl-5-methyl-8-(tetrahydro-2H-pyran-4-yl)-2-[5-(1,3-thiazol-2-yl)-1H-pyrazol-4-yl]-7,8-dihydropteridin-6(5H)-one
-
(7R)-7-ethyl-5-methyl-8-(tetrahydrofuran-3-yl)-2-[5-(1,3-thiazol-2-yl)-1H-pyrazol-4-yl]-7,8-dihydropteridin-6(5H)-one
-
(7R)-8-(3,3-difluorocyclobutyl)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-7,8-dihydropteridin-6(5H)-one
-
1-(26-oxo-2,5,8,11,14,17,20,23-octaoxahexacosan-26-yl)-L-prolyl-L-leucyl-3-(8-phenyloctyl)-L-histidyl-L-seryl-(3R)-4-phosphono-L-valinamide
-
1-acetyl-L-prolyl-L-leucyl-3-(8-phenyloctyl)-L-histidyl-L-seryl-O-phosphono-L-threoninamide
-
1-acetyl-L-prolyl-L-leucyl-3-[3-(2-hydroxyethyl)-1-(8-phenyloctyl)-1H-imidazol-3-ium-5-yl]-L-alanyl-L-seryl-O-phosphono-L-threoninamide
-
1-acetyl-L-prolyl-L-leucyl-3-[3-(2-hydroxyethyl)-1-(8-phenyloctyl)-1H-imidazol-3-ium-5-yl]-L-alanyl-L-seryl-O-[[[(2,2-dimethylpropanoyl)oxy]methoxy](hydroxy)phosphoryl]-L-threoninamide
-
1-methyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
1-methyl-8-[(2-methylphenyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
1-methyl-8-[(2-phenoxyphenyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
1-methyl-8-[[2-(methylamino)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
1-methyl-8-[[2-(methylsulfanyl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
1-methyl-8-[[2-(propan-2-yl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
1-methyl-8-[[2-(trifluoromethyl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
2'-(2-hydroxyethoxy)-5'-methyl-(1,1':3',1''-terphenyl)-4,4''-dinitrile
-
0.3 mM, 11% inhibition, full-length enzyme Plk1 with the mutation T210D in the active-site loop of kinase domain
2'-(2-hydroxyethoxy)-5'-methyl-(1,1':3':1''-terphenyl)-4''-(1H-tetrazol-5-yl)-4-nitrile
-
0.3 mM, 66% inhibition, full-length enzyme Plk1 with the mutation T210D in the active-site loop of kinase domain
2'-(2-hydroxyethoxy)-5'-methyl-[1,1':3',1''-terphenyl]-3,3'',5,5''-tetrafluoro-4,4''-diol
-
0.3 mM, 61% inhibition, full-length enzyme Plk1 with the mutation T210D in the active-site loop of kinase domain
2'-(2-hydroxyethoxy)-5'-methyl-[1,1':3',1''-terphenyl]-4,4''-diacetic acid
-
0.3 mM, 53% inhibition, full-length enzyme Plk1 with the mutation T210D in the active-site loop of kinase domain
2'-(2-hydroxyethoxy)-5'-methyl-[1,1':3',1''-terphenyl]-4,4''-dicarboxylic acid
-
0.3 mM, 14% inhibition, full-length enzyme Plk1 with the mutation T210D in the active-site loop of kinase domain
2'-(2-hydroxyethoxy)-5'-methyl-[1,1':3',1''-terphenyl]-4,4''-dipropionic acid
-
0.3 mM, 26% inhibition, full-length enzyme Plk1 with the mutation T210D in the active-site loop of kinase domain
2'-hydroxy-5'-methyl-[1,1':3',1''-terphenyl]-4,4''-dicarboxylic acid
-
0.3 mM, 36% inhibition, full-length enzyme Plk1 with the mutation T210D in the active-site loop of kinase domain
2'-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5'-methyl-8'-(propan-2-yl)-5',8'-dihydro-6'H-spiro[cyclobutane-1,7'-pteridin]-6'-one
-
2,3,4,6-tetrahydroxy-5H-benzo[7]annulen-5-one
HeLa cells treated with purpurogallin exhibit delayed onset of mitosis and prolonged mitosis progression
2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5,7,7-trimethyl-8-(propan-2-yl)-7,8-dihydropteridin-6(5H)-one
-
2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-7-(2,2,2-trifluoroethyl)-8-(3,3,3-trifluoropropyl)-7,8-dihydropteridin-6(5H)-one
-
2-[5'-methyl-4,4''-ditetrazol-5-yl-(1,1':3',1''-terphenyl)-2'-oxy]ethanol
-
0.3 mM, 47% inhibition, full-length enzyme Plk1 with the mutation T210D in the active-site loop of kinase domain
3-(1,3-benzodioxol-5-yl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
-
3-(2-methylcyclohexyl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
-
3-(3,4-dimethoxyphenyl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
-
3-(3,4-dimethylphenyl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
-
3-(3-chlorophenyl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
-
3-(3-methylphenyl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
3-(4-methylphenyl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
-
3-(4-methylthiophen-3-yl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
-
3-benzyl-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
>0.020
3-phenyl-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
-
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-methoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(2R)-2,3-dihydroxypropyl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(2R)-2-hydroxy-3-pyrrolidin-1-ylpropyl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(4R)-1-methylazepan-4-yl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(4S)-1-methylazepan-4-yl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)methoxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
-
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
-
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[3-(dimethylamino)propoxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
-
3-[(1S)-1-(2-chlorophenyl)ethoxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
3-[(2-chlorobenzyl)oxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
3-[1-(5-[[(1S)-1-phenylethyl]amino]isoxazolo[5,4-c]pyridin-3-yl)piperidin-3-yl]propanamide
-
3-[3-chloro-5-(5-[[(1S)-1-phenylethyl]amino]isoxazolo[5,4-c]pyridin-3-yl)phenyl]propan-1-ol
-
3-[3-chloro-5-(5-[[(1S)-1-phenylethyl]amino]isoxazolo[5,4-c]pyridin-3-yl)phenyl]propanamide
-
4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2-ol
selectivity profile of PLK2/4 over PLK1/3
4-[7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-6-oxo-6,7-dihydropteridin-8(5H)-yl]benzonitrile
-
5-(5,6-dimethoxy-1H-benzimidazol-1-yl)-3-[2-(trifluoromethyl)-benzyloxy]-thiophene-2-carboxamide
-
-
5-(5,6-dimethoxy-1H-benzimidazol-1-yl)-3-[2-(trifluoromethyl)-benzyl]oxythiophene-2-carboxamide
-
GW843682X
5-(5,6-dimethoxy-1H-benzimidazol-1-yl)-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide
-
5-(5,6-dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)phenyl]methoxy}thiophene-2-carboxamide
-
i.e. GW843682X, inhibition of PLK1 activity abrogates mitotic activation of AMP-activated protein kinasealpha through direct or indirect mechanisms
5-(6-methoxy-1H-benzimidazol-1-yl)-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
-
5-[6-(piperidin-4-yloxy)-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
-
5-[6-[(1-methylpiperidin-4-yl)methoxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
-
5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
-
7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5,7-dimethyl-8-(3,3,3-trifluoropropyl)-7,8-dihydropteridin-6(5H)-one
-
7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(1H-pyrazol-3-yl)-7,8-dihydropteridin-6(5H)-one
-
7-ethyl-5-methyl-8-(1-methyl-1H-pyrazol-4-yl)-2-[5-(1,3-thiazol-2-yl)-1H-pyrazol-4-yl]-7,8-dihydropteridin-6(5H)-one
-
7-ethyl-5-methyl-8-(1-methyl-1H-pyrazol-4-yl)-2-[5-(pyridin-2-yl)-1H-pyrazol-4-yl]-7,8-dihydropteridin-6(5H)-one
-
7-ethyl-5-methyl-8-phenyl-2-(2-phenyl-1H-imidazol-1-yl)-7,8-dihydropteridin-6(5H)-one
-
7-ethyl-8-(4-fluorophenyl)-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-7,8-dihydropteridin-6(5H)-one
-
8-(3,3-difluorocyclopentyl)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-7,8-dihydropteridin-6(5H)-one
-
8-[(2-acetylphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
8-[(2-aminophenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
8-[(2-fluorophenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
8-[(2-methoxyphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
8-[[2-(acetylamino)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
8-[[2-acetyl-3-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
8-[[2-acetyl-4-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
8-[[2-acetyl-5-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
8-[[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
8-[[2-methoxy-5-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
ataxia-telangiectasia mutant
-
i.e. ATM, inhibits p53 phosphorylation by Plk1 in vivo
-
FDPPLHSpTA
a PBIP1-derived phosphopeptide, the N-terminal phenylalanine sits in the hydrophobic pocket
MAGPMQSpTPLNGAKK
the peptide inhibitor blocks the interaction between the Plk1 PBD and Cdc25C
N-(26-(4-[(4-[[(7S)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl]amino]-3-methoxybenzoyl)amino]piperidin-1-yl)-19-oxo-3,6,9,12,15-pentaoxa-18-azahexacosan-1-oyl)glycyl-L-prolyl-L-leucyl-L-histidyl-L-seryl-O-phosphono-L-threonyl-L-alaninamide
-
N-(3-(2-[(8-[4-[(4-[[(7S)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl]amino]-3-methoxybenzoyl)amino]piperidin-1-yl]octanoyl)amino]ethoxy)propanoyl)glycyl-L-prolyl-L-leucyl-L-histidyl-L-seryl-O-phosphono-L-threonyl-L-alaninamide
-
N-(48-(4-[(4-[[(7S)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl]amino]-3-methoxybenzoyl)amino]piperidin-1-yl)-41-oxo-4,7,10,13,16,19,22,25,28,31,34,37-dodecaoxa-40-azaoctatetracontan-1-oyl)glycyl-L-prolyl-L-leucyl-L-histidyl-L-seryl-O-phosphono-L-threonyl-L-alaninamide
-
N-(72-(4-[(4-[[(7S)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl]amino]-3-methoxybenzoyl)amino]piperidin-1-yl)-65-oxo-4,7,10,13,16,19,22,25,28,31,34,37,40,43,46,49,52,55,58,61-icosaoxa-64-azadoheptacontan-1-oyl)glycyl-L-prolyl-L-leucyl-L-histidyl-L-seryl-O-phosphono-L-threonyl-L-alaninamide
-
N-acetyl-N-(6-phenylhexyl)glycyl-L-leucyl-L-histidyl-L-seryl-O-phosphono-L-threoninamide
-
N-adamantylacetyl-L-prolyl-L-leucyl-L-histidyl-L-seryl-O-phosphono-L-threonyl-L-methioninamide
i.e PL-55, PLHSpT-based peptide
N-[(1S)-1-phenylethyl]-3-thiophen-2-ylisoxazolo[5,4-c]pyridin-5-amine
-
N-[3-(1-benzothiophen-2-yl)propanoyl]-alpha-aspartyl-L-prolyl-L-prolyl-L-leucyl-L-histidyl-L-seryl-O-phosphono-L-threonyl-L-alaninamide
-
NMS-P937
inhibition via binding in the ATP-binding site
PL-49
cyclohexylmethyl-PLHSpTM
RNAi
induces Plk3 depletion, which causes a large fraction of cells to become quiescent, Plk3-depleted cells appear to pass through mitosis normally and complete cell division, but failed to reenter the cell cycle
-
Volasertib
BI6727, inhibition via binding in the ATP-binding site
(4E)-4-(hydroxyimino)-5-methyl-2-(propan-2-yl)cyclohexa-2,5-dien-1-one
-
(4E)-4-(hydroxyimino)-5-methyl-2-(propan-2-yl)cyclohexa-2,5-dien-1-one
i.e. poloxime, PXE
(4E)-5-methyl-4-{[(2-methylbenzoyl)oxy]imino}-2-(propan-2-yl)cyclohexa-2,5-dien-1-one
-
(4E)-5-methyl-4-{[(2-methylbenzoyl)oxy]imino}-2-(propan-2-yl)cyclohexa-2,5-dien-1-one
i.e. poloxin
2-methyl-5-(propan-2-yl)cyclohexa-2,5-diene-1,4-dione
-
2-methyl-5-(propan-2-yl)cyclohexa-2,5-diene-1,4-dione
i.e. thymoquinone
BI 2536
-
BI 2536
remarkable potency and selectivity towards Plk1, HeLa cells treated with BI 2536 are first delayed in prophase, after reluctantly entering mitosis, cells become blocked in prometaphase with aberrant monopolar spindles that fail to attach stably to chromosomes
BI 2536
time-dependent inhibition of PLK1
BI 2536
a dihydropteridinone and a ATP-competitive Plk1 inhibitor
BI 6727
a ATP-competitive Plk1 inhibitor
BI-2536
blocks contractile ring assembly by preventing the localization of Rho and Rho-GEF without affecting the assembly of the central spindle
BI-2536
potential anti-cancer therapeutic agent, shows strong selectivity for Plk1
BTO-1
-
BTO-1
blocks contractile ring assembly by preventing the localization of Rho and Rho-GEF without affecting the assembly of the central spindle
N-[2-methoxy-5-({[(E)-2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonyl}methyl)phenyl]glycine
-
N-[2-methoxy-5-({[(E)-2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonyl}methyl)phenyl]glycine
i.e. ON01910, exhibits little activity against Plk1 in vitro, effective in inhibiting the cell proliferation
siRNA
-
-
siRNA
depletion of Plk1, which leads to loss of BubR1 hyperphosphorylation, but has no significant effects on BubR1 localization
-
siRNA
reduces serine phosphorylation of HsCdc14A but not HsCdc14 protein level
-
3-(3-methylphenyl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
-
3-(3-methylphenyl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
>0.01
AG-013736
-
AG-013736
selective inhibition of PLK4 relative to PLK1-3
BAY 439006
-
BAY 439006
selective inhibition of PLK4 relative to PLK1-3
BI 2536
-
-
BI 2536
time-dependent inhibition
BI 2536
-
potent and selective inhibitor of Plk1, delays prophase and entrance into prometaphase, initiates cyclin A destruction without degrading Emi1, leads to spindle-assembly-checkpoint-induced prometaphase arrest, prevents Plk1s enrichment at kinetochores and centrosomes, in metaphase cells induces detachment of microtubules from kinetochores and leads to spindle collapse, the inhibitor may serve as a powerful tool in mitosis research
BI 2536
inhibition via binding in the ATP-binding site
BI-2536
-
BI-2536
inhibits the wild-type enzyme but not mutant Plk1as
BI2536
-
-
CHIR-258
-
CHIR-258
selectivity profile of PLK2/4 over PLK1/3
CP 547632
-
CP 547632
selective inhibition of PLK4 relative to PLK1-3
GO 6976
-
GO 6976
loses PLK2 activity by at least an order of magnitude, relative to staurosporine
GO 6976
loses PLK3 activity by at least an order of magnitude, relative to staurosporine
GSK461364A
-
-
GSK461364A
-
ATP-competitive inhibitor
GSK461364A
inhibition via binding in the ATP-binding site
H-1152
-
H-1152
selective inhibition of PLK4 relative to PLK1-3
imatinib
-
imatinib
selective inhibition of PLK4 relative to PLK1-3
LY294002
-
-
LY294002
selective inhibition of PLK4 relative to PLK1-3
ONO1910
-
ONO1910
does not significantly impacting Plk3 activity in vitro
SBE13
-
-
SBE13
-
selective type II Plk1 inhibitor
scytonemin
-
siRNA
-
-
staurosporine
-
staurosporine
specific for PLK4
SU11248
-
SU11248
selective inhibition of PLK4 relative to PLK1-3
VX-680
-
VX-680
selective inhibition of PLK4 relative to PLK1-3
Wortmannin
-
additional information
the kinase activity is regulated by the conserved C-terminal polo box domain which acts as both an autoinhibitory domain and a subcellular localization domain
-
additional information
-
the kinase activity is regulated by the conserved C-terminal polo box domain which acts as both an autoinhibitory domain and a subcellular localization domain
-
additional information
1-NM-PP1 and 3-MB-PP1 have little effect on wild-type
-
additional information
-
1-NM-PP1 and 3-MB-PP1 have little effect on wild-type
-
additional information
inhibited by Plk1-specific antibodies
-
additional information
-
inhibited by Plk1-specific antibodies
-
additional information
design and synthesis of series of small-molecule non-ATP-competitive Plk1 inhibitors targeting the substrate-binding pocket are designed through rational drug design, molecular docking. Some comound are selective against inhibitory selectivity against polo kinases Plk2 and Plk3. Growth inhibition activity with HeLa and MCF-7 cells
-
additional information
identification of indole-3-carboxylic acids as non-ATP-competitive Plk1 inhibitors
-
additional information
-
in vivo inhibition of Plk1 by DNA damage is ATM- or ATR-dependent
-
additional information
-
Plk1 activity is inhibited upon DNA damage involving ATM or ATR, caffeine blocks the inhibition
-
additional information
-
Plk1 depletion in HeLa Plk RNAi cells by Aurora B inhibitor hesperadin, enzyme depletion delays entry into mitosis and arrest in prometaphase activating the spindle checkpoint
-
additional information
-
Plk1 expression is decreased during ciplatin-induced apoptosis while p53 is stabilized
-
additional information
GO 6976 retains PLK4 activity
-
additional information
GO 6976 retains PLK4 activity
-
additional information
GO 6976 retains PLK4 activity
-
additional information
GO 6976 retains PLK4 activity
-
additional information
the polo-box domain is unique to the five-member family of polo-like kinases, and its inhibition is sufficient to inhibit the enzyme. Small molecule and peptide-based inhibitors of the Plk1 polo-box domain, PBD, detailed overview
-
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Adenocarcinoma
A randomised phase II trial of the Polo-like kinase inhibitor BI 2536 in chemo-naïve patients with unresectable exocrine adenocarcinoma of the pancreas - a study within the Central European Society Anticancer Drug Research (CESAR) collaborative network.
Adenocarcinoma
FOXM1 and polo-like kinase 1 are co-ordinately overexpressed in patients with gastric adenocarcinomas.
Adenocarcinoma
RNA interference-mediated silencing of the polo-like kinase 1 gene enhances chemosensitivity to gemcitabine in pancreatic adenocarcinoma cells.
Adenocarcinoma of Lung
[Effect of antisense RNA targeting Polo-like kinase 1 on cell cycle of lung cancer cell line A549]
Adrenal Cortex Neoplasms
Targeting polo-like kinase 1, a regulator of p53, in the treatment of adrenocortical carcinoma.
Adrenocortical Carcinoma
Targeting polo-like kinase 1, a regulator of p53, in the treatment of adrenocortical carcinoma.
Alzheimer Disease
Inhibition of Polo-like kinase 1 reduces beta-amyloid-induced neuronal cell death in Alzheimer's disease.
Alzheimer Disease
Inhibition of Polo-like kinase 2 ameliorates pathogenesis in Alzheimer's disease model mice.
Alzheimer Disease
Neuronal polo-like kinase in Alzheimer disease indicates cell cycle changes.
Anemia, Aplastic
Deregulation of vital mitotic kinase-phosphatase signaling in hematopoietic stem/progenitor compartment leads to cellular catastrophe in experimental aplastic anemia.
Aneurysm
Plk1 regulates contraction of postmitotic smooth muscle cells and is required for vascular homeostasis.
Aortic Rupture
Plk1 regulates contraction of postmitotic smooth muscle cells and is required for vascular homeostasis.
Arthritis, Rheumatoid
siRNA targeting PLK-1 induces apoptosis of synoviocytes in rheumatoid arthritis.
Ataxia Telangiectasia
Polo-like kinase 1 inactivation following mitotic DNA damaging treatments is independent of ataxia telangiectasia mutated kinase.
Atrial Fibrillation
Diminished PLK2 Induces Cardiac Fibrosis and Promotes Atrial Fibrillation.
Brain Neoplasms
Polo-Like Kinase 1 (PLK1) Inhibition Kills Glioblastoma Multiforme Brain Tumour Cells in Part Through Loss of SOX2 and Delays Tumour Progression in Mice.
Brain Neoplasms
Polo-Like Kinase 4 (PLK4) Is Overexpressed in Central Nervous System Neuroblastoma (CNS-NB).
Brain Neoplasms
ROS-Responsive Polymeric siRNA Nanomedicine Stabilized by Triple Interactions for the Robust Glioblastoma Combinational RNAi Therapy.
Breast Neoplasms
Anticancer effects of radiation therapy combined with Polo-Like Kinase 4 (PLK4) inhibitor CFI-400945 in triple negative breast cancer.
Breast Neoplasms
Augmented expression of Polo-like kinase 1 is a strong predictor of shorter cancer-specific overall survival in early stage breast cancer at 15-year follow-up.
Breast Neoplasms
Bioinformatics analysis of key genes in triple negative breast cancer and validation of oncogene PLK1.
Breast Neoplasms
Calcium-dependent inhibition of polo-like kinase 3 activity by CIB1 in breast cancer cells.
Breast Neoplasms
Characterization of adipose-derived stem cells from subcutaneous and visceral adipose tissues and their function in breast cancer cells.
Breast Neoplasms
Circular RNA circPLK1 promotes breast cancer cell proliferation, migration and invasion by regulating miR-4500/IGF1 axis.
Breast Neoplasms
Dendrimer mediated targeting of siRNA against polo-like kinase for the treatment of triple negative breast cancer.
Breast Neoplasms
Design, synthesis, and biological evaluation of polo-like kinase 1/eukaryotic elongation factor 2 kinase (PLK1/EEF2K) dual inhibitors for regulating breast cancer cells apoptosis and autophagy.
Breast Neoplasms
Detection of the Cell Cycle-Regulated Negative Feedback Phosphorylation of Mitogen-Activated Protein Kinases in Breast Carcinoma using Nanofluidic Proteomics.
Breast Neoplasms
Differentially expressed transcripts and dysregulated signaling pathways and networks in African American breast cancer.
Breast Neoplasms
DNA methylation data for identification of epigenetic targets of resveratrol in triple negative breast cancer cells.
Breast Neoplasms
Down-regulation of Polo-like kinase 1 elevates drug sensitivity of breast cancer cells in vitro and in vivo.
Breast Neoplasms
Essential Role of Polo-like Kinase 1 (Plk1) Oncogene in Tumor Growth and Metastasis of Tamoxifen-Resistant Breast Cancer.
Breast Neoplasms
Expression of Polo-Like Kinase 4(PLK4) in Breast Cancer and Its Response to Taxane-Based Neoadjuvant Chemotherapy.
Breast Neoplasms
Genome co-amplification upregulates a mitotic gene network activity that predicts outcome and response to mitotic protein inhibitors in breast cancer.
Breast Neoplasms
High expression of polo-like kinase 1 is associated with TP53 inactivation, DNA repair deficiency, and worse prognosis in ER positive Her2 negative breast cancer.
Breast Neoplasms
Identification of key genes in glioblastoma-associated stromal cells using bioinformatics analysis.
Breast Neoplasms
Identifying breast cancer subtypes associated modules and biomarkers by integrated bioinformatics analysis.
Breast Neoplasms
Immunohistochemical detection of Polo-like Kinase-1 (PLK1) in primary breast cancer is associated with TP53 mutation and poor clinical outcome.
Breast Neoplasms
Inhibition of Polo-like kinase 1 prevents the growth of metastatic breast cancer cells in the brain.
Breast Neoplasms
LFM-A13, a potent inhibitor of polo-like kinase, inhibits breast carcinogenesis by suppressing proliferation activity and inducing apoptosis in breast tumors of mice.
Breast Neoplasms
Matrix metalloproteinase 2-responsive micelle for siRNA delivery.
Breast Neoplasms
Multicentric parallel phase II trial of the polo-like kinase 1 inhibitor BI 2536 in patients with advanced head and neck cancer, breast cancer, ovarian cancer, soft tissue sarcoma and melanoma. The first protocol of the European Organization for Research and Treatment of Cancer (EORTC) Network Of Core Institutes (NOCI).
Breast Neoplasms
Nuclear cyclin B1 in human breast carcinoma as a potent prognostic factor.
Breast Neoplasms
PLK1 Inhibition Down-regulates Polycomb Group Protein BMI1 via Modulation of the miR-200c/141 Cluster.
Breast Neoplasms
PLK1 Inhibition Sensitizes Breast Cancer Cells to Radiation via Suppressing Autophagy.
Breast Neoplasms
Polo-like kinase 1 (Plk1) inhibition synergizes with taxanes in triple negative breast cancer.
Breast Neoplasms
Polo-like kinase 1: a potential therapeutic option in combination with conventional chemotherapy for the management of patients with triple-negative breast cancer.
Breast Neoplasms
Polo-like kinase isoforms in breast cancer: expression patterns and prognostic implications.
Breast Neoplasms
Polo-like kinase: a novel marker of proliferation: correlation with estrogen-receptor expression in human breast cancer.
Breast Neoplasms
Potentiation of cell killing by fractionated radiation and suppression of proliferative recovery in MCF-7 breast tumor cells by the Vitamin D3 analog EB 1089.
Breast Neoplasms
Resveratrol inhibits cell cycle progression by targeting Aurora kinase A and Polo-like kinase 1 in breast cancer cells.
Breast Neoplasms
Selective transferrin coating as a facile strategy to fabricate BBB-permeable and targeted vesicles for potent RNAi therapy of brain metastatic breast cancer in vivo.
Breast Neoplasms
SKA3 Promotes Cell Growth in Breast Cancer by Inhibiting PLK-1 Protein Degradation.
Breast Neoplasms
Small interfering RNA library screen identified polo-like kinase-1 (PLK1) as a potential therapeutic target for breast cancer that uniquely eliminates tumour-initiating cells.
Breast Neoplasms
Targeted delivery of PLK1-siRNA by ScFv suppresses Her2+ breast cancer growth and metastasis.
Breast Neoplasms
Targeting basal-like breast tumors with bromodomain and extraterminal domain (BET) and polo-like kinase inhibitors.
Burkitt Lymphoma
A specific inhibitor of polo-like kinase 1, GSK461364A, suppresses proliferation of Raji Burkitt's lymphoma cells through mediating cell cycle arrest, DNA damage, and apoptosis.
Burkitt Lymphoma
BI6727, a polo-like kinase 1 inhibitor with promising efficacy on Burkitt lymphoma cells.
Carcinogenesis
A Cereblon Modulator CC-885 Induces CRBN- and p97-Dependent PLK1 Degradation and Synergizes with Volasertib to Suppress Lung Cancer.
Carcinogenesis
Circular RNA circPLK1 promotes breast cancer cell proliferation, migration and invasion by regulating miR-4500/IGF1 axis.
Carcinogenesis
Expression of polo-like kinase in ovarian cancer is associated with histological grade and clinical stage.
Carcinogenesis
Foxm1 expression in prostate epithelial cells is essential for prostate carcinogenesis.
Carcinogenesis
Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors.
Carcinogenesis
Inhibition of Polo-like kinase 4 induces mitotic defects and DNA damage in diffuse large B-cell lymphoma.
Carcinogenesis
Intrahepatic hepatitis B virus large surface antigen induces hepatocyte hyperploidy via failure of cytokinesis.
Carcinogenesis
Knocking down of Polo-like kinase 2 inhibits cell proliferation and induced cell apoptosis in human glioma cells.
Carcinogenesis
LFM-A13, a potent inhibitor of polo-like kinase, inhibits breast carcinogenesis by suppressing proliferation activity and inducing apoptosis in breast tumors of mice.
Carcinogenesis
Low dietary folate initiates intestinal tumors in mice, with altered expression of G2-M checkpoint regulators polo-like kinase 1 and cell division cycle 25c.
Carcinogenesis
Mutual regulation between Polo-like kinase 3 and SIAH2 E3 ubiquitin ligase defines a regulatory network that fine-tunes the cellular response to hypoxia and nickel.
Carcinogenesis
PLK-1 Targeted Inhibitors and Their Potential against Tumorigenesis.
Carcinogenesis
PLK-1: Angel or devil for cell cycle progression.
Carcinogenesis
Plk1-mediated phosphorylation of Topors regulates p53 stability.
Carcinogenesis
Polo-like kinase 1 depletion induces DNA damage in early S prior to caspase activation.
Carcinogenesis
Polo-Like Kinase 1 phosphorylates and stabilizes KLF4 to promote tumorigenesis in nasopharyngeal carcinoma.
Carcinogenesis
Polo-like kinase 3, hypoxic responses, and tumorigenesis.
Carcinogenesis
Regulatory functional territory of PLK-1 and their substrates beyond mitosis.
Carcinogenesis
Selectivity-determining residues in Plk1.
Carcinogenesis
Splicing Regulator p54nrb /NONO Enhances Carcinogenesis Through Oncogenic Isoform Switch of BIN1 in Hepatocellular Carcinoma.
Carcinogenesis
The balance of Polo-like kinase 1 in tumorigenesis.
Carcinogenesis
The deregulated promoter methylation of the Polo-like kinases as a potential biomarker in hematological malignancies.
Carcinogenesis
The MicroRNA3686 Inhibits the Proliferation of Pancreas Carcinoma Cell Line by Targeting the Polo-Like Kinase 1.
Carcinogenesis
The role of polo-like kinase 1 in carcinogenesis: cause or consequence?
Carcinogenesis
Theoretical model of treatment strategies for clear cell carcinoma of the ovary: Focus on perspectives.
Carcinogenesis
Thymoquinone blocks pSer/pThr recognition by Plk1 Polo-box domain as a phosphate mimic.
Carcinogenesis
[Enhancive Effect of PLK1 Gene Silencing onSensitivity of K562/A02 Cells to Adriamycin.]
Carcinogenesis
p53 is not directly relevant to the response of Polo-like kinase 1 inhibitors.
Carcinoma
A PLK1 kinase inhibitor enhances the chemosensitivity of cisplatin by inducing pyroptosis in oesophageal squamous cell carcinoma.
Carcinoma
Antitumoral effect of PLK-1-inhibitor BI2536 in combination with cisplatin and docetaxel in squamous cell carcinoma cell lines of the head and neck.
Carcinoma
Association of Polo-Like Kinase 3 and PhosphoT273 Caspase 8 Levels With Disease-Related Outcomes Among Cervical Squamous Cell Carcinoma Patients Treated With Chemoradiation and Brachytherapy.
Carcinoma
BUBR1 overexpression predicts disease-specific survival after nephroureterectomy in patients with upper tract urothelial carcinoma.
Carcinoma
Cathepsin E, maspin, Plk1, and survivin are promising prognostic protein markers for progression in non-muscle invasive bladder cancer.
Carcinoma
Effects of marine sponge extracts on mitogen-activated protein kinase (MAPK/ERK(1,2)) activity in SW-13 human adrenal carcinoma cells.
Carcinoma
Evaluation of Polo-like kinase 1 as a potential therapeutic target in Merkel cell carcinoma.
Carcinoma
Expression of polo-like kinase 1 (PLK1) protein predicts the survival of patients with gastric carcinoma.
Carcinoma
High expression of polo-like kinase 1 is associated with the metastasis and recurrence in urothelial carcinoma of bladder.
Carcinoma
Immunohistochemical expression of polo-like kinase 1 in oral squamous cell carcinoma and oral submucous fibrosis.
Carcinoma
In vitro targeting of Polo-like kinase 1 in bladder carcinoma: comparative effects of four potent inhibitors.
Carcinoma
Molecular Targets of Genistein and Its Related Flavonoids to Exert Anticancer Effects.
Carcinoma
Oncogenic effect of Polo-like kinase 1 expression in human gastric carcinomas.
Carcinoma
Overexpression of cyclooxygenase-2 in human prostate carcinoma and prostatic intraepithelial neoplasia-association with increased expression of Polo-like kinase-1.
Carcinoma
PLK1 Is transcriptionally activated by NF-?B during cell detachment and enhances anoikis resistance through inhibiting ?-catenin degradation in esophageal squamous cell carcinoma.
Carcinoma
PLK1 promotes epithelial-mesenchymal transition and metastasis of gastric carcinoma cells.
Carcinoma
Polo-like kinase 1 as a promising diagnostic biomarker and potential therapeutic target for hepatocellular carcinoma.
Carcinoma
Polo-like kinase 1 expression is suppressed by CCAAT/enhancer-binding protein ? to mediate colon carcinoma cell differentiation and apoptosis.
Carcinoma
Polo-like kinase 1 overexpression is an early event in the progression of papillary carcinoma.
Carcinoma
Polo-like kinase 3 and phosphoT273 caspase-8 are associated with improved local tumor control and survival in patients with anal carcinoma treated with concomitant chemoradiotherapy.
Carcinoma
Polo-like kinase isoform expression is a prognostic factor in ovarian carcinoma.
Carcinoma
Prognostic significance of polo-like kinase (PLK) expression in squamous cell carcinomas of the head and neck.
Carcinoma
Prognostic significance of polo-like kinase expression in esophageal carcinoma.
Carcinoma
PSK, a novel STE20-like kinase derived from prostatic carcinoma that activates the c-Jun N-terminal kinase mitogen-activated protein kinase pathway and regulates actin cytoskeletal organization.
Carcinoma
RNA interference-mediated silencing of the polo-like kinase 1 gene enhances chemosensitivity to gemcitabine in pancreatic adenocarcinoma cells.
Carcinoma
Targeted inhibition of Polo-like kinase 1 by a novel small-molecule inhibitor induces mitotic catastrophe and apoptosis in human bladder cancer cells.
Carcinoma
Targeting polo-like kinase 1 enhances radiation efficacy for head-and-neck squamous cell carcinoma.
Carcinoma
The clinical and prognostic value of polo-like kinase 1 in lung squamous cell carcinoma patients: immunohistochemical analysis.
Carcinoma
The expression of PLK-1 in cervical carcinoma: a possible target for enhancing chemosensitivity.
Carcinoma
The MicroRNA3686 Inhibits the Proliferation of Pancreas Carcinoma Cell Line by Targeting the Polo-Like Kinase 1.
Carcinoma, Ehrlich Tumor
Effect of protein kinase inhibitors on activity of mammalian small heat-shock protein (HSP25) kinase.
Carcinoma, Hepatocellular
A cell-penetrating ARF peptide inhibitor of FoxM1 in mouse hepatocellular carcinoma treatment.
Carcinoma, Hepatocellular
Aberrant Polo-like kinase 1-Cdc25A pathway in metastatic hepatocellular carcinoma.
Carcinoma, Hepatocellular
An Open-Label, Multicenter, Phase I, Dose Escalation Study with Phase II Expansion Cohort to Determine the Safety, Pharmacokinetics, and Preliminary Antitumor Activity of Intravenous TKM-080301 in Subjects with Advanced Hepatocellular Carcinoma.
Carcinoma, Hepatocellular
Comprehensive and Integrative Analysis Reveals the Diagnostic, Clinicopathological and Prognostic Significance of Polo-Like Kinase 1 in Hepatocellular Carcinoma.
Carcinoma, Hepatocellular
Discovery of methyl 3-((2-((1-(dimethylglycyl)-5-methoxyindolin-6-yl)amino)-5-(trifluoro-methyl) pyrimidin-4-yl)amino)thiophene-2-carboxylate as a potent and selective polo-like kinase 1 (PLK1) inhibitor for combating hepatocellular carcinoma.
Carcinoma, Hepatocellular
Downregulation of polo-like kinase 4 in hepatocellular carcinoma associates with poor prognosis.
Carcinoma, Hepatocellular
Dual targeting of Polo-like kinase 1 and baculoviral inhibitor of apoptosis repeat-containing 5 in TP53-mutated hepatocellular carcinoma.
Carcinoma, Hepatocellular
High expression of polo-like kinase 1 is associated with early development of hepatocellular carcinoma.
Carcinoma, Hepatocellular
Inhibition of Polo-Like Kinase 1 by BI2536 Reverses the Multidrug Resistance of Human Hepatoma Cells In Vitro and In Vivo.
Carcinoma, Hepatocellular
Intravenous liposomal delivery of the short hairpin RNAs against Plk1 controls the growth of established human hepatocellular carcinoma.
Carcinoma, Hepatocellular
Polo-like kinase 1 as a promising diagnostic biomarker and potential therapeutic target for hepatocellular carcinoma.
Carcinoma, Hepatocellular
Polo-like kinase 1 contributes to the tumorigenicity of BEL-7402 hepatoma cells via regulation of Survivin expression.
Carcinoma, Hepatocellular
Polo-like kinase 1, a new therapeutic target in hepatocellular carcinoma.
Carcinoma, Hepatocellular
Polo-like Kinase 1-targeting Chitosan Nanoparticles Suppress the Progression of Hepatocellular Carcinoma.
Carcinoma, Hepatocellular
[Expression and prognostic value of Polo-like kinase 1, E-cadherin in the patients with hepatocellular carcinoma]
Carcinoma, Medullary
Polo-like kinase 1 expression in medullary carcinoma of the thyroid: its relationship with clinicopathological features.
Carcinoma, Merkel Cell
Evaluation of Polo-like kinase 1 as a potential therapeutic target in Merkel cell carcinoma.
Carcinoma, Non-Small-Cell Lung
Combined blockade of polo-like kinase and pan-RAF is effective against NRAS-mutant non-small cell lung cancer cells.
Carcinoma, Non-Small-Cell Lung
Comparison of different semi-mechanistic models for chemotherapy-related neutropenia: application to BI 2536 a Plk-1 inhibitor.
Carcinoma, Non-Small-Cell Lung
Comprehensive Biomarker Analyses in Patients with Advanced or Metastatic Non-Small Cell Lung Cancer Prospectively Treated with the Polo-Like Kinase 1 Inhibitor BI2536.
Carcinoma, Non-Small-Cell Lung
Epithelial-Mesenchymal Transition Predicts Polo-Like Kinase 1 Inhibitor-Mediated Apoptosis in Non-Small Cell Lung Cancer.
Carcinoma, Non-Small-Cell Lung
MicroRNA-100 is a potential molecular marker of non-small cell lung cancer and functions as a tumor suppressor by targeting polo-like kinase 1.
Carcinoma, Non-Small-Cell Lung
Overexpression of polo-like kinase 1 and its clinical significance in human non-small cell lung cancer.
Carcinoma, Non-Small-Cell Lung
PLK1 and EGFR targeted nanoparticle as a radiation sensitizer for non-small cell lung cancer.
Carcinoma, Non-Small-Cell Lung
Polo-like kinase 1 inhibition diminishes acquired resistance to epidermal growth factor receptor inhibition in non-small cell lung cancer with T790M mutations.
Carcinoma, Non-Small-Cell Lung
Polo-like kinase 1 inhibitor BI2536 causes mitotic catastrophe following activation of the spindle assembly checkpoint in non-small cell lung cancer cells.
Carcinoma, Non-Small-Cell Lung
Polo-like kinase 4 correlates with greater tumor size, lymph node metastasis and confers poor survival in non-small cell lung cancer.
Carcinoma, Non-Small-Cell Lung
Prognostic significance of polo-like kinase (PLK) expression in non-small cell lung cancer.
Carcinoma, Non-Small-Cell Lung
Radiosensitization of Non-Small Cell Lung Cancer Cells by the Plk1 Inhibitor Volasertib Is Dependent on the p53 Status.
Carcinoma, Non-Small-Cell Lung
Sepantronium is a DNA damaging agent that synergizes with PLK1 inhibitor volasertib.
Carcinoma, Non-Small-Cell Lung
Targeting Polo-like kinase 1 and TRAIL enhances apoptosis in non-small cell lung cancer.
Carcinoma, Non-Small-Cell Lung
The efficacy and safety of BI 2536, a novel Plk-1 inhibitor, in patients with stage IIIB/IV non-small cell lung cancer who had relapsed after, or failed, chemotherapy: results from an open-label, randomized phase II clinical trial.
Carcinoma, Non-Small-Cell Lung
Therapeutic targeting of polo-like kinase 1 using RNA-interfering nanoparticles (iNOPs) for the treatment of non-small cell lung cancer.
Carcinoma, Non-Small-Cell Lung
Towards Prognostic Profiling of Non-Small Cell Lung Cancer: New Perspectives on the Relevance of Polo-Like Kinase 1 Expression, the TP53 Mutation Status and Hypoxia.
Carcinoma, Ovarian Epithelial
Mitotic Exit Dysfunction through the Deregulation of APC/C Characterizes Cisplatin-Resistant State in Epithelial Ovarian Cancer.
Carcinoma, Papillary
Polo-like kinase 1 overexpression is an early event in the progression of papillary carcinoma.
Carcinoma, Squamous Cell
Antitumoral effect of PLK-1-inhibitor BI2536 in combination with cisplatin and docetaxel in squamous cell carcinoma cell lines of the head and neck.
Carcinoma, Squamous Cell
Association of Polo-Like Kinase 3 and PhosphoT273 Caspase 8 Levels With Disease-Related Outcomes Among Cervical Squamous Cell Carcinoma Patients Treated With Chemoradiation and Brachytherapy.
Carcinoma, Squamous Cell
Prognostic significance of polo-like kinase (PLK) expression in squamous cell carcinomas of the head and neck.
Carcinoma, Squamous Cell
Targeting polo-like kinase 1 enhances radiation efficacy for head-and-neck squamous cell carcinoma.
Carcinoma, Squamous Cell
The clinical and prognostic value of polo-like kinase 1 in lung squamous cell carcinoma patients: immunohistochemical analysis.
Cataract
Histone acetyltransferase and Polo-like kinase 3 inhibitors prevent rat galactose-induced cataract.
Cholangiocarcinoma
Bcl-2 degradation is an additional pro-apoptotic effect of polo-like kinase inhibition in cholangiocarcinoma cells.
Cholangiocarcinoma
Polo-like kinase 1 inhibition as a new therapeutic modality in therapy of cholangiocarcinoma.
Cholangiocarcinoma
Polo-like kinase 2 is a mediator of hedgehog survival signaling in cholangiocarcinoma.
Cholangiocarcinoma
Polo-like kinase 3 is associated with improved overall survival in cholangiocarcinoma.
Cholangiocarcinoma
Therapeutic Rationale to Target Highly Expressed Aurora kinase A Conferring Poor Prognosis in Cholangiocarcinoma.
Colonic Neoplasms
Aberrant Wnt/beta-catenin signaling can induce chromosomal instability in colon cancer.
Colonic Neoplasms
Apoptosis induction with polo-like kinase-1 antisense phosphorothioate oligodeoxynucleotide of colon cancer cell line SW480.
Colonic Neoplasms
Polo-like kinase 1 expression is a prognostic factor in human colon cancer.
Colonic Neoplasms
Preferential Killing of Tetraploid Colon Cancer Cells by Targeting the Mitotic Kinase PLK1.
Colorectal Neoplasms
Antitumor activity of the polo-like kinase inhibitor, TAK-960, against preclinical models of colorectal cancer.
Colorectal Neoplasms
Clinicopathological and prognostic implications of polo-like kinase 1 expression in colorectal cancer: A systematic review and meta-analysis.
Colorectal Neoplasms
Efficient inhibition of human colorectal carcinoma growth by RNA interference targeting polo-like kinase 1 in vitro and in vivo.
Colorectal Neoplasms
Forkhead box D1 promotes proliferation and suppresses apoptosis via regulating polo-like kinase 2 in colorectal cancer.
Colorectal Neoplasms
PLK-1 Expression is Associated with Histopathological Response to Neoadjuvant Therapy of Hepatic Metastasis of Colorectal Carcinoma.
Colorectal Neoplasms
Polo-like kinase 1 (PLK1) is overexpressed in primary colorectal cancers.
Colorectal Neoplasms
Polo-like kinase 1 is overexpressed in colorectal cancer and participates in the migration and invasion of colorectal cancer cells.
Colorectal Neoplasms
Polo-like kinase 2 promotes chemoresistance and predicts limited survival benefit from adjuvant chemotherapy in colorectal cancer.
Colorectal Neoplasms
Polo-like kinase 3 inhibits glucose metabolism in colorectal cancer by targeting HSP90/STAT3/HK2 signaling.
Colorectal Neoplasms
Tazarotene-induced gene 1 interacts with Polo-like kinase 2 and inhibits cell proliferation in HCT116 colorectal cancer cells.
Colorectal Neoplasms
Upregulated Polo-Like Kinase 1 Expression Correlates with Inferior Survival Outcomes in Rectal Cancer.
Colorectal Neoplasms
[Influence of silencing Polo-like kinase 1 on migration and invasion of colorectal cancer cells].
Cystadenoma
Impact of iASPP on chemoresistance through PLK1 and autophagy in ovarian clear cell carcinoma.
DNA Repair-Deficiency Disorders
High expression of polo-like kinase 1 is associated with TP53 inactivation, DNA repair deficiency, and worse prognosis in ER positive Her2 negative breast cancer.
Endometrial Neoplasms
Polo-like kinase (PLK) expression in endometrial carcinoma.
Endometriosis
High expression levels of cyclin B1 and Polo-like kinase 1 in ectopic endometrial cells associated with abnormal cell cycle regulation of endometriosis.
Endometriosis
Impact of iASPP on chemoresistance through PLK1 and autophagy in ovarian clear cell carcinoma.
Esophageal Neoplasms
Elucidation of PLK1 Linked Biomarkers in Oesophageal Cancer Cell Lines: A Step Towards Novel Signaling Pathways by p53 and PLK1- Linked Functions Crosstalk.
Esophageal Neoplasms
Moscatilin Inhibits Growth of Human Esophageal Cancer Xenograft and Sensitizes Cancer Cells to Radiotherapy.
Esophageal Neoplasms
Polo-like kinase 1 regulates cell proliferation and is targeted by miR-593* in esophageal cancer.
Esophageal Neoplasms
Silencing of polo-like kinase (Plk) 1 via siRNA causes inhibition of growth and induction of apoptosis in human esophageal cancer cells.
Esophageal Squamous Cell Carcinoma
A PLK1 kinase inhibitor enhances the chemosensitivity of cisplatin by inducing pyroptosis in oesophageal squamous cell carcinoma.
Esophageal Squamous Cell Carcinoma
PLK1 Is transcriptionally activated by NF-?B during cell detachment and enhances anoikis resistance through inhibiting ?-catenin degradation in esophageal squamous cell carcinoma.
Glioblastoma
A high-content small molecule screen identifies sensitivity of glioblastoma stem cells to inhibition of polo-like kinase 1.
Glioblastoma
Effects of phospholipase Cgamma on Polo-like kinase 1 expression in human glioma cells.
Glioblastoma
GSK461364A, a Polo-Like Kinase-1 Inhibitor Encapsulated in Polymeric Nanoparticles for the Treatment of Glioblastoma Multiforme (GBM).
Glioblastoma
Increased human polo-like kinase-1 expression in gliomas.
Glioblastoma
Inhibition of polo-like kinase 1 in glioblastoma multiforme induces mitotic catastrophe and enhances radiosensitisation.
Glioblastoma
Inhibition of polo-like kinase 1 induces cell cycle arrest and sensitizes glioblastoma cells to ionizing radiation.
Glioblastoma
Multiple forms of protein kinase from normal human brain and glioblastoma.
Glioblastoma
Polo-Like Kinase 1 (PLK1) Inhibition Kills Glioblastoma Multiforme Brain Tumour Cells in Part Through Loss of SOX2 and Delays Tumour Progression in Mice.
Glioblastoma
Polo-like kinase 1 inhibition causes decreased proliferation by cell cycle arrest, leading to cell death in glioblastoma.
Glioblastoma
The enhancement of siPLK1 penetration across BBB and its anti glioblastoma activity in vivo by magnet and transferrin co-modified nanoparticle.
Glioma
Circular RNA ZNF609 promotes the malignant progression of glioma by regulating miR-1224-3p/PLK1 signaling.
Glioma
Clinicopathological significance of Polo-like kinase 1 (PLK1) expression in human malignant glioma.
Glioma
Combined Delivery of Temozolomide and siPLK1 Using Targeted Nanoparticles to Enhance Temozolomide Sensitivity in Glioma.
Glioma
Dual PLK1 and STAT3 inhibition promotes glioblastoma cells apoptosis through MYC.
Glioma
Effects of phospholipase Cgamma on Polo-like kinase 1 expression in human glioma cells.
Glioma
Increased human polo-like kinase-1 expression in gliomas.
Glioma
Knocking down of Polo-like kinase 2 inhibits cell proliferation and induced cell apoptosis in human glioma cells.
Glioma
Long noncoding RNA ENST00000413528 sponges microRNA-593-5p to modulate human glioma growth via polo-like kinase 1.
Glioma
Protein kinase translocation following beta-adrenergic receptor activation in C6 glioma cells.
Glioma
The polo-like kinase 1 inhibitor volasertib synergistically increases radiation efficacy in glioma stem cells.
Head and Neck Neoplasms
Multicentric parallel phase II trial of the polo-like kinase 1 inhibitor BI 2536 in patients with advanced head and neck cancer, breast cancer, ovarian cancer, soft tissue sarcoma and melanoma. The first protocol of the European Organization for Research and Treatment of Cancer (EORTC) Network Of Core Institutes (NOCI).
Hematologic Neoplasms
A novel treatment strategy targeting polo-like kinase 1 in hematological malignancies.
Hematologic Neoplasms
c-Src activation through a TrkA and c-Src interaction is essential for cell proliferation and hematological malignancies.
Hematologic Neoplasms
Epigenetic inactivation implies a tumor suppressor function in hematologic malignancies for Polo-like kinase 2 but not Polo-like kinase 3.
Hematologic Neoplasms
Inhibiting Polo-like kinase 1 causes growth reduction and apoptosis in pediatric acute lymphoblastic leukemia cells.
Hematologic Neoplasms
Polo-like kinase inhibitors in hematologic malignancies.
Hematologic Neoplasms
Therapeutic polo-like kinase 1 inhibition results in mitotic arrest and subsequent cell death of blasts in the bone marrow of AML patients and has similar effects in non-neoplastic cell lines.
Hepatitis B
Polo-like kinase 1 activated by the hepatitis B virus X protein attenuates both the DNA damage checkpoint and DNA repair resulting in partial polyploidy.
Hepatitis B
Polo-like kinase 1 inhibition suppresses hepatitis B virus X protein-induced transformation in an in vitro model of liver cancer progression.
Hepatitis B
Polo-like-kinase 1 is a proviral host-factor for hepatitis B virus replication.
Hepatitis B
[Hepatitis B virus X protein-regulated expression of Plk1].
Hepatitis C
Polo-like kinase 1 is involved in hepatitis C virus replication by hyperphosphorylating NS5A.
Hypogonadism
Male Hypogonadism and Germ Cell Loss Caused by a Mutation in Polo-Like Kinase 4.
Infections
Clinical Significance of Polo-Like Kinase 4 as a Marker for Advanced Tumor Stage and Dismal Prognosis in Patients With Surgical Gastric Cancer.
Infections
In vivo and in vitro phosphorylation of DNA-dependent RNA polymerase of Escherichia coli by bacteriophage-T7-induced protein kinase.
Infections
Inhibition of polo-like kinase 1 (PLK1) facilitates reactivation of gamma-herpesviruses and their elimination.
Infections
Inhibition of Polo-like kinase 1 (PLK1) facilitates the elimination of HIV-1 viral reservoirs in CD4+ T cells ex vivo.
Infections
Protein kinase of bacteriophage T7. 1. Purification.
Infections
Temporal SILAC-based quantitative proteomics identifies host factors involved in chikungunya virus replication.
Infections
[PLK1 Expression in Mantle Cell Lymphoma and Its Clinical Significance].
Infertility, Female
Female infertility in PDE3A(-/-) mice: polo-like kinase 1 (Plk1) may be a target of protein kinase A (PKA) and involved in meiotic arrest of oocytes from PDE3A(-/-) mice.
Insulin Resistance
Insulin Resistance Promotes Parkinson's Disease through Aberrant Expression of ?-Synuclein, Mitochondrial Dysfunction, and Deregulation of the Polo-Like Kinase 2 Signaling.
Kidney Neoplasms
Polo-like kinase 1 is overexpressed in renal cancer and participates in the proliferation and invasion of renal cancer cells.
Leukemia
A systems biology approach for elucidating the interaction of curcumin with Fanconi anemia FANC G protein and the key disease targets of leukemia.
Leukemia
Beta-hydroxyisovalerylshikonin induces apoptosis in human leukemia cells by inhibiting the activity of a polo-like kinase 1 (PLK1).
Leukemia
c-Src activation through a TrkA and c-Src interaction is essential for cell proliferation and hematological malignancies.
Leukemia
Efficacy of the polo-like kinase inhibitor rigosertib, alone or in combination with Abelson tyrosine kinase inhibitors, against break point cluster region-c-Abelson-positive leukemia cells.
Leukemia
Enhanced polo-like kinase 1 expression in myelodysplastic syndromes.
Leukemia
PLK-1 Expression is Associated with Histopathological Response to Neoadjuvant Therapy of Hepatic Metastasis of Colorectal Carcinoma.
Leukemia
PLK1 inhibitors synergistically potentiate HDAC inhibitor lethality in imatinib mesylate-sensitive or -resistant BCR/ABL+ leukemia cells in vitro and in vivo.
Leukemia
Polo-like kinase-1 as novel target in neoplastic mast cells: demonstration of growth-inhibitory effects of siRNA and the Polo-like kinase-1 targeting drug BI 2536.
Leukemia
Polo-like kinases in AML.
Leukemia
Targeted Polo-like Kinase Inhibition Combined With Aurora Kinase Inhibition in Pediatric Acute Leukemia Cells.
Leukemia
Targeting polo-like kinase 1 suppresses essential functions of alloreactive T cells.
Leukemia
TrkC promotes survival and growth of leukemia cells through Akt-mTOR-Dependent Up-Regulation of PLK-1 and Twist-1.
Leukemia
[Expression of plk-1 gene in acute leukemia patients and its significance]
Leukemia, Mast-Cell
Polo-like kinase-1 as novel target in neoplastic mast cells: demonstration of growth-inhibitory effects of siRNA and the Polo-like kinase-1 targeting drug BI 2536.
Leukemia, Myelogenous, Chronic, BCR-ABL Positive
FOXM1 Transcription Factor: A New Component of Chronic Myeloid Leukemia Stem Cell Proliferation Advantage.
Leukemia, Myelogenous, Chronic, BCR-ABL Positive
Polo-like kinase 1 (Plk1) as a novel drug target in chronic myeloid leukemia: overriding imatinib resistance with the Plk1 inhibitor BI 2536.
Leukemia, Myeloid
Polo-like kinase-1 as novel target in neoplastic mast cells: demonstration of growth-inhibitory effects of siRNA and the Polo-like kinase-1 targeting drug BI 2536.
Leukemia, Myeloid, Acute
A phase 1b study of onvansertib, a novel oral PLK1 inhibitor, in combination therapy for patients with relapsed or refractory acute myeloid leukemia.
Leukemia, Myeloid, Acute
Adjunctive Volasertib in Patients With Acute Myeloid Leukemia not Eligible for Standard Induction Therapy: A Randomized, Phase 3 Trial.
Leukemia, Myeloid, Acute
Phase I trial of volasertib, a Polo-like kinase inhibitor, in Japanese patients with acute myeloid leukemia.
Leukemia, Myeloid, Acute
Polo-like kinase 1 is overexpressed in acute myeloid leukemia and its inhibition preferentially targets the proliferation of leukemic cells.
Leukemia, Myeloid, Acute
Polo-like kinase 2 (SNK/PLK2) is a novel epigenetically regulated gene in acute myeloid leukemia and myelodysplastic syndromes: genetic and epigenetic interactions.
Leukemia, Myeloid, Acute
Polo-like kinase inhibition as a therapeutic target in acute myeloid leukemia.
Leukemia, Myeloid, Acute
Polo-like kinase inhibitor volasertib marginally enhances the efficacy of the novel Fc-engineered anti-CD33 antibody BI 836858 in acute myeloid leukemia.
Leukemia, Myeloid, Acute
Protein targeting chimeric molecules specific for dual bromodomain 4 (BRD4) and Polo-like kinase 1 (PLK1) proteins in acute myeloid leukemia cells.
Leukemia, Myeloid, Acute
Radotinib inhibits mitosis entry in acute myeloid leukemia cells via suppression of Aurora kinase A expression.
Leukemia, Myeloid, Acute
RNAi prodrugs decrease elevated mRNA levels of Polo-like kinase 1 in ex vivo cultured primary cells from pediatric acute myeloid leukemia patients.
Leukemia, Myeloid, Acute
Synergistic activity of BET inhibitor BI 894999 with PLK inhibitor volasertib in AML in vitro and in vivo.
Leukemia, Myeloid, Acute
Targeted therapy of acute myeloid leukemia.
Leukemia, Myeloid, Acute
Targeting polo-like kinase 1 in acute myeloid leukemia.
Liver Cirrhosis
Polo-like kinase 1 as a promising diagnostic biomarker and potential therapeutic target for hepatocellular carcinoma.
Liver Neoplasms
Escheriosome-mediated cytosolic delivery of PLK1-specific siRNA: potential in treatment of liver cancer in BALB/c mice.
Liver Neoplasms
Polo-like kinase 1 inhibition suppresses hepatitis B virus X protein-induced transformation in an in vitro model of liver cancer progression.
Lung Neoplasms
Absolute quantification of protein and post-translational modification abundance with stable isotope-labeled synthetic peptides.
Lung Neoplasms
Administration of PLK-1 small interfering RNA with atelocollagen prevents the growth of liver metastases of lung cancer.
Lung Neoplasms
An open-label, phase II study of the polo-like kinase-1 (Plk-1) inhibitor, BI 2536, in patients with relapsed small cell lung cancer (SCLC).
Lung Neoplasms
Cell cycle inhibitors for the treatment of NSCLC.
Lung Neoplasms
Combined blockade of polo-like kinase and pan-RAF is effective against NRAS-mutant non-small cell lung cancer cells.
Lung Neoplasms
Comparison of different semi-mechanistic models for chemotherapy-related neutropenia: application to BI 2536 a Plk-1 inhibitor.
Lung Neoplasms
Comprehensive Biomarker Analyses in Patients with Advanced or Metastatic Non-Small Cell Lung Cancer Prospectively Treated with the Polo-Like Kinase 1 Inhibitor BI2536.
Lung Neoplasms
Effect of antisense RNA targeting polo-like kinase 1 on cell cycle and proliferation in A549 cells.
Lung Neoplasms
Effect of antisense RNA targeting Polo-like kinase 1 on cell growth in A549 lung cancer cells.
Lung Neoplasms
Epithelial-Mesenchymal Transition Predicts Polo-Like Kinase 1 Inhibitor-Mediated Apoptosis in Non-Small Cell Lung Cancer.
Lung Neoplasms
Inhibiting polo-like kinase 1 enhances radiosensitization via modulating DNA repair proteins in non-small-cell lung cancer.
Lung Neoplasms
Inhibition of Plk1 and Pin1 by 5'-nitro-indirubinoxime suppresses human lung cancer cells.
Lung Neoplasms
In vitro study of the Polo-like kinase 1 inhibitor volasertib in non-small-cell lung cancer reveals a role for the tumor suppressor p53.
Lung Neoplasms
MicroRNA-100 is a potential molecular marker of non-small cell lung cancer and functions as a tumor suppressor by targeting polo-like kinase 1.
Lung Neoplasms
Non-canonical cMet regulation by vimentin mediates Plk1 inhibitor-induced apoptosis.
Lung Neoplasms
Overexpression of polo-like kinase 1 and its clinical significance in human non-small cell lung cancer.
Lung Neoplasms
pH-responsive hybrid nanoparticle with enhanced dissociation characteristic for siRNA delivery.
Lung Neoplasms
PLK1 and EGFR targeted nanoparticle as a radiation sensitizer for non-small cell lung cancer.
Lung Neoplasms
Polo-like kinase 1 inhibition diminishes acquired resistance to epidermal growth factor receptor inhibition in non-small cell lung cancer with T790M mutations.
Lung Neoplasms
Polo-like kinase 1 inhibitor BI 6727 induces DNA damage and exerts strong antitumor activity in small cell lung cancer.
Lung Neoplasms
Polo-like kinase 1 inhibitor BI2536 causes mitotic catastrophe following activation of the spindle assembly checkpoint in non-small cell lung cancer cells.
Lung Neoplasms
Polo-like kinase 4 correlates with greater tumor size, lymph node metastasis and confers poor survival in non-small cell lung cancer.
Lung Neoplasms
Polo-like kinase 4 inhibition produces polyploidy and apoptotic death of lung cancers.
Lung Neoplasms
Prognostic significance of polo-like kinase (PLK) expression in non-small cell lung cancer.
Lung Neoplasms
Radiosensitization of Non-Small Cell Lung Cancer Cells by the Plk1 Inhibitor Volasertib Is Dependent on the p53 Status.
Lung Neoplasms
RNA interference against polo-like kinase-1 in advanced non-small cell lung cancers.
Lung Neoplasms
Sepantronium is a DNA damaging agent that synergizes with PLK1 inhibitor volasertib.
Lung Neoplasms
Targeting Polo-like kinase 1 and TRAIL enhances apoptosis in non-small cell lung cancer.
Lung Neoplasms
The efficacy and safety of BI 2536, a novel Plk-1 inhibitor, in patients with stage IIIB/IV non-small cell lung cancer who had relapsed after, or failed, chemotherapy: results from an open-label, randomized phase II clinical trial.
Lung Neoplasms
Therapeutic targeting of polo-like kinase 1 using RNA-interfering nanoparticles (iNOPs) for the treatment of non-small cell lung cancer.
Lung Neoplasms
Towards Prognostic Profiling of Non-Small Cell Lung Cancer: New Perspectives on the Relevance of Polo-Like Kinase 1 Expression, the TP53 Mutation Status and Hypoxia.
Lung Neoplasms
[Effect of antisense RNA targeting Polo-like kinase 1 on cell cycle of lung cancer cell line A549]
Lymphatic Metastasis
Nuclear cyclin B1 in human breast carcinoma as a potent prognostic factor.
Lymphatic Metastasis
Overexpression of polo-like kinase 1 and its clinical significance in human non-small cell lung cancer.
Lymphatic Metastasis
Polo-like kinase 4 correlates with greater tumor size, lymph node metastasis and confers poor survival in non-small cell lung cancer.
Lymphoma
Absence of tumor-specific over-expression of Polo-like kinase 1 (Plk1) in major non-Hodgkin lymphoma and relatively low expression of Plk1 in nasal NK/T cell lymphoma.
Lymphoma
Altered regulation of cyclic AMP-dependent protein kinase in a mouse lymphoma cell line.
Lymphoma
Enhanced polo-like kinase 1 expression in myelodysplastic syndromes.
Lymphoma
Expression of PLK1 and survivin in non-Hodgkinos lymphoma treated with CHOP.
Lymphoma
Expression of Polo-Like Kinase (PLK1) in non-Hodgkin's lymphomas.
Lymphoma
Kinase Inhibitor Indole Derivatives as Anticancer Agents: A Patent Review.
Lymphoma
PLK1: a promising and previously unexplored target in double-hit lymphoma.
Lymphoma
Polo-like kinase 1 (PLK1) expression is associated with cell proliferative activity and cdc2 expression in malignant lymphoma of the thyroid.
Lymphoma
Polo-like kinase 1 is essential to DNA damage recovery.
Lymphoma
Polo-like kinase 2 (SNK/PLK2) is a novel epigenetically regulated gene in acute myeloid leukemia and myelodysplastic syndromes: genetic and epigenetic interactions.
Lymphoma
Polo-like-kinase 1 (PLK-1) and c-myc inhibition with the dual kinase-bromodomain inhibitor volasertib in aggressive lymphomas.
Lymphoma
Resveratrol activates DNA damage response through inhibition of polo-like kinase 1 (PLK1) in natural killer/T cell lymphoma.
Lymphoma
Subunit interaction in cyclic AMP-dependent protein kinase of mutant lymphoma cells.
Lymphoma
Synergistic interactions between PLK1 and HDAC inhibitors in non-Hodgkin's lymphoma cells occur in vitro and in vivo and proceed through multiple mechanisms.
Lymphoma, B-Cell
Inhibition of Polo-like kinase 4 induces mitotic defects and DNA damage in diffuse large B-cell lymphoma.
Lymphoma, B-Cell
PLK1: a promising and previously unexplored target in double-hit lymphoma.
Lymphoma, B-Cell
Synergistic interactions between PLK1 and HDAC inhibitors in non-Hodgkin's lymphoma cells occur in vitro and in vivo and proceed through multiple mechanisms.
Lymphoma, B-Cell
The contribution of MYC and PLK1 expression to proliferative capacity in diffuse large B-cell lymphoma.
Lymphoma, Large B-Cell, Diffuse
Inhibition of Polo-like kinase 4 induces mitotic defects and DNA damage in diffuse large B-cell lymphoma.
Lymphoma, Large B-Cell, Diffuse
Synergistic interactions between PLK1 and HDAC inhibitors in non-Hodgkin's lymphoma cells occur in vitro and in vivo and proceed through multiple mechanisms.
Lymphoma, Mantle-Cell
Synergistic interactions between PLK1 and HDAC inhibitors in non-Hodgkin's lymphoma cells occur in vitro and in vivo and proceed through multiple mechanisms.
Lymphoma, Non-Hodgkin
Absence of tumor-specific over-expression of Polo-like kinase 1 (Plk1) in major non-Hodgkin lymphoma and relatively low expression of Plk1 in nasal NK/T cell lymphoma.
Lymphoma, Non-Hodgkin
Polo-like kinase 1 as a new target for non-Hodgkin's lymphoma treatment.
Lymphoma, Non-Hodgkin
The Plk1 inhibitor BI 2536 in patients with refractory or relapsed non-Hodgkin's lymphoma: A Phase I, open-label, single dose-escalation study.
Lymphoma, T-Cell, Cutaneous
Polo-like kinase 1 (Plk1) in cutaneous T-cell lymphoma.
Lymphoma, T-Cell, Cutaneous
Polo-like kinase 1 (Plk1) is expressed by cutaneous T-cell lymphomas (CTCLs) and its down-regulation promotes cell cycle arrest and apoptosis.
Lymphoproliferative Disorders
The role of aurora A and polo-like kinases in high-risk lymphomas.
Mastocytosis, Systemic
Polo-like kinase-1 as novel target in neoplastic mast cells: demonstration of growth-inhibitory effects of siRNA and the Polo-like kinase-1 targeting drug BI 2536.
Medulloblastoma
A Regulatory Loop of FBXW7-MYC-PLK1 Controls Tumorigenesis of MYC-Driven Medulloblastoma.
Medulloblastoma
Comparative Effects of Polo-Like Kinase 1 Inhibitors as Monotherapy and in Combination with Current Treatments for Medulloblastoma.
Medulloblastoma
Inhibition of polo-like kinase 4 (PLK4): a new therapeutic option for rhabdoid tumors and pediatric medulloblastoma.
Medulloblastoma
Personalizing the treatment of pediatric medulloblastoma: Polo-like kinase PLK1 as a molecular target in high-risk children.
Medulloblastoma
Polo-like kinase 1 (PLK1) inhibition suppresses cell growth and enhances radiation sensitivity in medulloblastoma cells.
Medulloblastoma
The polo-like kinase 4 gene (PLK4) is overexpressed in pediatric medulloblastoma.
Melanoma
Combined Inhibition of MEK and Plk1 Has Synergistic Antitumor Activity in NRAS Mutant Melanoma.
Melanoma
Downregulation of Polo-like kinase-1 (PLK-1) expression is associated with poor clinical outcome in uveal melanoma patients.
Melanoma
Expression of polo-like kinase (PLK1) in thin melanomas: a novel marker of metastatic disease.
Melanoma
In Vivo ERK1/2 Reporter Predictively Models Response and Resistance to Combined BRAF and MEK Inhibitors in Melanoma.
Melanoma
Kinase inhibitor library screening identifies synergistic drug combinations effective in sensitive and resistant melanoma cells.
Melanoma
Large-Scale Label-Free Comparative Proteomics Analysis of Polo-Like Kinase 1 Inhibition via the Small-Molecule Inhibitor BI 6727 (Volasertib) in BRAF(V600E) Mutant Melanoma Cells.
Melanoma
Multicentric parallel phase II trial of the polo-like kinase 1 inhibitor BI 2536 in patients with advanced head and neck cancer, breast cancer, ovarian cancer, soft tissue sarcoma and melanoma. The first protocol of the European Organization for Research and Treatment of Cancer (EORTC) Network Of Core Institutes (NOCI).
Melanoma
Multiple agminated Spitz nevi arising on a café au lait macule: review of the literature with contribution of another case.
Melanoma
Playing Polo-Like Kinase in NRAS-Mutant Melanoma.
Melanoma
PLK1 and NOTCH Positively Correlate in Melanoma and Their Combined Inhibition Results in Synergistic Modulations of Key Melanoma Pathways.
Melanoma
Polo-like kinase 1 is a potential therapeutic target in human melanoma.
Melanoma
Polo-like kinase-1 immunoreactivity is associated with metastases in cutaneous melanoma.
Melanoma
Small molecule inhibition of polo-like kinase 1 by volasertib (BI 6727) causes significant melanoma growth delay and regression in vivo.
Melanoma
Targeted Depletion of Polo-Like Kinase (Plk) 1 Through Lentiviral shRNA or a Small-Molecule Inhibitor Causes Mitotic Catastrophe and Induction of Apoptosis in Human Melanoma Cells.
Melanoma
Targeted knockdown of polo-like kinase 1 alters metabolic regulation in melanoma.
Melanoma
The role of polo-like kinase 3 in the response of BRAF-mutant cells to targeted anticancer therapies.
Mesothelioma, Malignant
A combination of a DNA-chimera siRNA against PLK-1 and zoledronic acid suppresses the growth of malignant mesothelioma cells in vitro.
Microcephaly
Microduplication of the ARID1A gene causes intellectual disability with recognizable syndromic features.
Microcephaly
Overexpression of the PLK4 Gene as a Novel Strategy for the Treatment of Autosomal Recessive Microcephaly by Improving Centrosomal Dysfunction.
Mouth Neoplasms
ER maleate is a novel anticancer agent in oral cancer: Implications for cancer therapy.
Mouth Neoplasms
Kinome-Wide Screening with Small Interfering RNA Identified Polo-like Kinase 1 as a Key Regulator of Proliferation in Oral Cancer Cells.
Multiple Myeloma
Expression, adverse prognostic significance and therapeutic small molecule inhibition of Polo-like kinase 1 in multiple myeloma.
Multiple Myeloma
Microenvironmental influence on pre-clinical activity of polo-like kinase inhibition in multiple myeloma: implications for clinical translation.
Multiple Myeloma
Polo-like kinase 2 (SNK/PLK2) is a novel epigenetically regulated gene in acute myeloid leukemia and myelodysplastic syndromes: genetic and epigenetic interactions.
Multiple Myeloma
The polo-like kinase inhibitor BI 2536 exhibits potent activity against malignant plasma cells and represents a novel therapy in multiple myeloma.
Mumps
Mumps Virus Nucleoprotein Enhances Phosphorylation of the Phosphoprotein by Polo-Like Kinase 1.
Myelodysplastic Syndromes
Enhanced polo-like kinase 1 expression in myelodysplastic syndromes.
Myelodysplastic Syndromes
Polo-like kinase 2 (SNK/PLK2) is a novel epigenetically regulated gene in acute myeloid leukemia and myelodysplastic syndromes: genetic and epigenetic interactions.
Nasopharyngeal Carcinoma
Polo-Like Kinase 1 phosphorylates and stabilizes KLF4 to promote tumorigenesis in nasopharyngeal carcinoma.
Nasopharyngeal Carcinoma
Polo-like kinase inhibitor Ro5203280 has potent antitumor activity in nasopharyngeal carcinoma.
Nasopharyngeal Carcinoma
Up-regulation of Polo-like Kinase 1 in nasopharyngeal carcinoma tissues: a comprehensive investigation based on RNA-sequencing, gene chips, and in-house tissue arrays.
Neoplasm Metastasis
Administration of PLK-1 small interfering RNA with atelocollagen prevents the growth of liver metastases of lung cancer.
Neoplasm Metastasis
Anticancer effects on TACC3 by treatment of paclitaxel in HPV-18 positive cervical carcinoma cells.
Neoplasm Metastasis
Battle of the eternal rivals: restoring functional p53 and inhibiting Polo-like kinase 1 as cancer therapy.
Neoplasm Metastasis
Clinical Significance of Polo-Like Kinase 4 as a Marker for Advanced Tumor Stage and Dismal Prognosis in Patients With Surgical Gastric Cancer.
Neoplasm Metastasis
Down-regulation of Polo-like kinase 4 (PLK4) induces G1 arrest via activation of the p38/p53/p21 signaling pathway in bladder cancer.
Neoplasm Metastasis
Essential Role of Polo-like Kinase 1 (Plk1) Oncogene in Tumor Growth and Metastasis of Tamoxifen-Resistant Breast Cancer.
Neoplasm Metastasis
Foxm1 expression in prostate epithelial cells is essential for prostate carcinogenesis.
Neoplasm Metastasis
High expression of polo-like kinase 1 is associated with the metastasis and recurrence in urothelial carcinoma of bladder.
Neoplasm Metastasis
Nuclear cyclin B1 in human breast carcinoma as a potent prognostic factor.
Neoplasm Metastasis
Overexpression of polo-like kinase 1 and its clinical significance in human non-small cell lung cancer.
Neoplasm Metastasis
Phosphorylation of human enhancer filamentation 1 (HEF1) stimulates interaction with Polo-like kinase 1 leading to HEF1 localization to focal adhesions.
Neoplasm Metastasis
PLK-1 Expression is Associated with Histopathological Response to Neoadjuvant Therapy of Hepatic Metastasis of Colorectal Carcinoma.
Neoplasm Metastasis
PLK1 promotes epithelial-mesenchymal transition and metastasis of gastric carcinoma cells.
Neoplasm Metastasis
Polo-like kinase 1 is a potential therapeutic target in human melanoma.
Neoplasm Metastasis
Polo-like kinase 3 is associated with poor prognosis and regulates proliferation and metastasis in prostate cancer.
Neoplasm Metastasis
Polo-like kinase 4 correlates with greater tumor size, lymph node metastasis and confers poor survival in non-small cell lung cancer.
Neoplasm Metastasis
Polo-like kinase-1 immunoreactivity is associated with metastases in cutaneous melanoma.
Neoplasm Metastasis
Regulation of E2F Transcription Factor 3 by microRNA-152 Modulates Gastric Cancer Invasion and Metastasis.
Neoplasm Metastasis
Role of NEK2A in Human Cancer and Its Therapeutic Potentials.
Neoplasm Metastasis
The Emerging Role of Polo-Like Kinase 1 in Epithelial-Mesenchymal Transition and Tumor Metastasis.
Neoplasm Metastasis
Wnt5a-induced docking of Plk1 on HEF1 promotes HEF1 translocation and tumorigenesis.
Neoplasm, Residual
Promoting tumor penetration of nanoparticles for cancer stem cell therapy by TGF-? signaling pathway inhibition.
Neoplasms
A cell-penetrating ARF peptide inhibitor of FoxM1 in mouse hepatocellular carcinoma treatment.
Neoplasms
A Cereblon Modulator CC-885 Induces CRBN- and p97-Dependent PLK1 Degradation and Synergizes with Volasertib to Suppress Lung Cancer.
Neoplasms
A combination therapy for KRAS-mutant lung cancer by targeting synthetic lethal partners of mutant KRAS.
Neoplasms
A fluorescence polarization assay for the discovery of inhibitors of the polo-box domain of polo-like kinase 1.
Neoplasms
A functional screening of the kinome identifies the Polo-like kinase 4 as a potential therapeutic target for malignant rhabdoid tumors, and possibly, other embryonal tumors of the brain.
Neoplasms
A high-throughput assay based on fluorescence polarization for inhibitors of the polo-box domain of polo-like kinase 1.
Neoplasms
A novel anti-tumor inhibitor identified by virtual screen with PLK1 structure and zebrafish assay.
Neoplasms
A phase I study of two dosing schedules of volasertib (BI 6727), an intravenous polo-like kinase inhibitor, in patients with advanced solid malignancies.
Neoplasms
A phase I study of volasertib combined with afatinib, in advanced solid tumors.
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A phase I, dose-escalation study of the novel Polo-like kinase inhibitor volasertib (BI 6727) in patients with advanced solid tumours.
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A Regulatory Loop of FBXW7-MYC-PLK1 Controls Tumorigenesis of MYC-Driven Medulloblastoma.
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A ribonucleoprotein octamer for targeted siRNA delivery.
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A Yeast Synthetic Dosage Lethal Screen Identifies a Conserved Interaction between PLK1 and CKS1B Affecting Cancer Cell Viability.
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Absence of polo-like kinase 3 in mice stabilizes Cdc25A after DNA damage but is not sufficient to produce tumors.
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An in-vitro evaluation of the polo-like kinase inhibitor GW843682X against paediatric malignancies.
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An oncoinformatics study to predict the inhibitory potential of recent FDA-approved anti-cancer drugs against human Polo-like kinase 1 enzyme: a step towards dual-target cancer medication.
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An open-label, phase I study of the polo-like kinase-1 inhibitor, BI 2536, in patients with advanced solid tumors.
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An open-label, single-arm, phase 2 trial of the polo-like kinase inhibitor volasertib (BI 6727) in patients with locally advanced or metastatic urothelial cancer.
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Anti-breast cancer activity of LFM-A13, a potent inhibitor of Polo-like kinase (PLK).
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Anticancer effects of radiation therapy combined with Polo-Like Kinase 4 (PLK4) inhibitor CFI-400945 in triple negative breast cancer.
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Anticancer effects on TACC3 by treatment of paclitaxel in HPV-18 positive cervical carcinoma cells.
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Antiproliferative in vitro effects of BI 2536-mediated PLK1 inhibition on cervical adenocarcinoma cells.
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Apoptotic effects of genistein, biochanin-A and apigenin on LNCaP and PC-3 cells by p21 through transcriptional inhibition of polo-like kinase-1.
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Application of Post Solid-Phase Oxime Ligation to Fine-Tune Peptide-Protein Interactions.
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Aurora-A and hBora join the game of Polo.
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Balancing polymer hydrophobicity for ligand presentation and siRNA delivery in dual function CXCR4 inhibiting polyplexes.
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Battle of the eternal rivals: restoring functional p53 and inhibiting Polo-like kinase 1 as cancer therapy.
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BI 2536, a potent and selective inhibitor of polo-like kinase 1, inhibits tumor growth in vivo.
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BI 2536-mediated PLK1 inhibition suppresses HOS and MG-63 osteosarcoma cell line growth and clonogenicity.
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BI 6727 and GSK461364 suppress growth and radiosensitize osteosarcoma cells, but show limited cytotoxic effects when combined with conventional treatments.
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BI-2536 and BI-6727, dual Polo-like kinase/bromodomain inhibitors, effectively reactivate latent HIV-1.
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Binding of the anticancer drug BI-2536 to human serum albumin. A spectroscopic and theoretical study.
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Biological impact of freezing Plk1 in its inactive conformation in cancer cells.
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Branched Antisense and siRNA Co-Assembled Nanoplatform for Combined Gene Silencing and Tumor Therapy.
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Cancer inhibition in nude mice after systemic application of U6 promoter-driven short hairpin RNAs against PLK1.
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Cancer Osaka thyroid (Cot) phosphorylates Polo-like kinase (PLK1) at Ser137 but not at Thr210.
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Cell biology. Reversible centriole depletion with an inhibitor of Polo-like kinase 4.
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Cell type-- dependent effects of Polo-like kinase 1 inhibition compared with targeted polo box interference in cancer cell lines.
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Characterization of protein tyrosine kinase activity in murine Leydig tumor cells.
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Click modified amphiphilic graft copolymeric micelles of poly(styrene-alt-maleic anhydride) for combinatorial delivery of doxorubicin and plk-1 siRNA in cancer therapy.
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Clinical Significance of Polo-Like Kinase 4 as a Marker for Advanced Tumor Stage and Dismal Prognosis in Patients With Surgical Gastric Cancer.
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Co-targeting PLK1 and mTOR induces synergistic inhibitory effects against esophageal squamous cell carcinoma.
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Combination of PI3K/Akt Pathway Inhibition and Plk1 Depletion Can Enhance Chemosensitivity to Gemcitabine in Pancreatic Carcinoma.
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Combined Gene Expression Profiling and RNAi Screening in Clear Cell Renal Cell Carcinoma Identify PLK1 and Other Therapeutic Kinase Targets.
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Computational analysis of phosphopeptide binding to the polo-box domain of the mitotic kinase PLK1 using molecular dynamics simulation.
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Conditional inhibition of cancer cell proliferation by tetracycline-responsive, H1 promoter-driven silencing of PLK1.
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Confirming the RNAi-mediated mechanism of action of siRNA-based cancer therapeutics in mice.
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Correction: Novel Oncolytic Adenovirus Selectively Targets Tumor-Associated Polo-Like Kinase 1 and Tumor Cell Viability.
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Cotargeting Polo-Like Kinase 1 and the Wnt/?-Catenin Signaling Pathway in Castration-Resistant Prostate Cancer.
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Current assessment of polo-like kinases as anti-tumor drug targets.
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Current clinical trials with polo-like kinase 1 inhibitors in solid tumors.
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Deciphering the performance of polo-like kinase 1 in triple-negative breast cancer progression according to the centromere protein U-phosphorylation pathway.
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Decreased KPNB1 Expression is Induced by PLK1 Inhibition and Leads to Apoptosis in Lung Adenocarcinoma.
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Defeat Mutant KRAS with Synthetic Lethality.
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Design and evaluation of ionizable peptide amphiphiles for siRNA delivery.
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Design and Synthesis of a Novel PLK1 Inhibitor Scaffold Using a Hybridized 3D-QSAR Model.
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Design of Cationic Multiwalled Carbon Nanotubes as Efficient siRNA Vectors for Lung Cancer Xenograft Eradication.
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Design of Peptidomimetic Functionalized Cholesterol Based Lipid Nanoparticles for Efficient Delivery of Therapeutic Nucleic Acids.
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Design, synthesis, and biological evaluation of novel highly selective polo-like kinase 2 inhibitors based on the tetrahydropteridin chemical scaffold.
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Designed inhibitor for nuclear localization signal of polo-like kinase 1 induces mitotic arrest.
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Detection and destruction of HER2-positive cancer cells by Ultra Quenchbody-siRNA complex.
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Development of a Novel Cell-Permeable Protein-Protein Interaction Inhibitor for the Polo-box Domain of Polo-like Kinase 1.
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Development of a Polo-like Kinase-1 Polo-Box Domain Inhibitor as a Tumor Growth Suppressor in Mice Models.
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Development of Bifunctional Inhibitors of Polo-Like Kinase 1 with Low-Nanomolar Activities Against the Polo-Box Domain.
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Differential Cellular Effects of Plk1 Inhibitors Targeting the ATP-binding Domain or Polo-box Domain.
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Discovery and development of the Polo-like kinase inhibitor volasertib in cancer therapy.
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Discovery of Novel Polo-Like Kinase 1 Polo-Box Domain Inhibitors to Induce Mitotic Arrest in Tumor Cells.
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Dissecting the phenotypes of Plk1 inhibition in cancer cells using novel kinase inhibitory chemical CBB2001.
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Distinct microRNA expression profiles in acute myeloid leukemia with common translocations.
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DITMD-induced mitotic defects and apoptosis in tumor cells by blocking the polo-box domain-dependent functions of polo-like kinase 1.
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Dominant-negative polo-like kinase 1 induces mitotic catastrophe independent of cdc25C function.
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Down-regulation of Polo-like kinase 4 (PLK4) induces G1 arrest via activation of the p38/p53/p21 signaling pathway in bladder cancer.
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Downregulation of human polo-like kinase activity by antisense oligonucleotides induces growth inhibition in cancer cells.
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Downregulation of PLK-1 expression in kaempferol-induced apoptosis of MCF-7 cells.
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Downregulation of Polo-like kinase-1 (PLK-1) expression is associated with poor clinical outcome in uveal melanoma patients.
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Dynamic and multi-pharmacophore modeling for designing polo-box domain inhibitors.
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Effect of AKT3 expression on MYC- and caspase-8-dependent apoptosis caused by polo-like kinase inhibitors in HCT 116 cells.
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Effect of Cationic Lipid Type in Folate-PEG-Modified Cationic Liposomes on Folate Receptor-Mediated siRNA Transfection in Tumor Cells.
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Effect of protein kinase inhibitors on activity of mammalian small heat-shock protein (HSP25) kinase.
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Effect of RNA silencing of polo-like kinase-1 (PLK1) on apoptosis and spindle formation in human cancer cells.
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Efficient inhibition of human colorectal carcinoma growth by RNA interference targeting polo-like kinase 1 in vitro and in vivo.
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Efficient internalization of the polo-box of polo-like kinase 1 fused to an Antennapedia peptide results in inhibition of cancer cell proliferation.
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Elucidation of PLK1 Linked Biomarkers in Oesophageal Cancer Cell Lines: A Step Towards Novel Signaling Pathways by p53 and PLK1- Linked Functions Crosstalk.
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Enabling and disabling Polo-like kinase 1 inhibition through chemical genetics.
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Engineering Human Epidermal Growth Receptor 2-Targeting Hepatitis B Virus Core Nanoparticles for siRNA Delivery in Vitro and in Vivo.
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Enhanced polo-like kinase 1 expression in myelodysplastic syndromes.
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Enhancing Gene-Knockdown Efficiency of Poly(N-isopropylacrylamide) Nanogels.
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Epigenetic inactivation implies a tumor suppressor function in hematologic malignancies for Polo-like kinase 2 but not Polo-like kinase 3.
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ER maleate is a novel anticancer agent in oral cancer: Implications for cancer therapy.
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Essential Role of Polo-like Kinase 1 (Plk1) Oncogene in Tumor Growth and Metastasis of Tamoxifen-Resistant Breast Cancer.
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Exploring the binding nature of pyrrolidine pocket-dependent interactions in the polo-box domain of polo-like kinase 1.
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Fate of primary cells at the G?/S boundary after polo-like kinase 1 inhibition by SBE13.
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Folate-Mediated Targeted Delivery of siPLK1 by Leucine-Bearing Polyethylenimine.
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Formation of extra centrosomal structures is dependent on beta-catenin.
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Foxm1 expression in prostate epithelial cells is essential for prostate carcinogenesis.
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Freezing Polo in its sleep: targeting the inactive conformation of Polo-like kinase 1 in cancer cells.
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Future prospect of RNA interference for cancer therapies.
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Gene regulation with carbon-based siRNA conjugates for cancer therapy.
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Glucose-linked sub-50-nm unimer polyion complex-assembled gold nanoparticles for targeted siRNA delivery to glucose transporter 1-overexpressing breast cancer stem-like cells.
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GSK461364A, a Polo-Like Kinase-1 Inhibitor Encapsulated in Polymeric Nanoparticles for the Treatment of Glioblastoma Multiforme (GBM).
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Helicobacter pylori promotes gastric epithelial cell survival through the PLK1/PI3K/Akt pathway.
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High expression of polo-like kinase 1 is associated with the metastasis and recurrence in urothelial carcinoma of bladder.
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High levels of polo-like kinase 1 and phosphorylated translationally controlled tumor protein indicate poor prognosis in neuroblastomas.
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Human ABCB1 (P-glycoprotein) and ABCG2 mediate resistance to BI 2536, a potent and selective inhibitor of Polo-like kinase 1.
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Human ATP-Binding Cassette Transporter ABCB1 Confers Resistance to Volasertib (BI 6727), a Selective Inhibitor of Polo-like Kinase 1.
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Identification of a high affinity selective inhibitor of Polo-like kinase 1 for cancer chemotherapy by computational approach.
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Identification of a New Heterocyclic Scaffold for Inhibitors of the Polo-Box Domain of Polo-like Kinase 1.
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Identification of a novel Polo-like kinase 1 inhibitor that specifically blocks the functions of Polo-Box domain.
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Identification of a Polo-like Kinase 4-Dependent Pathway for De Novo Centriole Formation.
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Identification of green tea catechins as potent inhibitors of the polo-box domain of polo-like kinase 1.
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Identification of novel polo-like kinase 1 inhibitors by a hybrid virtual screening.
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Identification of Polo-like kinase 1 interaction inhibitors using a novel cell-based assay.
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Identification of synthetic lethality of PLK1 inhibition and microtubule-destabilizing drugs.
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Immunohistochemical expression of polo-like kinase 1 in oral squamous cell carcinoma and oral submucous fibrosis.
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Impact Of Plk-1 Silencing On Endothelial Cells And Cancer Cells Of Diverse Histological Origin.
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In Vitro and In Vivo Tumor-Targeting siRNA Delivery Using Folate-PEG-appended Dendrimer (G4)/?-Cyclodextrin Conjugates.
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In vitro PLK1 inhibition by BI 2536 decreases proliferation and induces cell-cycle arrest in melanoma cells.
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In-silico design and synthesis of N9-substituted ?-Carbolines as PLK-1 inhibitors and their in-vitro/in-vivo tumor suppressing evaluation.
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Induction of antitumor immunity using dendritic cells electroporated with Polo-like kinase 1 (Plk1) mRNA in murine tumor models.
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Inhibiting Polo-like kinase 1 causes growth reduction and apoptosis in pediatric acute lymphoblastic leukemia cells.
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Inhibition of dynamin by dynole 34-2 induces cell death following cytokinesis failure in cancer cells.
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Inhibition of Plk1 represses androgen signaling pathway in castration-resistant prostate cancer.
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Inhibition of PLK4 might enhance the anti-tumour effect of bortezomib on glioblastoma via PTEN/PI3K/AKT/mTOR signalling pathway.
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Inhibition of Polo-Like Kinase 1 by BI2536 Reverses the Multidrug Resistance of Human Hepatoma Cells In Vitro and In Vivo.
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Inhibition of polo-like kinase 1 by blocking polo-box domain-dependent protein-protein interactions.
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Inhibition of polo-like kinase 1 induces cell cycle arrest and sensitizes glioblastoma cells to ionizing radiation.
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Inhibition of Polo-like kinase 1 prevents the growth of metastatic breast cancer cells in the brain.
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Inhibition of serine/threonine phosphatase PP2A enhances cancer chemotherapy by blocking DNA damage induced defense mechanisms.
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Inhibition of Suicidal Erythrocyte Death by Volasertib.
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Inhibitors of the Polo-Box Domain of Polo-like Kinase 1.
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Initial testing (stage 1) of the polo-like kinase inhibitor volasertib (BI 6727), by the Pediatric Preclinical Testing Program.
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Integrated bioinformatics analysis reveals CDK1 and PLK1 as potential therapeutic targets of lung adenocarcinoma.
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Integrative mRNA profiling comparing cultured primary cells with clinical samples reveals PLK1 and C20orf20 as therapeutic targets in cutaneous squamous cell carcinoma.
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Involvement of Polo-like kinase 1 (Plk1) in quiescence regulation of cancer stem-like cells of the gastric cancer cell lines.
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In vitro study of the Polo-like kinase 1 inhibitor volasertib in non-small-cell lung cancer reveals a role for the tumor suppressor p53.
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In vivo tumor imaging using polo-box domain of polo-like kinase 1 targeted peptide.
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Ionizing radiation inhibits the PLK cell cycle gene in a G2 checkpoint-dependent manner.
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Kinome inhibition reveals a role for polo-like kinase 1 in targeting post-transcriptional control in cancer.
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KRAS Cold Turkey: Using microRNAs to target KRAS-addicted cancer.
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Liaisons between survivin and PLK1 during cell division and cell death.
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Long-term downregulation of Polo-like kinase 1 increases the cyclin-dependent kinase inhibitor p21(WAF1/CIP1).
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Loss of p21Cip1/CDKN1A renders cancer cells susceptible to Polo-like kinase 1 inhibition.
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Low dietary folate initiates intestinal tumors in mice, with altered expression of G2-M checkpoint regulators polo-like kinase 1 and cell division cycle 25c.
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Luteolin-Fabricated ZnO Nanostructures Showed PLK-1 Mediated Anti-Breast Cancer Activity.
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Matrix metalloproteinase 2-responsive micelle for siRNA delivery.
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MCC1019, a selective inhibitor of the Polo-box domain of Polo-like kinase 1 as novel, potent anticancer candidate.
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Mechanisms of omega-3 fatty acid-induced growth inhibition in MDA-MB-231 human breast cancer cells.
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MicroRNA-100 is a potential molecular marker of non-small cell lung cancer and functions as a tumor suppressor by targeting polo-like kinase 1.
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miR-296-5p suppresses cell viability by directly targeting PLK1 in non-small cell lung cancer.
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Mitotic Exit Dysfunction through the Deregulation of APC/C Characterizes Cisplatin-Resistant State in Epithelial Ovarian Cancer.
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Modular Plasmonic Nanocarriers for Efficient and Targeted Delivery of Cancer-Therapeutic siRNA.
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Modulating Polo-Like Kinase 1 as a Means for Cancer Chemoprevention.
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Molecular alterations after Polo-like kinase 1 mRNA suppression versus pharmacologic inhibition in cancer cells.
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Molecular and enzoinformatics perspectives of targeting Polo-like kinase 1 in cancer therapy.
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Molecular interactions of polo-like kinase 1 in human cancers.
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Molecular targeting of the oncoprotein PLK1 in pediatric acute myeloid leukemia: RO3280, a novel PLK1 inhibitor, induces apoptosis in leukemia cells.
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Molecular Targets of Genistein and Its Related Flavonoids to Exert Anticancer Effects.
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Monitoring of changes in lipid profiles during PLK1 knockdown in cancer cells using DESI MS.
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Multicentric parallel phase II trial of the polo-like kinase 1 inhibitor BI 2536 in patients with advanced head and neck cancer, breast cancer, ovarian cancer, soft tissue sarcoma and melanoma. The first protocol of the European Organization for Research and Treatment of Cancer (EORTC) Network Of Core Institutes (NOCI).
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Multifunctional polyion complex micelle featuring enhanced stability, targetability, and endosome escapability for systemic siRNA delivery to subcutaneous model of lung cancer.
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Multiplexed random peptide library and phospho-specific antibodies facilitate human polo-like kinase 1 inhibitor screen.
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Network Pharmacological Analysis through a Bioinformatics Approach of Novel NSC765600 and NSC765691 Compounds as Potential Inhibitors of CCND1/CDK4/PLK1/CD44 in Cancer Types.
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New Inhibitors of Polo-like Kinase 1 Function and Their Emerging Role in Attenuating Tumor Growth in Systemic Malignancies.
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NMS-P937, an orally available, specific, small molecule Polo-Like Kinase 1 inhibitor with antitumor activity in solid and haematological malignancies.
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Nonviral gene editing via CRISPR/Cas9 delivery by membrane-disruptive and endosomolytic helical polypeptide.
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Normal cells, but not cancer cells, survive severe plk1 depletion.
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Novel biomarker for hepatocellular carcinoma: high tumoral PLK-4 expression is associated with better prognosis in patients without microvascular invasion.
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Novel oncolytic adenovirus selectively targets tumor-associated polo-like kinase 1 and tumor cell viability.
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Nuclear cyclin B1 in human breast carcinoma as a potent prognostic factor.
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Nuclear pore protein NUP88 activates anaphase-promoting complex to promote aneuploidy.
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OCT4B1 Promoted EMT and Regulated the Self-Renewal of CSCs in CRC: Effects Associated with the Balance of miR-8064/PLK1.
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Oncogenic regulators and substrates of the anaphase promoting complex/cyclosome are frequently overexpressed in malignant tumors.
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Overexpression of cyclooxygenase-2 in human prostate carcinoma and prostatic intraepithelial neoplasia-association with increased expression of Polo-like kinase-1.
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Overexpression of human ABCB1 in cancer cells leads to reduced activity of GSK461364, a specific inhibitor of polo-like kinase 1.
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Overexpression of polo-like kinase 1 and its clinical significance in human non-small cell lung cancer.
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p53 and its downstream proteins as molecular targets of cancer.
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pH-responsive polymeric sirna carriers sensitize multidrug resistant ovarian cancer cells to doxorubicin via knockdown of polo-like kinase 1.
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Pharmacoinformatics approach for the identification of Polo-like kinase-1 inhibitors from natural sources as anti-cancer agents.
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Phase 1 study of rigosertib, an inhibitor of the phosphatidylinositol 3-kinase and polo-like kinase 1 pathways, combined with gemcitabine in patients with solid tumors and pancreatic cancer.
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Phase I dose escalation and pharmacokinetic study of BI 2536, a novel Polo-like kinase 1 inhibitor, in patients with advanced solid tumors.
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Phase I dose escalation study of NMS-1286937, an orally available Polo-Like Kinase 1 inhibitor, in patients with advanced or metastatic solid tumors.
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Phase I study of GSK461364, a specific and competitive Polo-like Kinase 1 (PLK1) inhibitor in patients with advanced solid malignancies.
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Phase I study of ON 01910.Na, a novel modulator of the Polo-like kinase 1 pathway, in adult patients with solid tumors.
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Phase I Study of Oral Rigosertib (ON 01910.Na), a Dual Inhibitor of the PI3K and Plk1 Pathways, in Adult Patients with Advanced Solid Malignancies.
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Phase I trial of volasertib, a Polo-like kinase inhibitor, in Japanese patients with advanced solid tumors.
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Phase I trial of volasertib, a Polo-like kinase inhibitor, plus platinum agents in solid tumors: safety, pharmacokinetics and activity.
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Phosphopeptides with improved cellular uptake properties as ligands for the polo-box domain of polo-like kinase 1.
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Phosphorylation of human enhancer filamentation 1 (HEF1) stimulates interaction with Polo-like kinase 1 leading to HEF1 localization to focal adhesions.
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PLK-1 Expression is Associated with Histopathological Response to Neoadjuvant Therapy of Hepatic Metastasis of Colorectal Carcinoma.
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PLK-1 Targeted Inhibitors and Their Potential against Tumorigenesis.
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Plk1 and CK2 act in concert to regulate Rad51 during DNA double strand break repair.
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Plk1 depletion in nontransformed diploid cells activates the DNA-damage checkpoint.
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PLK1 Induces Chromosomal Instability and Overrides Cell-Cycle Checkpoints to Drive Tumorigenesis.
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Plk1 inhibition enhances the efficacy of androgen signaling blockade in castration-resistant prostate cancer.
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Plk1 Inhibition Enhances the Efficacy of BET Epigenetic Reader Blockade in Castration-Resistant Prostate Cancer.
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Plk1 Inhibitors in Cancer Therapy: From Laboratory to Clinics.
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Plk1 overexpression induces chromosomal instability and suppresses tumor development.
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PLK1 promotes epithelial-mesenchymal transition and metastasis of gastric carcinoma cells.
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Plk1 promotes the migration of human lung adenocarcinoma epithelial cells via STAT3 signaling.
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Plk1 regulates contraction of postmitotic smooth muscle cells and is required for vascular homeostasis.
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PLK1 signaling in breast cancer cells cooperates with estrogen receptor-dependent gene transcription.
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Plk1, upregulated by HIF-2, mediates metastasis and drug resistance of clear cell renal cell carcinoma.
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Plk1-dependent microtubule dynamics promotes androgen receptor signaling in prostate cancer.
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Plk2 promotes tumor growth and inhibits apoptosis by targeting Fbxw7/Cyclin E in colorectal cancer.
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Plk2 regulates mitotic spindle orientation and mammary gland development.
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Polo Like Kinase 2 Tumour Suppressor and cancer biomarker: new perspectives on drug sensitivity/resistance in ovarian cancer.
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Polo-like kinase (Plk)1 depletion induces apoptosis in cancer cells.
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Polo-like kinase 1 (Plk1) in non-melanoma skin cancers.
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Polo-Like Kinase 1 (PLK1) Inhibition Kills Glioblastoma Multiforme Brain Tumour Cells in Part Through Loss of SOX2 and Delays Tumour Progression in Mice.
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Polo-like kinase 1 (PLK1) inhibition suppresses cell growth and enhances radiation sensitivity in medulloblastoma cells.
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Polo-like kinase 1 (Plk1) overexpression enhances ionizing radiation-induced cancer formation in mice.
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Polo-like kinase 1 (PLK1) signaling in cancer and beyond.
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Polo-like kinase 1 as a therapeutic target for malignant peripheral nerve sheath tumors (MPNST) and schwannomas.
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Polo-like kinase 1 as target for cancer therapy.
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Polo-like kinase 1 contributes to the tumorigenicity of BEL-7402 hepatoma cells via regulation of Survivin expression.
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Polo-like kinase 1 coordinates biosynthesis during cell cycle progression by directly activating pentose phosphate pathway.
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Polo-like kinase 1 facilitates loss of Pten tumor suppressor-induced prostate cancer formation.
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Polo-like kinase 1 in the life and death of cancer cells.
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Polo-like kinase 1 induces epithelial-to-mesenchymal transition and promotes epithelial cell motility by activating CRAF/ERK signaling.
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Polo-like Kinase 1 Inhibition as a Therapeutic Approach to Selectively Target BRCA1-Deficient Cancer Cells by Synthetic Lethality Induction.
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Polo-like kinase 1 inhibition sensitizes neuroblastoma cells for vinca alkaloid-induced apoptosis.
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Polo-like kinase 1 inhibitor BI 6727 induces DNA damage and exerts strong antitumor activity in small cell lung cancer.
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Polo-like kinase 1 inhibitor BI2536 causes mitotic catastrophe following activation of the spindle assembly checkpoint in non-small cell lung cancer cells.
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Polo-like kinase 1 inhibitors in mono- and combination therapies: a new strategy for treating malignancies.
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Polo-like kinase 1 inhibitors, mitotic stress and the tumor suppressor p53.
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Polo-like kinase 1 is a therapeutic target in high-risk neuroblastoma.
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Polo-like kinase 1 is essential for early embryonic development and tumor suppression.
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Polo-like kinase 1 is overexpressed in acute myeloid leukemia and its inhibition preferentially targets the proliferation of leukemic cells.
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Polo-like kinase 1 is overexpressed in colorectal cancer and participates in the migration and invasion of colorectal cancer cells.
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Polo-like kinase 1 is overexpressed in prostate cancer and linked to higher tumor grades.
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Polo-like kinase 1 is overexpressed in renal cancer and participates in the proliferation and invasion of renal cancer cells.
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Polo-like kinase 1 regulates cell proliferation and is targeted by miR-593* in esophageal cancer.
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Polo-like kinase 2 acting as a promoter in human tumor cells with an abundance of TAp73.
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Polo-like kinase 2 is a mediator of hedgehog survival signaling in cholangiocarcinoma.
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Polo-like kinase 2, a novel ADAM17 signaling component, regulates tumor necrosis factor ? ectodomain shedding.
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Polo-like kinase 3 and phosphoT273 caspase-8 are associated with improved local tumor control and survival in patients with anal carcinoma treated with concomitant chemoradiotherapy.
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Polo-like kinase 3 functions as a tumor suppressor and is a negative regulator of hypoxia-inducible factor-1 alpha under hypoxic conditions.
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Polo-like kinase 3 inhibits glucose metabolism in colorectal cancer by targeting HSP90/STAT3/HK2 signaling.
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Polo-like kinase 3, hypoxic responses, and tumorigenesis.
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Polo-like kinase 4 correlates with greater tumor size, lymph node metastasis and confers poor survival in non-small cell lung cancer.
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Polo-like kinase 4 inhibition: a strategy for cancer therapy?
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Polo-Like Kinase 4's Critical Role in Cancer Development and Strategies for Plk4-Targeted Therapy.
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Polo-like Kinase Inhibitor Volasertib Exhibits Antitumor Activity and Synergy with Vincristine in Pediatric Malignancies.
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Polo-like kinase inhibitors: an emerging opportunity for cancer therapeutics.
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Polo-like kinase-1 as novel target in neoplastic mast cells: demonstration of growth-inhibitory effects of siRNA and the Polo-like kinase-1 targeting drug BI 2536.
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Polo-like kinase-1 immunoreactivity is associated with metastases in cutaneous melanoma.
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Polo-like Kinase-1 Regulates Myc Stabilization and Activates a Feedforward Circuit Promoting Tumor Cell Survival.
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Polo-like kinase1 (Plk1) knockdown enhances cisplatin chemosensitivity via up-regulation of p73? in p53 mutant human epidermoid squamous carcinoma cells.
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Polo-like kinase1, a new target for antisense tumor therapy.
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Polo-like kinase: a novel marker of proliferation: correlation with estrogen-receptor expression in human breast cancer.
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Polo-like kinases in AML.
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Polo-like-kinase 1 (PLK-1) and c-myc inhibition with the dual kinase-bromodomain inhibitor volasertib in aggressive lymphomas.
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Poly-l-lysine Functionalized Large Pore Cubic Mesostructured Silica Nanoparticles as Biocompatible Carriers for Gene Delivery.
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Potent Synergistic Effect on C-Myc-Driven Colorectal Cancers Using a Novel Indole-Substituted Quinoline with a Plk1 Inhibitor.
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Probing the nanoparticle-AGO2 interaction for enhanced gene knockdown.
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PSA-responsive and PSMA-mediated multifunctional liposomes for targeted therapy of prostate cancer.
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Quantitative phospho-proteomics to investigate the Polo-like kinase 1-dependent phospho-proteome.
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Reaction-driven de novo design, synthesis and testing of potential type II kinase inhibitors.
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Reciprocal Activation Between PLK1 and Stat3 Contributes to Survival and Proliferation of Esophageal Cancer Cells.
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Reduced NR4A gene dosage leads to mixed myelodysplastic/myeloproliferative neoplasms in mice.
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Regulation of cell apoptosis and proliferation in pancreatic cancer through PI3K/Akt pathway via Polo-like kinase 1.
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Regulatory functional territory of PLK-1 and their substrates beyond mitosis.
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Replication stress, defective S-phase checkpoint and increased death in Plk2-deficient human cancer cells.
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Resveratrol inhibits cell cycle progression by targeting Aurora kinase A and Polo-like kinase 1 in breast cancer cells.
Neoplasms
Revisiting the molecular interactions between the tumor protein TCTP and the drugs sertraline/thioridazine.
Neoplasms
RNA interference-mediated silencing of the polo-like kinase 1 gene enhances chemosensitivity to gemcitabine in pancreatic adenocarcinoma cells.
Neoplasms
RNAi prodrugs decrease elevated mRNA levels of Polo-like kinase 1 in ex vivo cultured primary cells from pediatric acute myeloid leukemia patients.
Neoplasms
RNAi prodrugs targeting Plk1 induce specific gene silencing in primary cells from pediatric T-acute lymphoblastic leukemia patients.
Neoplasms
Role of NEK2A in Human Cancer and Its Therapeutic Potentials.
Neoplasms
Role of polo-like kinase 4 (PLK4) in epithelial cancers and recent progress in its small molecule targeting for cancer management.
Neoplasms
Roles of Polo-like kinase 3 in suppressing tumor angiogenesis.
Neoplasms
ROS-Responsive Polymeric Micelles for Triggered Simultaneous Delivery of PLK1 Inhibitor/miR-34a and Effective Synergistic Therapy in Pancreatic Cancer.
Neoplasms
ROS-Responsive Polymeric siRNA Nanomedicine Stabilized by Triple Interactions for the Robust Glioblastoma Combinational RNAi Therapy.
Neoplasms
SAPK pathways and p53 cooperatively regulate PLK4 activity and centrosome integrity under stress.
Neoplasms
ScFv-Decorated PEG-PLA-Based Nanoparticles for Enhanced siRNA Delivery to Her2(+) Breast Cancer.
Neoplasms
Selective Cell Penetrating Peptide-Functionalized Envelope-Type Chimeric Lipopepsomes Boost Systemic RNAi Therapy for Lung Tumors.
Neoplasms
Selectivity-determining residues in Plk1.
Neoplasms
Semi-mechanistic population pharmacokinetic/pharmacodynamic model for neutropenia following therapy with the Plk-1 inhibitor BI 2536 and its application in clinical development.
Neoplasms
Sensitivity of TP53-Mutated Cancer Cells to the Phytoestrogen Genistein Is Associated With Direct Inhibition of Plk1 Activity.
Neoplasms
Sialic Acid-Targeted Nanovectors with Phenylboronic Acid-Grafted Polyethylenimine Robustly Enhance siRNA-Based Cancer Therapy.
Neoplasms
Silencing of polo-like kinase (Plk) 1 via siRNA causes induction of apoptosis and impairment of mitosis machinery in human prostate cancer cells: implications for the treatment of prostate cancer.
Neoplasms
Silencing of polo-like kinase (Plk) 1 via siRNA causes inhibition of growth and induction of apoptosis in human esophageal cancer cells.
Neoplasms
Simultaneous delivery of siRNA and paclitaxel via a "two-in-one" micelleplex promotes synergistic tumor suppression.
Neoplasms
Simultaneous PLK1 inhibition improves local tumour control after fractionated irradiation.
Neoplasms
Single-step assembly of cationic lipid-polymer hybrid nanoparticles for systemic delivery of siRNA.
Neoplasms
Small interfering RNA-mediated Polo-like kinase 1 depletion preferentially reduces the survival of p53-defective, oncogenic transformed cells and inhibits tumor growth in animals.
Neoplasms
Small-molecular, non-peptide, non-ATP-competitive polo-like kinase 1 (Plk1) inhibitors with a terphenyl skeleton.
Neoplasms
SPDEF inhibits prostate carcinogenesis by disrupting a positive feedback loop in regulation of the Foxm1 oncogene.
Neoplasms
Structural basis for the inhibition of Polo-like kinase 1.
Neoplasms
Structural insights into the inhibitor binding and new inhibitor design to Polo-Like Kinase-1 Polo-Box Domain using computational studies.
Neoplasms
Structure of wild-type Plk-1 kinase domain in complex with a selective DARPin.
Neoplasms
Structure-based design and SAR development of novel selective polo-like kinase 1 inhibitors having the tetrahydropteridin scaffold.
Neoplasms
Suppression of KRas-mutant cancer through the combined inhibition of KRAS with PLK1 and ROCK.
Neoplasms
Synergistic effects of FGFR1 and PLK1 inhibitors target a metabolic liability in KRAS-mutant cancer.
Neoplasms
Systematic expression analysis of WEE family kinases reveals the importance of PKMYT1 in breast carcinogenesis.
Neoplasms
Targeted delivery of CRISPR/Cas9 to prostate cancer by modified gRNA using a flexible aptamer-cationic liposome.
Neoplasms
Targeted Delivery of CRISPR/Cas9-Mediated Cancer Gene Therapy via Liposome-Templated Hydrogel Nanoparticles.
Neoplasms
Targeted delivery of PLK1-siRNA by ScFv suppresses Her2+ breast cancer growth and metastasis.
Neoplasms
Targeting cell cycle by ?-carboline alkaloids in vitro: Novel therapeutic prospects for the treatment of cancer.
Neoplasms
Targeting kinases with thymoquinone: a molecular approach to cancer therapeutics.
Neoplasms
Targeting Plk1 to Enhance Efficacy of Olaparib in Castration-Resistant Prostate Cancer.
Neoplasms
Targeting Polo-like Kinase 1 by a Novel Pyrrole-imidazole Polyamide-Hoechst Conjugate Suppresses Tumor Growth in vivo.
Neoplasms
Targeting polo-like kinase 1 by NMS-P937 in osteosarcoma cell lines inhibits tumor cell growth and partially overcomes drug resistance.
Neoplasms
Targeting polo-like kinase 1 for cancer therapy.
Neoplasms
Targeting polo-like kinase 1 suppresses essential functions of alloreactive T cells.
Neoplasms
Targeting Polo-like kinase in cancer therapy.
Neoplasms
The CINs of Polo-Like Kinase 1 in Cancer.
Neoplasms
The clinical and prognostic value of polo-like kinase 1 in lung squamous cell carcinoma patients: immunohistochemical analysis.
Neoplasms
The Discovery of Polo-Like Kinase 4 Inhibitors: Identification of (1R,2S)-2-(3-((E)-4-(((cis)-2,6-Dimethylmorpholino)methyl)styryl)-1H-indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a Potent, Orally Active Antitumor Agent.
Neoplasms
The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor agent.
Neoplasms
The Dual Pathway Inhibitor Rigosertib Is Effective in Direct Patient Tumor Xenografts of Head and Neck Squamous Cell Carcinomas.
Neoplasms
The dual role of BI 2536, a small-molecule inhibitor that targets PLK1, in induction of apoptosis and attenuation of autophagy in neuroblastoma cells.
Neoplasms
The Emerging Role of Polo-Like Kinase 1 in Epithelial-Mesenchymal Transition and Tumor Metastasis.
Neoplasms
The expression of PLK-1 in cervical carcinoma: a possible target for enhancing chemosensitivity.
Neoplasms
The Mitotic Cancer Target Polo-Like Kinase 1: Oncogene or Tumor Suppressor?
Neoplasms
The Multifaced Role of STAT3 in Cancer and Its Implication for Anticancer Therapy.
Neoplasms
The natural product Aristolactam AIIIa as a new ligand targeting the polo-box domain of polo-like kinase 1 potently inhibits cancer cell proliferation.
Neoplasms
The Plk1 inhibitor BI 2536 in patients with refractory or relapsed non-Hodgkin's lymphoma: A Phase I, open-label, single dose-escalation study.
Neoplasms
The Plk1 inhibitor BI 2536 temporarily arrests primary cardiac fibroblasts in mitosis and generates aneuploidy in vitro.
Neoplasms
The polo-like kinase inhibitor BI 2536 exhibits potent activity against malignant plasma cells and represents a novel therapy in multiple myeloma.
Neoplasms
The potential mechanism of action of Sorcin and its interacting proteins.
Neoplasms
The responses of cancer cells to PLK1 inhibitors reveal a novel protective role for p53 in maintaining centrosome separation.
Neoplasms
The RNA helicase/transcriptional co-regulator, p68 (DDX5), stimulates expression of oncogenic protein kinase, Polo-like kinase-1 (PLK1), and is associated with elevated PLK1 levels in human breast cancers.
Neoplasms
The small-molecule inhibitor BI 2536 reveals novel insights into mitotic roles of polo-like kinase 1.
Neoplasms
Therapeutic relevance of the protein phosphatase 2A in cancer.
Neoplasms
Therapeutic targeting of polo-like kinase 1 using RNA-interfering nanoparticles (iNOPs) for the treatment of non-small cell lung cancer.
Neoplasms
Therapeutic targeting of the PLK1-PRC1-axis triggers cell death in genomically silent childhood cancer.
Neoplasms
Therapeutic Targeting PLK1 by ON-01910.Na Is Effective in Local Treatment of Retinoblastoma.
Neoplasms
Transcriptional silencing of Polo-like kinase 2 (SNK/PLK2) is a frequent event in B-cell malignancies.
Neoplasms
Transient genomic instability drives tumorigenesis through accelerated clonal evolution.
Neoplasms
Tumor inhibition by genomically integrated inducible RNAi-cassettes.
Neoplasms
Tumor regression by combination antisense therapy against Plk1 and Bcl-2.
Neoplasms
Tumour-specific delivery of siRNA-coupled superparamagnetic iron oxide nanoparticles, targeted against PLK1, stops progression of pancreatic cancer.
Neoplasms
Tuned Density of Anti-Tissue Factor Antibody Fragment onto siRNA-Loaded Polyion Complex Micelles for Optimizing Targetability into Pancreatic Cancer Cells.
Neoplasms
Vitamin E-Conjugated Phosphopeptide Inhibitor of the Polo-Box Domain of Polo-Like Kinase 1.
Neoplasms
Volasertib suppresses the growth of human hepatocellular carcinoma
Neoplasms
Wnt5a-induced docking of Plk1 on HEF1 promotes HEF1 translocation and tumorigenesis.
Neoplasms
[Enhancive Effect of PLK1 Gene Silencing onSensitivity of K562/A02 Cells to Adriamycin.]
Neoplasms
[Mining Polo-Box domain of Polo-like kinase 1 as a new therapeutic target for cancer].
Neoplasms, Radiation-Induced
Polo-like kinase 1 (Plk1) overexpression enhances ionizing radiation-induced cancer formation in mice.
Nervous System Diseases
Structure-based design and confirmation of peptide ligands for neuronal polo-like kinase to promote neuroregeneration.
Neurilemmoma
Polo-like kinase 1 as a therapeutic target for malignant peripheral nerve sheath tumors (MPNST) and schwannomas.
Neuroblastoma
High levels of polo-like kinase 1 and phosphorylated translationally controlled tumor protein indicate poor prognosis in neuroblastomas.
Neuroblastoma
Participation of type II protein kinase A in the retinoic acid-induced growth inhibition of SH-SY5Y human neuroblastoma cells.
Neuroblastoma
Phosphorylation of endogenous proteins by adenosine 3':5'-monophosphate-dependent protein kinase in mouse neuroblastoma cells.
Neuroblastoma
Polo-like kinase 1 inhibition sensitizes neuroblastoma cells for vinca alkaloid-induced apoptosis.
Neuroblastoma
Polo-like kinase 1 is a therapeutic target in high-risk neuroblastoma.
Neuroblastoma
Polo-Like Kinase 4 (PLK4) Is Overexpressed in Central Nervous System Neuroblastoma (CNS-NB).
Neuroblastoma
Polo-like kinase 4 mediates epithelial-mesenchymal transition in neuroblastoma via PI3K/Akt signaling pathway.
Neuroblastoma
Small molecule kinase inhibitor screen identifies polo-like kinase 1 as a target for neuroblastoma tumor-initiating cells.
Neuroblastoma
The dual role of BI 2536, a small-molecule inhibitor that targets PLK1, in induction of apoptosis and attenuation of autophagy in neuroblastoma cells.
Neuroblastoma
The GSK461364 PLK1 inhibitor exhibits strong antitumoral activity in preclinical neuroblastoma models.
Neurofibrosarcoma
Polo-like kinase 1 as a therapeutic target for malignant peripheral nerve sheath tumors (MPNST) and schwannomas.
Neutropenia
Comparison of different semi-mechanistic models for chemotherapy-related neutropenia: application to BI 2536 a Plk-1 inhibitor.
Neutropenia
PLK-1 Targeted Inhibitors and Their Potential against Tumorigenesis.
Neutropenia
Semi-mechanistic population pharmacokinetic/pharmacodynamic model for neutropenia following therapy with the Plk-1 inhibitor BI 2536 and its application in clinical development.
Nevus
Multiple agminated Spitz nevi arising on a café au lait macule: review of the literature with contribution of another case.
Oral Submucous Fibrosis
Immunohistochemical expression of polo-like kinase 1 in oral squamous cell carcinoma and oral submucous fibrosis.
Osteoarthritis
siRNA targeting PLK-1 induces apoptosis of synoviocytes in rheumatoid arthritis.
Osteosarcoma
BI 2536-mediated PLK1 inhibition suppresses HOS and MG-63 osteosarcoma cell line growth and clonogenicity.
Osteosarcoma
CHOP negatively regulates Polo-like kinase 2 expression via recruiting C/EBP? to the upstream-promoter in human osteosarcoma cell line during ER stress.
Osteosarcoma
Cytotoxic effects of 15d-PGJ2 against osteosarcoma through ROS-mediated AKT and cell cycle inhibition.
Osteosarcoma
Inhibition of polo-like kinase 1 leads to the suppression of osteosarcoma cell growth in vitro and in vivo.
Osteosarcoma
Lentiviral shRNA screen of human kinases identifies PLK1 as a potential therapeutic target for osteosarcoma.
Osteosarcoma
Polo-Like Kinase 1 as a Potential Therapeutic Target for Osteosarcoma.
Osteosarcoma
Poly-l-lysine Functionalized Large Pore Cubic Mesostructured Silica Nanoparticles as Biocompatible Carriers for Gene Delivery.
Osteosarcoma
T-cell activation and early gene response in dogs.
Osteosarcoma
Targeting polo-like kinase 1 by NMS-P937 in osteosarcoma cell lines inhibits tumor cell growth and partially overcomes drug resistance.
Osteosarcoma
Targeting the centrosome and polo-like kinase 4 in osteosarcoma.
Osteosarcoma
Upregulation of Polo-like kinase 2 gene expression by GATA-1 acetylation in human osteosarcoma MG-63 cells.
Ovarian Neoplasms
Aurora Borealis (Bora), Which Promotes Plk1 Activation by Aurora A, Has an Oncogenic Role in Ovarian Cancer.
Ovarian Neoplasms
Blocking Mitotic Exit of Ovarian Cancer Cells by Pharmaceutical Inhibition of the Anaphase-Promoting Complex Reduces Chromosomal Instability.
Ovarian Neoplasms
Expression of polo-like kinase in ovarian cancer is associated with histological grade and clinical stage.
Ovarian Neoplasms
Multicentric parallel phase II trial of the polo-like kinase 1 inhibitor BI 2536 in patients with advanced head and neck cancer, breast cancer, ovarian cancer, soft tissue sarcoma and melanoma. The first protocol of the European Organization for Research and Treatment of Cancer (EORTC) Network Of Core Institutes (NOCI).
Ovarian Neoplasms
pH-responsive polymeric sirna carriers sensitize multidrug resistant ovarian cancer cells to doxorubicin via knockdown of polo-like kinase 1.
Ovarian Neoplasms
Polo-like kinase PLK 2 is an epigenetic determinant of chemosensitivity and clinical outcomes in ovarian cancer.
Ovarian Neoplasms
Synthetic lethality in CCNE1-amplified high grade serous ovarian cancer through combined inhibition of Polo-like kinase 1 and microtubule dynamics.
Ovarian Neoplasms
Therapeutic Gene Silencing Using Targeted Lipid Nanoparticles in Metastatic Ovarian Cancer.
Ovarian Neoplasms
YLZ-F5, a novel polo-like kinase 4 inhibitor, inhibits human ovarian cancer cell growth by inducing apoptosis and mitotic defects.
Pancreatic Neoplasms
A fine-needle aspirate-based vulnerability assay identifies polo-like kinase 1 as a mediator of gemcitabine resistance in pancreatic cancer.
Pancreatic Neoplasms
A phase I pharmacokinetic study of HMN-214, a novel oral stilbene derivative with polo-like kinase-1-interacting properties, in patients with advanced solid tumors.
Pancreatic Neoplasms
A phase II/III randomized study to compare the efficacy and safety of rigosertib plus gemcitabine versus gemcitabine alone in patients with previously untreated metastatic pancreatic cancer.
Pancreatic Neoplasms
Activity of the novel polo-like kinase 4 inhibitor CFI-400945 in pancreatic cancer patient-derived xenografts.
Pancreatic Neoplasms
Identification of human polo-like kinase 1 as a potential therapeutic target in pancreatic cancer.
Pancreatic Neoplasms
Overexpression of Polo-like kinase 1 is a common and early event in pancreatic cancer.
Pancreatic Neoplasms
Phase 1 study of rigosertib, an inhibitor of the phosphatidylinositol 3-kinase and polo-like kinase 1 pathways, combined with gemcitabine in patients with solid tumors and pancreatic cancer.
Pancreatic Neoplasms
Plk1 inhibition enhances the efficacy of gemcitabine in human pancreatic cancer.
Pancreatic Neoplasms
Regulation of cell apoptosis and proliferation in pancreatic cancer through PI3K/Akt pathway via Polo-like kinase 1.
Pancreatic Neoplasms
RNA interference-mediated silencing of the polo-like kinase 1 gene enhances chemosensitivity to gemcitabine in pancreatic adenocarcinoma cells.
Pancreatic Neoplasms
ROS-Responsive Polymeric Micelles for Triggered Simultaneous Delivery of PLK1 Inhibitor/miR-34a and Effective Synergistic Therapy in Pancreatic Cancer.
Pancreatic Neoplasms
Vaccinia-related kinase 2 drives pancreatic cancer progression by protecting Plk1 from Chfr-mediated degradation.
Pancreatic Neoplasms
Validation of Polo-like kinase 1 as a therapeutic target in pancreatic cancer cells.
Parkinson Disease
Design and synthesis of highly selective, orally active Polo-like kinase-2 (Plk-2) inhibitors.
Parkinson Disease
Identification of the PLK2-dependent phosphopeptidomeby quantitative proteomics.
Parkinson Disease
Insulin Resistance Promotes Parkinson's Disease through Aberrant Expression of ?-Synuclein, Mitochondrial Dysfunction, and Deregulation of the Polo-Like Kinase 2 Signaling.
Parkinson Disease
Selective and brain-permeable polo-like kinase-2 (Plk-2) inhibitors that reduce ?-synuclein phosphorylation in rat brain.
Pituitary Neoplasms
Role of E2F3 expression in modulating cellular proliferation rate in human bladder and prostate cancer cells.
Plasmacytoma
Resolution and general properties of different types of ribosomal protein kinases in mouse plasmocytoma.
Precursor Cell Lymphoblastic Leukemia-Lymphoma
Inhibiting Polo-like kinase 1 causes growth reduction and apoptosis in pediatric acute lymphoblastic leukemia cells.
Precursor Cell Lymphoblastic Leukemia-Lymphoma
Integrated analysis of CRLF2 signaling in acute lymphoblastic leukemia identifies Polo-like kinase 1 as a potential therapeutic target.
Precursor Cell Lymphoblastic Leukemia-Lymphoma
Therapeutic targeting of Polo-like kinase-1 and Aurora kinases in T-cell acute lymphoblastic leukemia.
Prion Diseases
Overexpression of PLK3 Mediates the Degradation of Abnormal Prion Proteins Dependent on Chaperone-Mediated Autophagy.
Prostatic Intraepithelial Neoplasia
Overexpression of cyclooxygenase-2 in human prostate carcinoma and prostatic intraepithelial neoplasia-association with increased expression of Polo-like kinase-1.
Prostatic Neoplasms
A ribonucleoprotein octamer for targeted siRNA delivery.
Prostatic Neoplasms
Androgen receptor as a driver of therapeutic resistance in advanced prostate cancer.
Prostatic Neoplasms
Apoptotic effects of genistein, biochanin-A and apigenin on LNCaP and PC-3 cells by p21 through transcriptional inhibition of polo-like kinase-1.
Prostatic Neoplasms
Cotargeting Polo-Like Kinase 1 and the Wnt/?-Catenin Signaling Pathway in Castration-Resistant Prostate Cancer.
Prostatic Neoplasms
Cross Talk between Wnt/?-Catenin and CIP2A/Plk1 Signaling in Prostate Cancer: Promising Therapeutic Implications.
Prostatic Neoplasms
Inhibition of Polo-like Kinase 1 (Plk1) Enhances the Antineoplastic Activity of Metformin in Prostate Cancer.
Prostatic Neoplasms
Overexpression of cyclooxygenase-2 in human prostate carcinoma and prostatic intraepithelial neoplasia-association with increased expression of Polo-like kinase-1.
Prostatic Neoplasms
Plk1 inhibition enhances the efficacy of androgen signaling blockade in castration-resistant prostate cancer.
Prostatic Neoplasms
Plk1-dependent microtubule dynamics promotes androgen receptor signaling in prostate cancer.
Prostatic Neoplasms
Polo-like kinase (Plk) 1 as a target for prostate cancer management.
Prostatic Neoplasms
Polo-like kinase (Plk) 1: a novel target for the treatment of prostate cancer.
Prostatic Neoplasms
Polo-like kinase 1 facilitates loss of Pten tumor suppressor-induced prostate cancer formation.
Prostatic Neoplasms
Polo-like kinase 1 induces epithelial-to-mesenchymal transition and promotes epithelial cell motility by activating CRAF/ERK signaling.
Prostatic Neoplasms
Polo-like kinase 1 is overexpressed in prostate cancer and linked to higher tumor grades.
Prostatic Neoplasms
Polo-like kinase 1, on the rise from cell cycle regulation to prostate cancer development.
Prostatic Neoplasms
Polo-like kinase 3 is associated with poor prognosis and regulates proliferation and metastasis in prostate cancer.
Prostatic Neoplasms
Prostate cancer: PLK-1 inhibition improves abiraterone efficacy.
Prostatic Neoplasms
Silencing of polo-like kinase (Plk) 1 via siRNA causes induction of apoptosis and impairment of mitosis machinery in human prostate cancer cells: implications for the treatment of prostate cancer.
Prostatic Neoplasms
Targeting prostate cancer cell lines with polo-like kinase 1 inhibitors as a single agent and in combination with histone deacetylase inhibitors.
Rectal Neoplasms
Polo-like kinase 1 as predictive marker and therapeutic target for radiotherapy in rectal cancer.
Rectal Neoplasms
Upregulated Polo-Like Kinase 1 Expression Correlates with Inferior Survival Outcomes in Rectal Cancer.
Retinoblastoma
Anexelekto /MER Tyrosine Kinase inhibitor ONO-7475 growth arrests and kills FMS-Like Tyrosine Kinase 3-Internal Tandem Duplication Mutant Acute Myeloid Leukemia cells by diverse mechanisms.
Retinoblastoma
Inhibition of polo-like kinase 1 promotes hyperthermia sensitivity via inactivation of heat shock transcription factor 1 in human retinoblastoma cells.
Retinoblastoma
Pharmaceutically inhibiting polo-like kinase 1 exerts a broad anti-tumour activity in retinoblastoma cell lines.
Rhabdoid Tumor
A functional screening of the kinome identifies the Polo-like kinase 4 as a potential therapeutic target for malignant rhabdoid tumors, and possibly, other embryonal tumors of the brain.
Rhabdoid Tumor
Inhibition of polo-like kinase 4 (PLK4): a new therapeutic option for rhabdoid tumors and pediatric medulloblastoma.
Rhabdoid Tumor
Targeting Polo-like kinase 1 in SMARCB1 deleted atypical teratoid rhabdoid tumor.
Rhabdomyosarcoma
A Perspective on Polo-Like Kinase-1 Inhibition for the Treatment of Rhabdomyosarcomas.
Rhabdomyosarcoma
Eribulin synergizes with Polo-like kinase 1 inhibitors to induce apoptosis in rhabdomyosarcoma.
Rhabdomyosarcoma
Small interfering RNA library screen of human kinases and phosphatases identifies polo-like kinase 1 as a promising new target for the treatment of pediatric rhabdomyosarcomas.
Sarcoma
Inhibition of polo like kinase 1 in sarcomas induces apoptosis that is dependent on Mcl-1 suppression.
Sarcoma
Multicentric parallel phase II trial of the polo-like kinase 1 inhibitor BI 2536 in patients with advanced head and neck cancer, breast cancer, ovarian cancer, soft tissue sarcoma and melanoma. The first protocol of the European Organization for Research and Treatment of Cancer (EORTC) Network Of Core Institutes (NOCI).
Sarcoma
Viral src gene products are related to the catalytic chain of mammalian cAMP-dependent protein kinase.
Sarcoma, Avian
Cytosolic malic dehydrogenase activity is associated with a putative substrate for the transforming gene product of Rous sarcoma virus.
Sarcoma, Avian
Protein kinase and its regulatory effect on reverse transcriptase activity of Rous sarcoma virus.
Sarcoma, Ewing
Synergistic induction of apoptosis by a polo-like kinase 1 inhibitor and microtubule-interfering drugs in Ewing sarcoma cells.
Schistosomiasis
Algorithmic Mapping and Characterization of the Drug-Induced Phenotypic-Response Space of Parasites Causing Schistosomiasis.
Schistosomiasis
Schistosoma mansoni Polo-like kinase 1: A mitotic kinase with key functions in parasite reproduction.
Schistosomiasis
Schistosoma mansoni Polo-like kinases and their function in control of mitosis and parasite reproduction.
Seizures
Mammalian target of rapamycin complex 1 activation negatively regulates Polo-like kinase 2-mediated homeostatic compensation following neonatal seizures.
Sepsis
LncRNA DANCR improves the dysfunction of the intestinal barrier and alleviates epithelial injury by targeting the miR-1306-5p/PLK1 axis in sepsis.
Sepsis
Polo-like kinase 1 protects intestinal epithelial cells from apoptosis during sepsis via the nuclear factor-?B pathway.
Skin Neoplasms
Polo-like kinase 1 (Plk1) in non-melanoma skin cancers.
Small Cell Lung Carcinoma
An open-label, phase II study of the polo-like kinase-1 (Plk-1) inhibitor, BI 2536, in patients with relapsed small cell lung cancer (SCLC).
Small Cell Lung Carcinoma
Polo-like kinase 1 inhibitor BI 6727 induces DNA damage and exerts strong antitumor activity in small cell lung cancer.
Squamous Cell Carcinoma of Head and Neck
Immunohistochemical expression of polo-like kinase 1 in oral squamous cell carcinoma and oral submucous fibrosis.
Squamous Cell Carcinoma of Head and Neck
Mutations of the LIM protein AJUBA mediate sensitivity of head and neck squamous cell carcinoma to treatment with cell-cycle inhibitors.
Squamous Cell Carcinoma of Head and Neck
Targeting polo-like kinase 1 enhances radiation efficacy for head-and-neck squamous cell carcinoma.
Stomach Neoplasms
Advances of Molecular Targeted Therapy in Gastric Cancer.
Stomach Neoplasms
BI2536, a potent and selective inhibitor of polo-like kinase 1, in combination with cisplatin exerts synergistic effects on gastric cancer cells.
Stomach Neoplasms
Clinical Significance of Polo-Like Kinase 4 as a Marker for Advanced Tumor Stage and Dismal Prognosis in Patients With Surgical Gastric Cancer.
Stomach Neoplasms
Effect of PLK1 inhibition on cisplatin-resistant gastric cancer cells.
Stomach Neoplasms
Effects of PLK1 on proliferation, invasion and metastasis of gastric cancer cells through epithelial-mesenchymal transition.
Stomach Neoplasms
Expression patterns of polo-like kinase 1 in human gastric cancer.
Stomach Neoplasms
Gastric Cancer Patients with High PLK1 Expression and DNA Aneuploidy Correlate with Poor Prognosis.
Stomach Neoplasms
Helicobacter pylori promotes gastric epithelial cell survival through the PLK1/PI3K/Akt pathway.
Stomach Neoplasms
Inhibitory effect of Polo-like kinase 1 depletion on mitosis and apoptosis of gastric cancer cells.
Stomach Neoplasms
Involvement of Polo-like kinase 1 (Plk1) in quiescence regulation of cancer stem-like cells of the gastric cancer cell lines.
Stomach Neoplasms
MicroRNA-505 suppresses gastric cancer cell proliferation and invasion by directly targeting Polo-like kinase-1.
Stomach Neoplasms
Pharmacogenomic Analysis Reveals CCNA2 as a Predictive Biomarker of Sensitivity to Polo-Like Kinase I Inhibitor in Gastric Cancer.
Stomach Neoplasms
Silencing of polo-like kinase 2 increases cell proliferation and decreases apoptosis in SGC-7901 gastric cancer cells.
Stomach Neoplasms
[Mitosis arrest caused by inhibition of PLK1 expression in gastric cancer MKN45 cells]
Synucleinopathies
Identification of the PLK2-dependent phosphopeptidomeby quantitative proteomics.
Thyroid Carcinoma, Anaplastic
Identification of Polo-like kinase 1 as a potential therapeutic target in anaplastic thyroid carcinoma.
Thyroid Carcinoma, Anaplastic
PLK1 gene suppresses cell invasion of undifferentiated thyroid carcinoma through the inhibition of CD44v6, MMP-2 and MMP-9.
Thyroid Neoplasms
[Cellular tumor markers in thyroid cancer]
Triple Negative Breast Neoplasms
Anticancer effects of radiation therapy combined with Polo-Like Kinase 4 (PLK4) inhibitor CFI-400945 in triple negative breast cancer.
Triple Negative Breast Neoplasms
Combination Treatment of Polo-Like Kinase 1 and Tankyrase-1 Inhibitors Enhances Anticancer Effect in Triple-negative Breast Cancer Cells.
Triple Negative Breast Neoplasms
Deciphering the performance of polo-like kinase 1 in triple-negative breast cancer progression according to the centromere protein U-phosphorylation pathway.
Triple Negative Breast Neoplasms
Dendrimer mediated targeting of siRNA against polo-like kinase for the treatment of triple negative breast cancer.
Triple Negative Breast Neoplasms
Polo-like kinase 1 (Plk1) inhibition synergizes with taxanes in triple negative breast cancer.
Triple Negative Breast Neoplasms
Polo-like kinase 1: a potential therapeutic option in combination with conventional chemotherapy for the management of patients with triple-negative breast cancer.
Triple Negative Breast Neoplasms
Selective transferrin coating as a facile strategy to fabricate BBB-permeable and targeted vesicles for potent RNAi therapy of brain metastatic breast cancer in vivo.
Triple Negative Breast Neoplasms
Systemic Administration of siRNA with Anti-HB-EGF Antibody-Modified Lipid Nanoparticles for the Treatment of Triple-Negative Breast Cancer.
Tuberous Sclerosis
Hamartin, the tuberous sclerosis complex 1 gene product, interacts with polo-like kinase 1 in a phosphorylation-dependent manner.
Urinary Bladder Neoplasms
Down-regulation of Polo-like kinase 4 (PLK4) induces G1 arrest via activation of the p38/p53/p21 signaling pathway in bladder cancer.
Urinary Bladder Neoplasms
Intravesical administration of small interfering RNA targeting PLK-1 successfully prevents the growth of bladder cancer.
Urinary Bladder Neoplasms
Overexpression of polo-like kinase 1 (PLK1) and chromosomal instability in bladder cancer.
Urinary Bladder Neoplasms
PLK-1 Silencing in Bladder Cancer by siRNA Delivered With Exosomes.
Urinary Bladder Neoplasms
Role of E2F3 expression in modulating cellular proliferation rate in human bladder and prostate cancer cells.
Urinary Bladder Neoplasms
Targeted inhibition of Polo-like kinase 1 by a novel small-molecule inhibitor induces mitotic catastrophe and apoptosis in human bladder cancer cells.
Uterine Cervical Neoplasms
[Knockdown of Polo-like kinase 1 (PLK1) inhibits the growth of cervical cancer HeLa cells].
Virus Diseases
Dysregulation of the polo-like kinase pathway in CD4+ T cells is characteristic of pathogenic simian immunodeficiency virus infection.
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0.00126
(7R)-2-[5-(2,4-difluorophenyl)-1H-pyrazol-4-yl]-7-ethyl-5-methyl-8-(1-methyl-1H-pyrazol-4-yl)-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.00135
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(1-methyl-1H-pyrazol-3-yl)-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.00327
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(1-methyl-1H-pyrazol-4-yl)-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.0288
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(1-methyl-1H-pyrazol-5-yl)-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.00867
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(1H-pyrazol-4-yl)-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.00355
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(3,3,3-trifluoropropyl)-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.00753
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-[(3S)-tetrahydrofuran-3-yl]-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.00025
(7R)-7-ethyl-5-methyl-2-(2-phenyl-1H-imidazol-1-yl)-8-(3,3,3-trifluoropropyl)-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.00087
(7R)-7-ethyl-5-methyl-2-(2-phenyl-1H-imidazol-1-yl)-8-(propan-2-yl)-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.00776
(7R)-7-ethyl-5-methyl-2-(2-phenyl-1H-imidazol-1-yl)-8-(pyrimidin-5-yl)-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.00048
(7R)-7-ethyl-5-methyl-2-(2-phenyl-1H-imidazol-1-yl)-8-[(3R)-tetrahydrofuran-3-yl]-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.00038
(7R)-7-ethyl-5-methyl-2-(2-phenyl-1H-imidazol-1-yl)-8-[(3S)-tetrahydrofuran-3-yl]-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.00303
(7R)-7-ethyl-5-methyl-8-(1H-pyrazol-4-yl)-2-[5-(1,3-thiazol-2-yl)-1H-pyrazol-4-yl]-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.00025
(7R)-7-ethyl-5-methyl-8-(tetrahydro-2H-pyran-4-yl)-2-[5-(1,3-thiazol-2-yl)-1H-pyrazol-4-yl]-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.00141
(7R)-7-ethyl-5-methyl-8-(tetrahydrofuran-3-yl)-2-[5-(1,3-thiazol-2-yl)-1H-pyrazol-4-yl]-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.00939
(7R)-8-(3,3-difluorocyclobutyl)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.01
1-(1-methylpiperidin-4-yl)-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
larger than 0.010, pH 7.9, 25°C
0.000102
1-(2-hydroxyethyl)-2-(2-[[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridin-4-one
Homo sapiens
pH and temperature not specified in the publication
0.000151
1-(2-hydroxyethyl)-5-(2-[[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-1H-pyrrole-3-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.009
1-acetyl-L-prolyl-L-leucyl-3-(5-[[(Z)-benzylideneamino]oxy]pentyl)-L-histidyl-L-seryl-O-phosphono-L-threoninamide
Homo sapiens
at pH 7.4 and 25°C
0.00505
1-acetyl-L-prolyl-L-leucyl-3-(6-[[(Z)-benzylideneamino]oxy]hexyl)-L-histidyl-L-seryl-O-phosphono-L-threoninamide
Homo sapiens
at pH 7.4 and 25°C
0.000121
1-acetyl-L-prolyl-L-leucyl-3-(8-phenyloctyl)-L-histidyl-L-seryl-O-phosphono-L-threoninamide
Homo sapiens
at pH 7.4 and 25°C
0.00155
1-acetyl-L-prolyl-L-leucyl-3-[5-([(Z)-[(2-fluoro-6-phenoxyphenyl)methylidene]amino]oxy)pentyl]-L-histidyl-L-seryl-O-phosphono-L-threoninamide
Homo sapiens
at pH 7.4 and 25°C
0.000139
1-acetyl-L-prolyl-L-leucyl-3-[6-(2-phenoxyphenyl)hexyl]-L-histidyl-L-seryl-O-phosphono-L-threoninamide
Homo sapiens
at pH 7.4 and 25°C
0.00067
1-acetyl-L-prolyl-L-leucyl-3-[6-([(Z)-[(2-fluoro-6-phenoxyphenyl)methylidene]amino]oxy)hexyl]-L-histidyl-L-seryl-O-phosphono-L-threoninamide
Homo sapiens
at pH 7.4 and 25°C
0.000066
1-acetyl-L-prolyl-L-leucyl-3-[8-(2-fluoro-6-phenoxyphenyl)octyl]-L-histidyl-L-seryl-O-phosphono-L-threoninamide
Homo sapiens
at pH 7.4 and 25°C
0.000052
1-acetyl-L-prolyl-L-leucyl-3-[8-(2-phenoxyphenyl)octyl]-L-histidyl-L-seryl-O-phosphono-L-threoninamide
Homo sapiens
at pH 7.4 and 25°C
0.000043
1-acetyl-L-prolyl-L-leucyl-3-[8-([1,1'-biphenyl]-2-yl)octyl]-L-histidyl-L-seryl-O-phosphono-L-threoninamide
Homo sapiens
at pH 7.4 and 25°C
0.000032
1-acetyl-L-prolyl-L-leucyl-3-[8-[2-(benzyloxy)phenyl]octyl]-L-histidyl-L-seryl-O-phosphono-L-threoninamide
Homo sapiens
at pH 7.4 and 25°C
0.000139
1-acetyl-L-prolyl-L-leucyl-3-[9-(2-fluoro-6-phenoxyphenyl)nonyl]-L-histidyl-L-seryl-O-phosphono-L-threoninamide
Homo sapiens
at pH 7.4 and 25°C
0.3
1-acetyl-L-prolyl-L-leucyl-L-histidyl-L-seryl-O-phosphono-L-threoninamide
Homo sapiens
IC50 above 0.3 mM, at pH 7.4 and 25°C
0.000143
1-cyclohexyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.000009
1-methyl-2-(2-[[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridin-4-one
Homo sapiens
pH and temperature not specified in the publication
0.000015
1-methyl-5-(2-[[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-1H-pyrrole-3-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000018
1-methyl-5-(2-[[5-(piperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-1H-pyrrole-3-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000068
1-methyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.00011
1-methyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxylic acid
Homo sapiens
pH 7.9, 25°C
0.000015
1-methyl-8-[(2-methylphenyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.000488
1-methyl-8-[(2-nitrophenyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.000278
1-methyl-8-[(2-phenoxyphenyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.003733
1-methyl-8-[(2-sulfamoylphenyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.01
1-methyl-8-[(3-nitrophenyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
larger than 0.010, pH 7.9, 25°C
0.01
1-methyl-8-[(4-nitrophenyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
larger than 0.010, pH 7.9, 25°C
0.00011
1-methyl-8-[[2-(methylamino)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.000097
1-methyl-8-[[2-(methylsulfanyl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.000949
1-methyl-8-[[2-(phenylamino)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.001969
1-methyl-8-[[2-(phenylcarbonyl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.002033
1-methyl-8-[[2-(phenylsulfanyl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.000365
1-methyl-8-[[2-(propan-2-yl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.000432
1-methyl-8-[[2-(trifluoromethyl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.000051
1-methyl-8-[[3-(trifluoromethyl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.000872
1-methyl-8-[[4-(trifluoromethyl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.01
1-methyl-N-phenyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
larger than 0.010, pH 7.9, 25°C
0.01
1-phenyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
larger than 0.010, pH 7.9, 25°C
0.00347
1-[2-hydroxy-3-(4-methylpiperazin-1-yl)propyl]-1H-indole-3-carboxylic acid
Homo sapiens
pH 7.5, 30°C
0.0021
1-[2-hydroxy-3-(piperidin-1-yl)propyl]-1H-indole-3-carboxylic acid
Homo sapiens
pH 7.5, 30°C
0.00484
1-[2-hydroxy-3-(pyrrolidin-1-yl)propyl]-1H-indole-3-carboxylic acid
Homo sapiens
pH 7.5, 30°C
0.00191
1-[3-(diethylamino)-2-hydroxypropyl]-1H-indole-3-carboxylic acid
Homo sapiens
pH 7.5, 30°C
0.0253
2'-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5'-methyl-8'-(propan-2-yl)-5',8'-dihydro-6'H-spiro[cyclobutane-1,7'-pteridin]-6'-one
Homo sapiens
22°C, pH not specified in the publication
0.000028
2-(2-[[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-1-(2,2,2-trifluoroethyl)-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridin-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00218
2-methyl-5-(propan-2-yl)cyclohexa-2,5-diene-1,4-dione
Homo sapiens
pH 7.5, 30°C
0.00348
2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-7-(2,2,2-trifluoroethyl)-8-(3,3,3-trifluoropropyl)-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.0000008
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
Homo sapiens
-
0.000001
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-methoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
Homo sapiens
-
0.000001
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(2R)-2,3-dihydroxypropyl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
Homo sapiens
-
0.000003
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(2R)-2-hydroxy-3-pyrrolidin-1-ylpropyl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
Homo sapiens
-
0.000004
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(4R)-1-methylazepan-4-yl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
Homo sapiens
-
0.000003
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(4S)-1-methylazepan-4-yl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
Homo sapiens
-
0.000006
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)methoxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
Homo sapiens
-
0.000002
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
Homo sapiens
-
0.000004
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[3-(dimethylamino)propoxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
Homo sapiens
-
0.00003
3-[(1S)-1-(2-chlorophenyl)ethoxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
Homo sapiens
-
0.000002
3-[(2-chlorobenzyl)oxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
Homo sapiens
-
0.00571
3-[1-[2-hydroxy-3-(piperidin-1-yl)propyl]-1H-indol-3-yl]propanoic acid
Homo sapiens
pH 7.5, 30°C
0.0029
3-[1-[2-hydroxy-3-(pyrrolidin-1-yl)propyl]-1H-indol-3-yl]propanoic acid
Homo sapiens
pH 7.5, 30°C
0.00000083
4-((R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydro-pteridin-2-ylamino)-3-methoxy-N-(1-methyl-piperidin-4-yl)-benzamide
Homo sapiens
-
0.00376
4-[7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-6-oxo-6,7-dihydropteridin-8(5H)-yl]benzonitrile
Homo sapiens
22°C, pH not specified in the publication
0.0000018
5-(2-[[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-1-(2,2,2-trifluoroethyl)-1H-pyrrole-3-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000272
5-(2-[[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-1-[2-(tetrahydro-2H-pyran-4-yloxy)ethyl]-1H-pyrrole-3-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000002
5-(5,6-dimethoxy-1H-benzimidazol-1-yl)-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide
Homo sapiens
-
0.000003
5-(6-methoxy-1H-benzimidazol-1-yl)-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
Homo sapiens
-
0.000003
5-[6-(piperidin-4-yloxy)-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
Homo sapiens
-
0.000007
5-[6-[(1-methylpiperidin-4-yl)methoxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
Homo sapiens
-
0.000002
5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
Homo sapiens
-
0.00716
7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5,7-dimethyl-8-(3,3,3-trifluoropropyl)-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.00342
7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(1H-pyrazol-3-yl)-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.00182
7-ethyl-5-methyl-8-(1-methyl-1H-pyrazol-4-yl)-2-[5-(1,3-thiazol-2-yl)-1H-pyrazol-4-yl]-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.00182
7-ethyl-5-methyl-8-(1-methyl-1H-pyrazol-4-yl)-2-[5-(pyridin-2-yl)-1H-pyrazol-4-yl]-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.00283
7-ethyl-5-methyl-8-phenyl-2-(2-phenyl-1H-imidazol-1-yl)-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.00234
7-ethyl-8-(4-fluorophenyl)-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.00032
8-(3,3-difluorocyclopentyl)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.001565
8-(biphenyl-2-ylamino)-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.000006
8-(phenylamino)-1-(2,2,2-trifluoroethyl)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.00043
8-(phenylamino)-1-(propan-2-yl)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.01
8-(phenylamino)-1-[2-(piperidin-1-yl)ethyl]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
larger than 0.010, pH 7.9, 25°C
0.000248
8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.000346
8-[(2-acetylphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.00015
8-[(2-aminophenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.000943
8-[(2-benzylphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.002076
8-[(2-carbamoylphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.000125
8-[(2-fluorophenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.000042
8-[(2-methoxyphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.0001
8-[(3-acetylphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.000135
8-[(3-methoxyphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.000197
8-[(4-acetylphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.000256
8-[(4-methoxyphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.002523
8-[[2-(acetylamino)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.002051
8-[[2-acetyl-3-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.000464
8-[[2-acetyl-4-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.000109
8-[[2-acetyl-5-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.00004
8-[[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.000007
8-[[2-methoxy-5-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.00000083
BI 2536
Homo sapiens
pH 7.5, 30°C
0.00000087
BI 6727
Homo sapiens
pH 7.5, 30°C
0.0008
BI-2536
Homo sapiens
-
0.008
BTO-1
Homo sapiens
-
0.0098
cyclic (-CH2-CO-Pro-Leu-His-Ser-pThr-Cys-S-)
Homo sapiens
25°C, pH not specified in the publication
0.0085
cyclic [-CH2-CO-N[2-(1H-indol-3-yl)ethyl]-CH2-CO-Leu-His-Ser-pThr-NH-CH[CONH2]-CH2-S-]
Homo sapiens
25°C, pH not specified in the publication
0.0048
cyclic [-CH2-CO-N[3-[[2-(1H-indol-3-yl)ethyl]amino]-3-oxopropyl]-CH2-CO-Leu-His-Ser-p-Thr-NH-CH[CONH2]-CH2-S-]
Homo sapiens
25°C, pH not specified in the publication
0.0026
cyclic [-CH2-CO-N[6-[[2-(1-acetyl-1H-indol-3-yl)ethyl]amino]-6-oxohexyl]-CH2-CO-Leu-His-Ser-pThr-NH-CH[CONH2]-CH2-S-]
Homo sapiens
25°C, pH not specified in the publication
0.0011
cyclic [-CH2-CO-N[6-[[2-(1-acetyl-1H-indol-3-yl)ethyl]amino]-6-oxohexyl]-CH2-CO-Leu-His[N3-(8-phenyloctyl)]-Ser-pThr-NH-CH[CONH2]-CH2-S-]
Homo sapiens
25°C, pH not specified in the publication
0.01
ethyl 1-methyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxylate
Homo sapiens
larger than 0.010, pH7.9, 25°C
0.001117
methyl 2-[(3-carbamoyl-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazolin-8-yl)amino]benzoate
Homo sapiens
pH 7.9, 25°C
0.004215
N,1-dimethyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
pH 7.9, 25°C
0.0026
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-2-methylbenzamide
Homo sapiens
pH 7.5, 30°C
0.01
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-2-nitrobenzamide
Homo sapiens
pH 7.5, 30°C
0.00322
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-chlorobenzylaniline
Homo sapiens
pH 7.5, 30°C
0.00093
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-methoxybenzamide
Homo sapiens
pH 7.5, 30°C
0.00205
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-methoxybenzylaniline
Homo sapiens
pH 7.5, 30°C
0.00709
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-methylbenzamide
Homo sapiens
pH 7.5, 30°C
0.00466
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-methylbenzylaniline
Homo sapiens
pH 7.5, 30°C
0.01
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-nitrobenzamide
Homo sapiens
pH 7.5, 30°C
0.01
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-nitrobenzylaniline
Homo sapiens
pH 7.5, 30°C
0.00683
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-acetamide
Homo sapiens
pH 7.5, 30°C
0.00633
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-benzamide
Homo sapiens
pH 7.5, 30°C
0.00948
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-benzylaniline
Homo sapiens
pH 7.5, 30°C
0.00559
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)-2-methylbenzamide
Homo sapiens
pH 7.5, 30°C
0.01
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)-2-nitrobenzamide
Homo sapiens
pH 7.5, 30°C
0.00068
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)-4-methoxybenzamide
Homo sapiens
pH 7.5, 30°C
0.01
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)-4-nitrobenzamide
Homo sapiens
pH 7.5, 30°C
0.0047
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)acetamide
Homo sapiens
pH 7.5, 30°C
0.01
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)benzamide
Homo sapiens
pH 7.5, 30°C
0.00702
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)benzylaniline
Homo sapiens
pH 7.5, 30°C
0.01
N-cyclopentyl-1-methyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
larger than 0.010, pH 7.9, 25°C
0.01
N-cyclopropyl-1-methyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
larger than 0.010, pH 7.9, 25°C
0.0000002
N-[4-[(6-chloropyridin-3-yl)methoxy]-3-methoxybenzyl]-2-(3,4-dimethoxyphenyl)ethanamine
Homo sapiens
-
0.000009
ONO1910
Homo sapiens
-
0.00034 - 0.00053
PHA-680626
0.000817
tert-butyl 1-methyl-2-(2-[[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-4-oxo-1,4,6,7-tetrahydro-5H-pyrrolo[3,2-c]pyridine-5-carboxylate
Homo sapiens
pH and temperature not specified in the publication
0.00218
thymoquinone
Homo sapiens
pH 7.5, 30°C
0.00188
[1-[2-hydroxy-3-(4-methylpiperazin-1-yl)propyl]-1H-indol-3-yl]acetic acid
Homo sapiens
pH 7.5, 30°C
0.00096
[1-[2-hydroxy-3-(morpholin-4-yl)propyl]-1H-indol-3-yl]acetic acid
Homo sapiens
pH 7.5, 30°C
0.00041
[1-[2-hydroxy-3-(piperidin-1-yl)propyl]-1H-indol-3-yl]acetic acid
Homo sapiens
pH 7.5, 30°C
0.00013
[1-[2-hydroxy-3-(pyrrolidin-1-yl)propyl]-1H-indol-3-yl]acetic acid
Homo sapiens
pH 7.5, 30°C
0.00264
[1-[3-(diethylamino)-2-hydroxypropyl]-1H-indol-3-yl]acetic acid
Homo sapiens
pH 7.5, 30°C
0.00256
(1R)-1-[(3S,6S,9S,12S,15S)-19-(6-[[2-(1-acetyl-1H-indol-3-yl)ethyl]amino]-6-oxohexyl)-3-carbamoyl-9-(hydroxymethyl)-12-(1H-imidazol-5-ylmethyl)-15-(2-methylpropyl)-5,8,11,14,17,20-hexaoxo-1-thia-4,7,10,13,16,19-hexaazacyclohenicosan-6-yl]ethyl phosphate
Homo sapiens
pH and temperature not specified in the publication
-
0.00108
(1R)-1-[(3S,6S,9S,12S,15S)-19-(6-[[2-(1-acetyl-1H-indol-3-yl)ethyl]amino]-6-oxohexyl)-3-carbamoyl-9-(hydroxymethyl)-15-(2-methylpropyl)-5,8,11,14,17,20-hexaoxo-12-[[1-(9-phenylnonyl)-1H-imidazol-5-yl]methyl]-1-thia-4,7,10,13,16,19-hexaazacyclohenicosan-6-yl]ethyl phosphate
Homo sapiens
pH and temperature not specified in the publication
0.0032
(2Z)-2-(5-bromo-2-methoxybenzylidene)-6-methyl-7H-[1,3]thiazolo[3,2-b][1,2,4]triazine-3,7(2H)-dione
Homo sapiens
pH and temperature not specified in the publication
0.0045
(3S)-4-amino-4-oxo-3-([[2-(4-phenylbutyl)-1-(2-phenylethyl)-1H-benzimidazol-5-yl]carbonyl]amino)butan-2-yl phosphate
Homo sapiens
pH and temperature not specified in the publication
0.00114 - 0.00136
(4E)-5-methyl-4-[[(2-methylbenzoyl)oxy]imino]-2-(propan-2-yl)cyclohexa-2,5-dien-1-one
0.000014
(4R)-1-acetyl-4-(4-phenylbutoxy)prolyl-L-leucyl-L-histidyl-L-seryl-O-phosphono-L-threoninamide
Homo sapiens
pH and temperature not specified in the publication
122
(4R)-1-acetyl-4-[[(E)-(3-phenylpropylidene)amino]oxy]prolyl-L-leucyl-L-histidyl-L-seryl-O-phosphono-L-threoninamide
Homo sapiens
pH and temperature not specified in the publication
0.000103
(7R)-2-[5-(2,4-difluorophenyl)-1H-pyrazol-4-yl]-7-ethyl-5-methyl-8-(1-methyl-1H-pyrazol-4-yl)-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.000007
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(1-methyl-1H-pyrazol-3-yl)-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.000021
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(1-methyl-1H-pyrazol-4-yl)-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.000532
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(1-methyl-1H-pyrazol-5-yl)-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.000012
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(1H-pyrazol-4-yl)-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.000042
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(3,3,3-trifluoropropyl)-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.00104
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(oxetan-3-yl)-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.000033
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-[(3S)-tetrahydrofuran-3-yl]-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.000009
(7R)-7-ethyl-5-methyl-2-(2-phenyl-1H-imidazol-1-yl)-8-(3,3,3-trifluoropropyl)-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.000025
(7R)-7-ethyl-5-methyl-2-(2-phenyl-1H-imidazol-1-yl)-8-(propan-2-yl)-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.000044
(7R)-7-ethyl-5-methyl-2-(2-phenyl-1H-imidazol-1-yl)-8-(pyrimidin-5-yl)-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.000021
(7R)-7-ethyl-5-methyl-2-(2-phenyl-1H-imidazol-1-yl)-8-[(3R)-tetrahydrofuran-3-yl]-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.000008
(7R)-7-ethyl-5-methyl-2-(2-phenyl-1H-imidazol-1-yl)-8-[(3S)-tetrahydrofuran-3-yl]-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.000092
(7R)-7-ethyl-5-methyl-8-(1H-pyrazol-4-yl)-2-[5-(1,3-thiazol-2-yl)-1H-pyrazol-4-yl]-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.000036
(7R)-7-ethyl-5-methyl-8-(tetrahydro-2H-pyran-4-yl)-2-[5-(1,3-thiazol-2-yl)-1H-pyrazol-4-yl]-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.000039
(7R)-7-ethyl-5-methyl-8-(tetrahydrofuran-3-yl)-2-[5-(1,3-thiazol-2-yl)-1H-pyrazol-4-yl]-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.000012
(7R)-8-(3,3-difluorocyclobutyl)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.38
1-(26-oxo-2,5,8,11,14,17,20,23-octaoxahexacosan-26-yl)-L-prolyl-L-leucyl-3-(8-phenyloctyl)-L-histidyl-L-seryl-(3R)-4-phosphono-L-valinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000025 - 0.000017
1-acetyl-L-prolyl-L-leucyl-3-(8-phenyloctyl)-L-histidyl-L-seryl-O-phosphono-L-threoninamide
Homo sapiens
pH and temperature not specified in the publication
0.085
1-acetyl-L-prolyl-L-leucyl-3-[3-(2-hydroxyethyl)-1-(8-phenyloctyl)-1H-imidazol-3-ium-5-yl]-L-alanyl-L-seryl-O-phosphono-L-threoninamide
Homo sapiens
pH and temperature not specified in the publication
0.055
1-acetyl-L-prolyl-L-leucyl-3-[3-(2-hydroxyethyl)-1-(8-phenyloctyl)-1H-imidazol-3-ium-5-yl]-L-alanyl-L-seryl-O-[[[(2,2-dimethylpropanoyl)oxy]methoxy](hydroxy)phosphoryl]-L-threoninamide
Homo sapiens
pH and temperature not specified in the publication
0.000009 - 0.000014
1-methyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
0.000002 - 0.000006
1-methyl-8-[(2-methylphenyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
0.000051 - 0.002666
1-methyl-8-[(2-phenoxyphenyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
0.000011 - 0.000012
1-methyl-8-[[2-(methylamino)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
0.000014 - 0.000016
1-methyl-8-[[2-(methylsulfanyl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
0.000146 - 0.000509
1-methyl-8-[[2-(propan-2-yl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
0.000095 - 0.000109
1-methyl-8-[[2-(trifluoromethyl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
0.00115
2'-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5'-methyl-8'-(propan-2-yl)-5',8'-dihydro-6'H-spiro[cyclobutane-1,7'-pteridin]-6'-one
Homo sapiens
22°C, pH not specified in the publication
0.00271
2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5,7,7-trimethyl-8-(propan-2-yl)-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.00012
2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-7-(2,2,2-trifluoroethyl)-8-(3,3,3-trifluoropropyl)-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.000004 - 0.000214
3-(1,3-benzodioxol-5-yl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
0.005689
3-(2-methylcyclohexyl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
Homo sapiens
-
0.004927
3-(3,4-dimethoxyphenyl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
Homo sapiens
-
0.00033
3-(3,4-dimethylphenyl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
Homo sapiens
-
0.000625
3-(3-chlorophenyl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
Homo sapiens
-
0.000549 - 0.01
3-(3-methylphenyl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
0.00117
3-(4-methylphenyl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
Homo sapiens
-
0.000779
3-(4-methylthiophen-3-yl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
Homo sapiens
-
0.02
3-benzyl-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
Homo sapiens
>0.020
0.001616
3-phenyl-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
Homo sapiens
-
0.000006 - 0.000025
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.000035 - 0.000321
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-methoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.000061 - 0.000073
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(2R)-2,3-dihydroxypropyl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.000045 - 0.00061
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(2R)-2-hydroxy-3-pyrrolidin-1-ylpropyl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.000013 - 0.00025
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(4R)-1-methylazepan-4-yl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.000017 - 0.00024
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(4S)-1-methylazepan-4-yl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.000034 - 0.0011
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)methoxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
0.000003 - 0.00063
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
0.000032 - 0.00046
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[3-(dimethylamino)propoxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
0.000044 - 0.000994
3-[(1S)-1-(2-chlorophenyl)ethoxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.000009 - 0.00114
3-[(2-chlorobenzyl)oxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.007479
3-[1-(5-[[(1S)-1-phenylethyl]amino]isoxazolo[5,4-c]pyridin-3-yl)piperidin-3-yl]propanamide
Homo sapiens
-
0.000099
3-[3-chloro-5-(5-[[(1S)-1-phenylethyl]amino]isoxazolo[5,4-c]pyridin-3-yl)phenyl]propan-1-ol
Homo sapiens
-
0.000051 - 0.001382
3-[3-chloro-5-(5-[[(1S)-1-phenylethyl]amino]isoxazolo[5,4-c]pyridin-3-yl)phenyl]propanamide
0.000031
4-[7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-6-oxo-6,7-dihydropteridin-8(5H)-yl]benzonitrile
Homo sapiens
22°C, pH not specified in the publication
0.000009
5-(5,6-dimethoxy-1H-benzimidazol-1-yl)-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide
Homo sapiens
-
0.000041 - 0.000476
5-(6-methoxy-1H-benzimidazol-1-yl)-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
0.000015 - 0.00035
5-[6-(piperidin-4-yloxy)-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
0.00003 - 0.00055
5-[6-[(1-methylpiperidin-4-yl)methoxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
0.000003 - 0.00027
5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
0.00003
7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5,7-dimethyl-8-(3,3,3-trifluoropropyl)-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.000009
7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(1H-pyrazol-3-yl)-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.00013
7-ethyl-5-methyl-8-(1-methyl-1H-pyrazol-4-yl)-2-[5-(1,3-thiazol-2-yl)-1H-pyrazol-4-yl]-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.000168
7-ethyl-5-methyl-8-(1-methyl-1H-pyrazol-4-yl)-2-[5-(pyridin-2-yl)-1H-pyrazol-4-yl]-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.000017
7-ethyl-5-methyl-8-phenyl-2-(2-phenyl-1H-imidazol-1-yl)-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.000015
7-ethyl-8-(4-fluorophenyl)-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.000013
8-(3,3-difluorocyclopentyl)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-7,8-dihydropteridin-6(5H)-one
Homo sapiens
22°C, pH not specified in the publication
0.000103 - 0.000261
8-[(2-acetylphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
0.000012 - 0.000013
8-[(2-aminophenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
0.000027 - 0.000037
8-[(2-fluorophenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
0.000013 - 0.000024
8-[(2-methoxyphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
0.000049 - 0.002104
8-[[2-(acetylamino)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
0.01
8-[[2-acetyl-3-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
larger than 0.010
0.002292 - 0.01
8-[[2-acetyl-4-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
0.01
8-[[2-acetyl-5-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
larger than 0.010
0.000066 - 0.000082
8-[[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
0.000238 - 0.00045
8-[[2-methoxy-5-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
0.00000083
BI 2536
Homo sapiens
-
-
0.0000008
BI2536
Homo sapiens
-
-
0.00000087
BI6727
Homo sapiens
-
-
0.00000005
GSK461364A
Homo sapiens
-
less than 50 nM
0.00525
LY294002
Homo sapiens
-
-
0.0126
morin
Homo sapiens
-
-
0.00082
N-adamantylacetyl-L-prolyl-L-leucyl-L-histidyl-L-seryl-O-phosphono-L-threonyl-L-methioninamide
Homo sapiens
pH and temperature not specified in the publication
0.003007
N-[(1S)-1-phenylethyl]-3-thiophen-2-ylisoxazolo[5,4-c]pyridin-5-amine
Homo sapiens
-
0.00025
N-[3-(1-benzothiophen-2-yl)propanoyl]-alpha-aspartyl-L-prolyl-L-prolyl-L-leucyl-L-histidyl-L-seryl-O-phosphono-L-threonyl-L-alaninamide
Homo sapiens
pH and temperature not specified in the publication
0.00053
PHA-680626
Homo sapiens
-
0.0018
PL-42
Homo sapiens
pH and temperature not specified in the publication
0.00036
PL-49
Homo sapiens
pH and temperature not specified in the publication
0.064
quercetin
Homo sapiens
-
-
0.0000002
SBE13
Homo sapiens
-
immunoprecipitated Plk1 from HeLa cells
0.002
scytonemin
Homo sapiens
-
additional information
additional information
Homo sapiens
IC50 values for cell growth inhibition of HeLa and MCF-7 cells
-
0.14
AMPPNP
Homo sapiens
mutant T210D
0.155
AMPPNP
Homo sapiens
mutant T210V
0.166
AMPPNP
Homo sapiens
wild-type
0.00034
PHA-680626
Homo sapiens
mutant T210D
0.00044
PHA-680626
Homo sapiens
mutant T210V
0.00053
PHA-680626
Homo sapiens
wild-type
0.00114
(4E)-5-methyl-4-[[(2-methylbenzoyl)oxy]imino]-2-(propan-2-yl)cyclohexa-2,5-dien-1-one
Homo sapiens
pH and temperature not specified in the publication
0.00136
(4E)-5-methyl-4-[[(2-methylbenzoyl)oxy]imino]-2-(propan-2-yl)cyclohexa-2,5-dien-1-one
Homo sapiens
pH and temperature not specified in the publication
0.000009
1-methyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
0.000014
1-methyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
0.000002
1-methyl-8-[(2-methylphenyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
0.000006
1-methyl-8-[(2-methylphenyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
0.000051
1-methyl-8-[(2-phenoxyphenyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
0.002666
1-methyl-8-[(2-phenoxyphenyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
0.000011
1-methyl-8-[[2-(methylamino)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
0.000012
1-methyl-8-[[2-(methylamino)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
0.000014
1-methyl-8-[[2-(methylsulfanyl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
0.000016
1-methyl-8-[[2-(methylsulfanyl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
0.000146
1-methyl-8-[[2-(propan-2-yl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
0.000509
1-methyl-8-[[2-(propan-2-yl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
0.000095
1-methyl-8-[[2-(trifluoromethyl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
0.000109
1-methyl-8-[[2-(trifluoromethyl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
0.000004
3-(1,3-benzodioxol-5-yl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
Homo sapiens
-
0.000024
3-(1,3-benzodioxol-5-yl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
Homo sapiens
-
0.000214
3-(1,3-benzodioxol-5-yl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
Homo sapiens
-
0.000549
3-(3-methylphenyl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
Homo sapiens
-
0.001449
3-(3-methylphenyl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
Homo sapiens
-
0.01
3-(3-methylphenyl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
Homo sapiens
>0.01
0.000006
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
Homo sapiens
-
0.000025
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
Homo sapiens
HCT-116 cell
0.000035
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-methoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
Homo sapiens
-
0.000321
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-methoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
Homo sapiens
HCT-116 cell
0.000061
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(2R)-2,3-dihydroxypropyl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
Homo sapiens
-
0.000073
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(2R)-2,3-dihydroxypropyl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
Homo sapiens
HCT-116 cell
0.000045
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(2R)-2-hydroxy-3-pyrrolidin-1-ylpropyl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
Homo sapiens
HCT-116 cell
0.00061
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(2R)-2-hydroxy-3-pyrrolidin-1-ylpropyl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
Homo sapiens
-
0.000013
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(4R)-1-methylazepan-4-yl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
Homo sapiens
HCT-116 cell
0.00025
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(4R)-1-methylazepan-4-yl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
Homo sapiens
-
0.000017
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(4S)-1-methylazepan-4-yl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
Homo sapiens
HCT-116 cell
0.00024
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(4S)-1-methylazepan-4-yl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
Homo sapiens
-
0.000034
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)methoxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
Homo sapiens
HCT-116 cell
0.0011
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)methoxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
Homo sapiens
-
0.000003
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
Homo sapiens
HT-29 cell
0.000005
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
Homo sapiens
Colo-205 cell
0.000009
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
Homo sapiens
MX-1 cell
0.000011
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
Homo sapiens
A-549 cell
0.000011
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
Homo sapiens
HCT-116 cell
0.000011
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
Homo sapiens
SKOV-3 cell
0.00063
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
Homo sapiens
-
0.000032
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[3-(dimethylamino)propoxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
Homo sapiens
HCT-116 cell
0.00046
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[3-(dimethylamino)propoxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
Homo sapiens
-
0.000044
3-[(1S)-1-(2-chlorophenyl)ethoxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
Homo sapiens
-
0.000994
3-[(1S)-1-(2-chlorophenyl)ethoxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
Homo sapiens
HCT-116 cell
0.000009
3-[(2-chlorobenzyl)oxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
Homo sapiens
-
0.00114
3-[(2-chlorobenzyl)oxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
Homo sapiens
HCT-116 cell
0.000051
3-[3-chloro-5-(5-[[(1S)-1-phenylethyl]amino]isoxazolo[5,4-c]pyridin-3-yl)phenyl]propanamide
Homo sapiens
-
0.000172
3-[3-chloro-5-(5-[[(1S)-1-phenylethyl]amino]isoxazolo[5,4-c]pyridin-3-yl)phenyl]propanamide
Homo sapiens
-
0.001382
3-[3-chloro-5-(5-[[(1S)-1-phenylethyl]amino]isoxazolo[5,4-c]pyridin-3-yl)phenyl]propanamide
Homo sapiens
-
0.000041
5-(6-methoxy-1H-benzimidazol-1-yl)-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
Homo sapiens
-
0.000476
5-(6-methoxy-1H-benzimidazol-1-yl)-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
Homo sapiens
HCT-116 cell
0.000015
5-[6-(piperidin-4-yloxy)-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
Homo sapiens
HCT-116 cell
0.00035
5-[6-(piperidin-4-yloxy)-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
Homo sapiens
-
0.00003
5-[6-[(1-methylpiperidin-4-yl)methoxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
Homo sapiens
HCT-116 cell
0.00055
5-[6-[(1-methylpiperidin-4-yl)methoxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
Homo sapiens
-
0.000003
5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
Homo sapiens
HT-29 cell
0.000005
5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
Homo sapiens
Colo-205 cell
0.00001
5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
Homo sapiens
MX-1 cell
0.000012
5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
Homo sapiens
HCT-116 cell
0.000014
5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
Homo sapiens
A-549 cell
0.000032
5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
Homo sapiens
SKOV-3 cell
0.00027
5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
Homo sapiens
-
0.000103
8-[(2-acetylphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
0.000261
8-[(2-acetylphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
0.000012
8-[(2-aminophenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
0.000013
8-[(2-aminophenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
0.000027
8-[(2-fluorophenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
0.000037
8-[(2-fluorophenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
0.000013
8-[(2-methoxyphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
0.000024
8-[(2-methoxyphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
0.000049
8-[[2-(acetylamino)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
0.002104
8-[[2-(acetylamino)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
0.002292
8-[[2-acetyl-4-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
0.01
8-[[2-acetyl-4-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
larger than 0.010
0.000066
8-[[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
0.000082
8-[[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
0.000238
8-[[2-methoxy-5-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
0.00045
8-[[2-methoxy-5-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
0.00026
ONO1910
Homo sapiens
Plk2
0.01
ONO1910
Homo sapiens
-
0.000024
Wortmannin
Homo sapiens
-
0.000024
Wortmannin
Homo sapiens
-
-
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Holtrich, U.; Wolf, G.; Yuan, J.; Bereiter-Hahn, J.; Karn, T.; Weiler, M.; Kauselmann, G.; Rehli, M.; Andreesen, R.; Kaufmann, M.; Kuhl, D.; Strebhardt, K.
Adhesion induced expression of the serine/threonine kinase Fnk in human macrophages
Oncogene
19
4832-4839
2000
Homo sapiens (Q9H4B4), Homo sapiens
brenda
Li, B.; Ouyang, B.; Pan, H.; Reissmann, P.T.; Slamon, D.J.; Arceci, R.; Lu, L.; Dai, W.
Prk, a cytokine-inducible human protein serine/threonine kinase whose expression appears to be down-regulated in lung carcinomas
J. Biol. Chem.
271
19402-19408
1996
Homo sapiens (Q9H4B4)
brenda
Ouyang, B.; Li, W.; Pan, H.; Meadows, J.; Hoffmann, I.; Dai, W.
The physical association and phosphorylation of Cdc25C protein phosphatase by Prk
Oncogene
18
6029-6036
1999
Homo sapiens (Q9H4B4)
brenda
Ouyang, B.; Pan, H.; Lu, L.; Li, J.; Stambrook, P.; Li, B.; Dai, W.
Human Prk is a conserved protein serine/threonine kinase involved in regulating M phase functions
J. Biol. Chem.
272
28646-28651
1997
Homo sapiens (Q9H4B4)
brenda
Holtrich, U.; Wolf, G.; Brauninger, A.; Karn, T.; Bohme, B.; Rubsamen-Waigmann, H.; Strebhardt, K.
Induction and down-regulation of PLK, a human serine/threonine kinase expressed in proliferating cells and tumors
Proc. Natl. Acad. Sci. USA
91
1736-1740
1994
Homo sapiens (P53350)
brenda
Hamanaka, R.; Maloid, S.; Smith, M.R.; O'Connell, C.D.; Longo, D.L.; Ferris, D.K.
Cloning and characterization of human and murine homologues of the Drosophila polo serine-threonine kinase
Cell Growth Differ.
5
249-257
1994
Homo sapiens (P53350), Homo sapiens, Mus musculus (Q07832), Mus musculus
brenda
Golsteyn, R.M.; Schultz, S.J.; Bartek, J.; Ziemiecki, A.; Ried, T.; Nigg, E.A.
Cell cycle analysis and chromosomal localization of human Plk1, a putative homologue of the mitotic kinases Drosophila polo and Saccharomyces cerevisiae Cdc5
J. Cell Sci.
107
1509-1517
1994
Homo sapiens (P53350)
-
brenda
Lake, R.J.; Jelinek, W.R.
Cell cycle- and terminal differentiation-associated regulation of the mouse mRNA encoding a conserved mitotic protein kinase
Mol. Cell. Biol.
13
7793-7801
1993
Homo sapiens (P53350), Mus musculus (Q07832)
brenda
Warnke, S.; Kemmler, S.; Hames, R.S.; Tsai, H.L.; Hoffmann-Rohrer, U.; Fry, A.M.; Hoffmann, I.
Polo-like kinase-2 is required for centriole duplication in mammalian cells
Curr. Biol.
14
1200-1207
2004
Homo sapiens
brenda
Sumara, I.; Gimenez-Abian, J.F.; Gerlich, D.; Hirota, T.; Kraft, C.; de la Torre, C.; Ellenberg, J.; Peters, J.M.
Roles of polo-like kinase 1 in the assembly of functional mitotic spindles
Curr. Biol.
14
1712-1722
2004
Homo sapiens
brenda
Ahonen, L.J.; Kallio, M.J.; Daum, J.R.; Bolton, M.; Manke, I.A.; Yaffe, M.B.; Stukenberg, P.T.; Gorbsky, G.J.
Polo-like kinase 1 creates the tension-sensing 3F3/2 phosphoepitope and modulates the association of spindle-checkpoint proteins at kinetochores
Curr. Biol.
15
1078-1089
2005
Homo sapiens, Xenopus laevis
brenda
Cheng, K.Y.; Lowe, E.D.; Sinclair, J.; Nigg, E.A.; Johnson, L.N.
The crystal structure of the human polo-like kinase-1 polo box domain and its phospho-peptide complex
EMBO J.
22
5757-5768
2003
Homo sapiens (P53350), Homo sapiens
brenda
Ruan, Q.; Wang, Q.; Xie, S.; Fang, Y.; Darzynkiewicz, Z.; Guan, K.; Jhanwar-Uniyal, M.; Dai, W.
Polo-like kinase 3 is Golgi localized and involved in regulating Golgi fragmentation during the cell cycle
Exp. Cell Res.
294
51-59
2004
Homo sapiens
brenda
Nakajima, H.; Toyoshima-Morimoto, F.; Taniguchi, E.; Nishida, E.
Identification of a consensus motif for Plk (Polo-like kinase) phosphorylation reveals Myt1 as a Plk1 substrate
J. Biol. Chem.
278
25277-25280
2003
Homo sapiens
brenda
Tsvetkov, L.; Xu, X.; Li, J.; Stern, D.F.
Polo-like kinase 1 and Chk2 interact and co-localize to centrosomes and the midbody
J. Biol. Chem.
278
8468-8475
2003
Homo sapiens
brenda
Ando, K.; Ozaki, T.; Yamamoto, H.; Furuya, K.; Hosoda, M.; Hayashi, S.; Fukuzawa, M.; Nakagawara, A.
Polo-like kinase 1 (Plk1) inhibits p53 function by physical interaction and phosphorylation
J. Biol. Chem.
279
25549-25561
2004
Homo sapiens
brenda
Eckerdt, F.; Yuan, J.; Saxena, K.; Martin, B.; Kappel, S.; Lindenau, C.; Kramer, A.; Naumann, S.; Daum, S.; Fischer, G.; Dikic, I.; Kaufmann, M.; Strebhardt, K.
Polo-like kinase 1-mediated phosphorylation stabilizes Pin1 by inhibiting its ubiquitination in human cells
J. Biol. Chem.
280
36575-36583
2005
Homo sapiens (P53350), Homo sapiens
brenda
Zhang, W.; Fletcher, L.; Muschel, R.J.
The role of polo-like kinase 1 in the inhibition of centrosome separation after ionizing radiation
J. Biol. Chem.
280
42994-42999
2005
Homo sapiens
brenda
Xie, S.; Xie, B.; Lee, M.Y.; Dai, W.
Regulation of cell cycle checkpoints by polo-like kinases
Oncogene
24
277-286
2005
Saccharomyces cerevisiae, Drosophila melanogaster, Homo sapiens, Schizosaccharomyces pombe, Xenopus laevis
brenda
Liu, X.; Erikson, R.L.
Polo-like kinase (Plk)1 depletion induces apoptosis in cancer cells
Proc. Natl. Acad. Sci. USA
100
5789-5794
2003
Homo sapiens (P53350)
brenda
Garcia-Alvarez, B.; Ibanez, S.; Montoya, G.
Crystallization and preliminary X-ray diffraction studies on the human Plk1 Polo-box domain in complex with an unphosphorylated and a phosphorylated target peptide from Cdc25C
Acta Crystallogr. Sect. F
62
372-375
2006
Homo sapiens (P53350), Homo sapiens
brenda
Sato, F.; Abraham, J.M.; Yin, J.; Kan, T.; Ito, T.; Mori, Y.; Hamilton, J.P.; Jin, Z.; Cheng, Y.; Paun, B.; Berki, A.T.; Wang, S.; Shimada, Y.; Meltzer, S.J.
Polo-like kinase and survivin are esophageal tumor-specific promoters
Biochem. Biophys. Res. Commun.
342
465-471
2006
Homo sapiens
brenda
Kothe, M.; Kohls, D.; Low, S.; Coli, R.; Cheng, A.C.; Jacques, S.L.; Johnson, T.L.; Lewis, C.; Loh, C.; Nonomiya, J.; Sheils, A.L.; Verdries, K.A.; Wynn, T.A.; Kuhn, C.; Ding, Y.H.
Structure of the catalytic domain of human polo-like kinase 1
Biochemistry
46
5960-5971
2007
Homo sapiens, Homo sapiens (P53350)
brenda
Johnson, E.F.; Stewart, K.D.; Woods, K.W.; Giranda, V.L.; Luo, Y.
Pharmacological and functional comparison of the polo-like kinase family: insight into inhibitor and substrate specificity
Biochemistry
46
9551-9563
2007
Homo sapiens (O00444), Homo sapiens (P53350), Homo sapiens (Q9H4B4), Homo sapiens (Q9NYY3)
brenda
Zimmerman, W.C.; Erikson, R.L.
Finding Plk3
Cell Cycle
6
1314-1318
2007
Saccharomyces cerevisiae, Drosophila melanogaster, Homo sapiens (P53350), Homo sapiens (Q9H4B4), Homo sapiens (Q9NYY3)
brenda
Randall, C.L.; Burkard, M.E.; Jallepalli, P.V.
Polo kinase and cytokinesis initiation in Mammalian cells: harnessing the awesome power of chemical genetics
Cell Cycle
6
1713-1717
2007
Homo sapiens (P53350), Homo sapiens
brenda
Dai, B.N.; Yang, Y.; Chau, Z.; Jhanwar-Uniyal, M.
Polo-like kinase 1 regulates RhoA during cytokinesis exit in human cells
Cell Prolif.
40
550-557
2007
Homo sapiens, Homo sapiens (P53350)
brenda
Lenart, P.; Petronczki, M.; Steegmaier, M.; Di Fiore, B.; Lipp, J.J.; Hoffmann, M.; Rettig, W.J.; Kraut, N.; Peters, J.M.
The small-molecule inhibitor BI 2536 reveals novel insights into mitotic roles of polo-like kinase 1
Curr. Biol.
17
304-315
2007
Homo sapiens
brenda
Plyte, S.; Musacchio, A.
PLK1 inhibitors: setting the mitotic death trap
Curr. Biol.
17
R280-R283
2007
Mus musculus, Homo sapiens (P53350), Homo sapiens
brenda
Elowe, S.; Huemmer, S.; Uldschmid, A.; Li, X.; Nigg, E.A.
Tension-sensitive Plk1 phosphorylation on BubR1 regulates the stability of kinetochore microtubule interactions
Genes Dev.
21
2205-2219
2007
Homo sapiens (P53350)
brenda
Matsumura, S.; Toyoshima, F.; Nishida, E.
Polo-like kinase 1 facilitates chromosome alignment during prometaphase through BubR1
J. Biol. Chem.
282
15217-15227
2007
Mus musculus, Homo sapiens (P53350)
brenda
Yuan, K.; Hu, H.; Guo, Z.; Fu, G.; Shaw, A.P.; Hu, R.; Yao, X.
Phospho-regulation of HsCdc14A By Polo-like kinase 1 is essential for mitotic progression
J. Biol. Chem.
282
27414-27423
2007
Homo sapiens, Homo sapiens (P53350)
brenda
Brennan, I.M.; Peters, U.; Kapoor, T.M.; Straight, A.F.
Polo-like kinase controls vertebrate spindle elongation and cytokinesis
PLoS ONE
2
e409
2007
Homo sapiens, Homo sapiens (P53350)
brenda
Garcia-Alvarez, B.; de Carcer, G.; Ibanez, S.; Bragado-Nilsson, E.; Montoya, G.
Molecular and structural basis of polo-like kinase 1 substrate recognition: Implications in centrosomal localization
Proc. Natl. Acad. Sci. USA
104
3107-3112
2007
Homo sapiens, Homo sapiens (P53350)
brenda
Burkard, M.E.; Randall, C.L.; Larochelle, S.; Zhang, C.; Shokat, K.M.; Fisher, R.P.; Jallepalli, P.V.
Chemical genetics reveals the requirement for Polo-like kinase 1 activity in positioning RhoA and triggering cytokinesis in human cells
Proc. Natl. Acad. Sci. USA
104
4383-4388
2007
Homo sapiens (P53350), Homo sapiens
brenda
Elling, R.A.; Fucini, R.V.; Romanowski, M.J.
Structures of the wild-type and activated catalytic domains of Brachydanio rerio Polo-like kinase 1 (Plk1): changes in the active-site conformation and interactions with ligands
Acta Crystallogr. Sect. D
64
909-918
2008
Homo sapiens, Danio rerio (Q6DRK7), Danio rerio
brenda
Hanan, E.J.; Fucini, R.V.; Romanowski, M.J.; Elling, R.A.; Lew, W.; Purkey, H.E.; VanderPorten, E.C.; Yang, W.
Design and synthesis of 2-amino-isoxazolopyridines as Polo-like kinase inhibitors
Bioorg. Med. Chem. Lett.
18
5186-5189
2008
Homo sapiens, Homo sapiens (Q9H4B4)
brenda
Nishi, Y.; Rogers, E.; Robertson, S.M.; Lin, R.
Polo kinases regulate C. elegans embryonic polarity via binding to DYRK2-primed MEX-5 and MEX-6
Development
135
687-697
2008
Caenorhabditis elegans, Homo sapiens
brenda
Higashimoto, T.; Chan, N.; Lee, Y.K.; Zandi, E.
Regulation of IKK by phosphorylation of gamma binding domain of Ikappa Ba kinase beta by polo-like kinase 1
J. Biol. Chem.
283
35354-35367
2008
Homo sapiens (P53350)
brenda
Chi, Y.H.; Haller, K.; Ward, M.D.; Semmes, O.J.; Li, Y.; Jeang, K.T.
Requirements for protein phosphorylation and the kinase activity of polo-like kinase 1 (Plk1) for the kinetochore function of mitotic arrest deficiency protein 1 (Mad1)
J. Biol. Chem.
283
35834-35844
2008
Homo sapiens
brenda
Tamura, Y.; Simizu, S.; Muroi, M.; Takagi, S.; Kawatani, M.; Watanabe, N.; Osada, H.
Polo-like kinase 1 phosphorylates and regulates Bcl-x(L) during pironetin-induced apoptosis
Oncogene
28
107-116
2009
Homo sapiens
brenda
Liu, L.; Zhang, M.; Zou, P.
Polo-like kinase 1 as a new target for non-Hodgkins lymphoma treatment
Oncology
74
96-103
2008
Homo sapiens (P53350)
brenda
Emmitte, K.A.; Adjabeng, G.M.; Adjebang, G.M.; Andrews, C.W.; Alberti, J.G.; Bambal, R.; Chamberlain, S.D.; Davis-Ward, R.G.; Dickson, H.D.; Hassler, D.F.; Hornberger, K.R.; Jackson, J.R.; Kuntz, K.W.; Lansing, T.J.; Mook, R.A.; Nailor, K.E.; Pobanz, M.A.; Smith, S.C.; Sung, C.M.; Cheung, M.
Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding
Bioorg. Med. Chem. Lett.
19
1694-1697
2009
Homo sapiens, Homo sapiens (P53350), Homo sapiens (Q9H4B4)
brenda
Uckun, F.M.; Ozer, Z.; Qazi, S.; Tuel-Ahlgren, L.; Mao, C.
Polo-like-kinase 1 (PLK1) as a molecular target to overcome SYK-mediated resistance of B-lineage acute lymphoblastic leukaemia cells to oxidative stress
Br. J. Haematol.
148
714-725
2010
Homo sapiens (P53350), Homo sapiens
brenda
Duan, Z.; Ji, D.; Weinstein, E.J.; Liu, X.; Susa, M.; Choy, E.; Yang, C.; Mankin, H.; Hornicek, F.J.
Lentiviral shRNA screen of human kinases identifies PLK1 as a potential therapeutic target for osteosarcoma
Cancer Lett.
293
220-229
2010
Homo sapiens (P53350), Homo sapiens
brenda
Nappi, T.C.; Salerno, P.; Zitzelsberger, H.; Carlomagno, F.; Salvatore, G.; Santoro, M.
Identification of Polo-like kinase 1 as a potential therapeutic target in anaplastic thyroid carcinoma
Cancer Res.
69
1916-1923
2009
Homo sapiens (P53350)
brenda
Gilmartin, A.G.; Bleam, M.R.; Richter, M.C.; Erskine, S.G.; Kruger, R.G.; Madden, L.; Hassler, D.F.; Smith, G.K.; Gontarek, R.R.; Courtney, M.P.; Sutton, D.; Diamond, M.A.; Jackson, J.R.; Laquerre, S.G.
Distinct concentration-dependent effects of the polo-like kinase 1-specific inhibitor GSK461364A, including differential effect on apoptosis
Cancer Res.
69
6969-6977
2009
Homo sapiens
brenda
Gleixner, K.V.; Ferenc, V.; Peter, B.; Gruze, A.; Meyer, R.A.; Hadzijusufovic, E.; Cerny-Reiterer, S.; Mayerhofer, M.; Pickl, W.F.; Sillaber, C.; Valent, P.
Polo-like kinase 1 (Plk1) as a novel drug target in chronic myeloid leukemia: overriding imatinib resistance with the Plk1 inhibitor BI 2536
Cancer Res.
70
1513-1523
2010
Homo sapiens (P53350), Homo sapiens
brenda
Chun, G.; Bae, D.; Nickens, K.; OBrien, T.J.; Patierno, S.R.; Ceryak, S.
Polo-like kinase 1 enhances survival and mutagenesis after genotoxic stress in normal cells through cell cycle checkpoint bypass
Carcinogenesis
31
785-793
2010
Homo sapiens
brenda
Schmit, T.L.; Zhong, W.; Nihal, M.; Ahmad, N.
Polo-like kinase 1 (Plk1) in non-melanoma skin cancers
Cell Cycle
8
2697-2702
2009
Homo sapiens (P53350), Homo sapiens
brenda
Keppner, S.; Proschak, E.; Kaufmann, M.; Strebhardt, K.; Schneider, G.; Spaenkuch, B.
Biological impact of freezing Plk1 in its inactive conformation in cancer cells
Cell Cycle
9
761-773
2010
Homo sapiens
brenda
Keppner, S.; Proschak, E.; Schneider, G.; Spaenkuch, B.
Identification and validation of a potent type II inhibitor of inactive polo-like kinase 1
ChemMedChem
4
1806-1809
2009
Homo sapiens (P53350)
brenda
Degenhardt, Y.; Lampkin, T.
Targeting Polo-like kinase in cancer therapy
Clin. Cancer Res.
16
384-389
2010
Homo sapiens
brenda
Chopra, P.; Sethi, G.; Dastidar, S.G.; Ray, A.
Polo-like kinase inhibitors: an emerging opportunity for cancer therapeutics
Expert Opin. Investig. Drugs
19
27-43
2010
Homo sapiens
brenda
Shi, W.; Alajez, N.M.; Bastianutto, C.; Hui, A.B.; Mocanu, J.D.; Ito, E.; Busson, P.; Lo, K.W.; Ng, R.; Waldron, J.; OSullivan, B.; Liu, F.F.
Significance of Plk1 regulation by miR-100 in human nasopharyngeal cancer
Int. J. Cancer
126
2036-2048
2010
Homo sapiens (P53350), Homo sapiens
brenda
Vitour, D.; Dabo, S.; Ahmadi Pour, M.; Vilasco, M.; Vidalain, P.O.; Jacob, Y.; Mezel-Lemoine, M.; Paz, S.; Arguello, M.; Lin, R.; Tangy, F.; Hiscott, J.; Meurs, E.F.
Polo-like kinase 1 (PLK1) regulates interferon (IFN) induction by MAVS
J. Biol. Chem.
284
21797-21809
2009
Homo sapiens (P53350)
brenda
Beria, I.; Ballinari, D.; Bertrand, J.A.; Borghi, D.; Bossi, R.T.; Brasca, M.G.; Cappella, P.; Caruso, M.; Ceccarelli, W.; Ciavolella, A.; Cristiani, C.; Croci, V.; De Ponti, A.; Fachin, G.; Ferguson, R.D.; Lansen, J.; Moll, J.K.; Pesenti, E.; Posteri, H.; Perego, R.; Rocchetti, M.; Storici, P.; Volpi, D.
Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors
J. Med. Chem.
53
3532-3551
2010
Homo sapiens (P53350), Homo sapiens (Q9H4B4), Homo sapiens (Q9NYY3)
brenda
Wang, W.S.; Lee, M.S.; Tseng, C.E.; Liao, I.H.; Huang, S.P.; Lin, R.I.; Li, C.
Interaction between human papillomavirus type 5 E2 and polo-like kinase 1
J. Med. Virol.
81
536-544
2009
Homo sapiens (P53350), Homo sapiens
brenda
Sillibourne, J.E.; Tack, F.; Vloemans, N.; Boeckx, A.; Thambirajah, S.; Bonnet, P.; Ramaekers, F.C.; Bornens, M.; Grand-Perret, T.
Autophosphorylation of polo-like kinase 4 and its role in centriole duplication
Mol. Biol. Cell
21
547-561
2010
Homo sapiens (Q00444)
brenda
Kishi, K.; van Vugt, M.A.; Okamoto, K.; Hayashi, Y.; Yaffe, M.B.
Functional dynamics of Polo-like kinase 1 at the centrosome
Mol. Cell. Biol.
29
3134-3150
2009
Homo sapiens (P53350)
brenda
Benoit, D.S.; Henry, S.M.; Shubin, A.D.; Hoffman, A.S.; Stayton, P.S.
pH-responsive polymeric sirna carriers sensitize multidrug resistant ovarian cancer cells to doxorubicin via knockdown of polo-like kinase 1
Mol. Pharm.
7
442-455
2010
Homo sapiens (P53350)
brenda
Archambault, V.; Glover, D.
Polo-like kinases: Conservation and divergence in their functions and regulation
Nat. Rev. Mol. Cell Biol.
10
265-275
2009
Saccharomyces cerevisiae, Drosophila melanogaster, Homo sapiens, Saccharomyces pombe, Xenopus laevis
brenda
Andrysik, Z.; Bernstein, W.Z.; Deng, L.; Myer, D.L.; Li, Y.Q.; Tischfield, J.A.; Stambrook, P.J.; Bahassi, E.M.
The novel mouse Polo-like kinase 5 responds to DNA damage and localizes in the nucleolus
Nucleic Acids Res.
38
2931-2943
2010
Homo sapiens, Mus musculus (Q4FZD7), Mus musculus
brenda
Sun, D.; Luthra, P.; Li, Z.; He, B.
PLK1 down-regulates parainfluenza virus 5 gene expression
PLoS Pathog.
5
e1000525
2009
Homo sapiens (P53350), Homo sapiens
brenda
Park, J.E.; Li, L.; Park, J.; Knecht, R.; Strebhardt, K.; Yuspa, S.H.; Lee, K.S.
Direct quantification of polo-like kinase 1 activity in cells and tissues using a highly sensitive and specific ELISA assay
Proc. Natl. Acad. Sci. USA
106
1725-1730
2009
Mus musculus, Homo sapiens (P53350), Homo sapiens
brenda
Sledz, P.; Stubbs, C.J.; Lang, S.; Yang, Y.; McKenzie, G.; Venkitaraman, A.; Hyvnen, M.; Abell, C.
From crystal packing to molecular recognition: Prediction and discovery of a binding site on the surface of polo-like kinase 1
Angew. Chem.
50
4003-4006
2011
Homo sapiens (P53350)
brenda
Caruso, M.; Valsasina, B.; Ballinari, D.; Bertrand, J.; Brasca, M.G.; Caldarelli, M.; Cappella, P.; Fiorentini, F.; Gianellini, L.M.; Scolaro, A.; Beria, I.
5-(2-amino-pyrimidin-4-yl)-1H-pyrrole and 2-(2-amino-pyrimidin-4-yl)-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one derivatives as new classes of selective and orally available Polo-like kinase 1 inhibitors
Bioorg. Med. Chem. Lett.
22
96-101
2012
Homo sapiens (P53350)
brenda
Bowers, S.; Truong, A.P.; Ye, M.; Aubele, D.L.; Sealy, J.M.; Neitz, R.J.; Hom, R.K.; Chan, W.; Dappen, M.S.; Galemmo, R.A.; Konradi, A.W.; Sham, H.L.; Zhu, Y.L.; Beroza, P.; Tonn, G.; Zhang, H.; Hoffman, J.; Motter, R.; Fauss, D.; Tanaka, P.; Bova, M.P.; Ren, Z.; Tam, D.; Ruslim, L.; Baker, J.; Pandya, D.; Diep, L.; F, F.i.
Design and synthesis of highly selective, orally active Polo-like kinase-2 (Plk-2) inhibitors
Bioorg. Med. Chem. Lett.
23
2743-2749
2013
Homo sapiens (P53350), Homo sapiens (Q9NYY3)
brenda
Murugan, R.N.; Park, J.E.; Lim, D.; Ahn, M.; Cheong, C.; Kwon, T.; Nam, K.Y.; Choi, S.H.; Kim, B.Y.; Yoon, D.Y.; Yaffe, M.B.; Yu, D.Y.; Lee, K.S.; Bang, J.K.
Development of cyclic peptomer inhibitors targeting the polo-box domain of polo-like kinase 1
Bioorg. Med. Chem.
21
2623-2634
2013
Homo sapiens (P53350)
brenda
Mita, Y.; Noguchi-Yachide, T.; Ishikawa, M.; Hashimoto, Y.
Small-molecular, non-peptide, non-ATP-competitive polo-like kinase 1 (Plk1) inhibitors with a terphenyl skeleton
Bioorg. Med. Chem.
21
608-617
2013
Homo sapiens
brenda
Vazquez-Martin, A.; Oliveras-Ferraros, C.; Cufi, S.; Menendez, J.A.
Polo-like kinase 1 regulates activation of AMP-activated protein kinase (AMPK) at the mitotic apparatus
Cell Cycle
10
1295-1302
2011
Homo sapiens
brenda
Lera, R.F.; Burkard, M.E.
High mitotic activity of Polo-like kinase 1 is required for chromosome segregation and genomic integrity in human epithelial cells
J. Biol. Chem.
287
42812-42825
2012
Homo sapiens (P53350), Homo sapiens
brenda
Liu, D.; Davydenko, O.; Lampson, M.A.
Polo-like kinase-1 regulates kinetochore-microtubule dynamics and spindle checkpoint silencing
J. Cell Biol.
198
491-499
2012
Homo sapiens (P53350)
brenda
Liu, L.; Zhang, M.; Zou, P.
Polo-like kinase 1 is essential to DNA damage recovery
Leuk. Lymphoma
51
1079-1089
2010
Homo sapiens
brenda
Holland, A.J.; Fachinetti, D.; Da Cruz, S.; Zhu, Q.; Vitre, B.; Lince-Faria, M.; Chen, D.; Parish, N.; Verma, I.M.; Bettencourt-Dias, M.; Cleveland, D.W.
Polo-like kinase 4 controls centriole duplication but does not directly regulate cytokinesis
Mol. Biol. Cell
23
1838-1845
2012
Homo sapiens (O00444), Homo sapiens, Mus musculus (Q64702), Mus musculus
brenda
Johmura, Y.; Soung, N.K.; Park, J.E.; Yu, L.R.; Zhou, M.; Bang, J.K.; Kim, B.Y.; Veenstra, T.D.; Erikson, R.L.; Lee, K.S.
Regulation of microtubule-based microtubule nucleation by mammalian polo-like kinase 1
Proc. Natl. Acad. Sci. USA
108
11446-11451
2011
Homo sapiens
brenda
Chen, D.X.; Huang, J.; Liu, M.; Xu, Y.G.; Jiang, C.
Design, synthesis, and evaluation of non-ATP-competitive small-molecule polo-like kinase 1 (Plk1) inhibitors
Arch. Pharm.
348
2-9
2015
Homo sapiens (P53350)
brenda
Shan, H.M.; Wang, T.; Quan, J.M.
Crystal structure of the polo-box domain of polo-like kinase 2
Biochem. Biophys. Res. Commun.
456
780-784
2015
Homo sapiens (Q9NYY3)
brenda
O'Connor, A.; Maffini, S.; Rainey, M.D.; Kaczmarczyk, A.; Gaboriau, D.; Musacchio, A.; Santocanale, C.
Requirement for PLK1 kinase activity in the maintenance of a robust spindle assembly checkpoint
Biol. Open
5
11-19
2015
Homo sapiens (P53350)
brenda
Liu, M.; Huang, J.; Chen, D.X.; Jiang, C.
Identification of indole-3-carboxylic acids as non-ATP-competitive Polo-like kinase 1 (Plk1) inhibitors
Bioorg. Med. Chem. Lett.
25
431-434
2015
Homo sapiens (P53350)
brenda
Benada, J.; Burdova, K.; Lidak, T.; von Morgen, P.; Macurek, L.
Polo-like kinase 1 inhibits DNA damage response during mitosis
Cell Cycle
14
219-231
2015
Homo sapiens (Q9NYY3)
brenda
Berg, A.; Berg, T.
Inhibitors of the polo-Box domain of polo-like kinase 1
ChemBioChem
17
650-656
2016
Homo sapiens (Q9NYY3)
brenda
Huang, Y.; Sun, L.; Liu, N.; Wei, Q.; Jiang, L.; Tong, X.; Ye, X.
Polo-like kinase 1 (Plk1) up-regulates telomerase activity by affecting human telomerase reverse transcriptase (hTERT) stability
J. Biol. Chem.
290
18865-18873
2015
Homo sapiens (Q9NYY3), Homo sapiens
brenda
Park, C.H.; Park, J.E.; Kim, T.S.; Kang, Y.H.; Soung, N.K.; Zhou, M.; Kim, N.H.; Bang, J.K.; Lee, K.S.
Mammalian polo-like kinase 1 (Plk1) promotes proper chromosome segregation by phosphorylating and delocalizing the PBIP1-CENP-Q complex from kinetochores
J. Biol. Chem.
290
8569-8581
2015
Homo sapiens (Q9NYY3)
brenda
Xiao, D.; Yue, M.; Su, H.; Ren, P.; Jiang, J.; Li, F.; Hu, Y.; Du, H.; Liu, H.; Qing, G.
Polo-like kinase-1 regulates Myc stabilization and activates a feedforward circuit promoting tumor cell survival
Mol. Cell
64
493-506
2016
Homo sapiens (P53350), Homo sapiens
brenda
Lera, R.F.; Potts, G.K.; Suzuki, A.; Johnson, J.M.; Salmon, E.D.; Coon, J.J.; Burkard, M.E.
Decoding Polo-like kinase 1 signaling along the kinetochore-centromere axis
Nat. Chem. Biol.
12
411-418
2016
Homo sapiens (Q9NYY3), Homo sapiens
brenda
Ritter, A.; Friemel, A.; Kreis, N.N.; Louwen, F.; Yuan, J.
Impact of Polo-like kinase 1 inhibitors on human adipose tissue-derived mesenchymal stem cells
Oncotarget
6
6641-6655
2016
Homo sapiens (Q9NYY3), Homo sapiens
brenda
Zhao, X.Z.; Hymel, D.; Burke, T.R.
Application of oxime-diversification to optimize ligand interactions within a cryptic pocket of the polo-like kinase 1 polo-box domain
Bioorg. Med. Chem. Lett.
26
5009-5012
2016
Homo sapiens (P53350)
brenda
Yu, X.; Li, Y.; Lou, Y.; Wang, T.
Molecular design and engineering of phosphopeptide ligands to target lung cancer polo-like kinase
Biotechnol. Bioprocess Eng.
22
218-224
2017
Homo sapiens (P53350)
-
brenda
Wu, J.; Ivanov, A.I.; Fisher, P.B.; Fu, Z.
Polo-like kinase 1 induces epithelial-to-mesenchymal transition and promotes epithelial cell motility by activating CRAF/ERK signaling
eLife
5
e10734
2016
Homo sapiens (P53350)
brenda
Rodriguez-Nogales, C.; Garbayo, E.; Martinez-Valbuena, I.; Sebastian, V.; Luquin, M.R.; Blanco-Prieto, M.J.
Development and characterization of polo-like kinase 2 loaded nanoparticles - A novel strategy for (serine-129) phosphorylation of alpha-synuclein
Int. J. Pharm.
514
142-149
2016
Homo sapiens (Q9NYY3)
brenda
Lee, Y.; Lee, J.S.; Lee, K.J.; Turner, R.S.; Hoe, H.S.; Pak, D.T.S.
Polo-like kinase 2 phosphorylation of amyloid precursor protein regulates activity-dependent amyloidogenic processing
Neuropharmacology
117
387-400
2017
Homo sapiens (Q9NYY3)
brenda
Pintard, L.; Archambault, V.
A unified view of spatio-temporal control of mitotic entry Polo kinase as the key
Open Biology
8
180114
2018
Homo sapiens (P53350)
brenda