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(13alpha)-3-hydroxyestra-1(10),2,4-trien-17-one
inhibits the enzyme activity effectively, enzyme affinity is similar to that of the natural estrone substrate
(15alpha)-3-hydroxy-N-(5-methyl-1,3-thiazol-2-yl)-17-oxoestra-1(10),2,4-triene-15-carboxamide
-
(15beta)-15-(4-morpholin-4-yl-4-oxobutyl)-17-oxoestra-1(10),2,4-trien-3-yl sulfamate
0.0001 mM, 10% inhibition
(15beta)-3-hydroxy-15-(3-hydroxypropyl)estra-1(10),2,4-trien-17-one
-
(15beta)-3-hydroxy-15-(5-hydroxypentyl)estra-1(10),2,4-trien-17-one
-
(16alpa,17beta)-16-(3-bromopropyl)estra-1(10),2,4-triene-3,17-diol
EM-251
(16alpha)-2-chloro-16-fluoro-3-hydroxyestra-1(10),2,4-trien-17-one
-
(16alpha)-3-hydroxy-17-oxoestra-1(10),2,4-triene-16-carbonitrile
-
(16beta)-16-(ethoxymethyl)-3-hydroxyestra-1(10),2,4-trien-17-one
-
(16beta)-2-chloro-16-fluoro-3-hydroxyestra-1(10),2,4-trien-17-one
-
(16beta)-3-hydroxy-16-methyl-17-oxoestra-1(10),2,4-triene-16-carbonitrile
-
(16beta)-3-hydroxy-17-oxoestra-1(10),2,4-triene-16-carbonitrile
-
(16Z)-3-hydroxy-16-(2,2,2-trifluoro-1-hydroxyethylidene)estra-1(10),2,4-trien-17-one
-
(16Z)-3-hydroxy-16-(hydroxymethylidene)estra-1(10),2,4-trien-17-one
-
(17beta)-3,17-dihydroxy-N-(pyridin-3-ylmethyl)estra-1(10),2,4-triene-16-carboxamide
-
(17E)-3-hydroxyestra-1(10),2,4-trien-17-one oxime
-
(17Z)-3-hydroxyestra-1(10),2,4-triene-16,17-dione dioxime
-
(1Z)-N'-[[(3,5-dimethylisoxazol-4-yl)carbonyl]oxy]-2-[4-(1,2,3-thiadiazol-4-yl)phenyl]ethanimidamide
-
(2E)-3-[2-hydroxy-6-(3-hydroxyphenyl)-1-naphthyl]-N-methylacrylamide
58% inhibition at 0.001 mM
(2E)-3-[2-hydroxy-6-(3-hydroxyphenyl)-1-naphthyl]-N-phenylacrylamide
60% inhibition at 0.001 mM
(2R,4aS,4bR,10bS,12aS)-9-chloro-2-fluoro-8-hydroxy-12a-methyl-3,4,4a,4b,5,6,10b,11,12,12a-decahydrochrysen-1(2H)-one
-
(2S,4aS,4bR,10bS,12aS)-9-chloro-2-fluoro-8-hydroxy-12a-methyl-3,4,4a,4b,5,6,10b,11,12,12a-decahydrochrysen-1(2H)-one
-
(2Z,2'E)-N,N'-1H-1,5-benzodiazepine-2,4-diylbis(3-phenylprop-2-enamide)
30% inhibition at 0.006 mM
(3-amino-5-[13-[(16beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-16-yl]tridecyl]phenyl)acetic acid
-
(3-[(4-aminophenyl)carbonyl]-5-[13-[(16beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-16-yl]tridecyl]phenyl)acetic acid
-
(3-[13-[(16beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-16-yl]tridecyl]phenyl)acetic acid
-
(3alpha,7alpha,17beta)-17-ethynyl-7-methylestr-5(10)-ene-3,17-diol
-
(3beta,7alpha,17beta)-17-ethynyl-7-methylestr-5(10)-ene-3,17-diol
-
(4aS,4bR,10bS,12aS)-8-hydroxy-12a-methyl-9-(2-phenylethyl)-3,4,4a,4b,5,6,10b,11,12,12a-decahydrochrysen-1(2H)-one
-
(4aS,4bR,10bS,12aS)-8-hydroxy-12a-methyl-9-prop-2-en-1-yl-3,4,4a,4b,5,6,10b,11,12,12a-decahydrochrysen-1(2H)-one
-
(4aS,4bR,10bS,12aS)-8-hydroxy-9-iodo-12a-methyl-3,4,4a,4b,5,6,10b,11,12,12a-decahydrochrysen-1(2H)-one
-
(4aS,4bR,10bS,12aS)-8-hydroxy-9-methoxy-12a-methyl-3,4,4a,4b,5,6,10b,11,12,12a-decahydrochrysen-1(2H)-one
-
(4aS,4bR,10bS,12aS)-9-bromo-8-hydroxy-12a-methyl-3,4,4a,4b,5,6,10b,11,12,12a-decahydrochrysen-1(2H)-one
-
(4aS,4bR,10bS,12aS)-9-chloro-8-hydroxy-12a-methyl-3,4,4a,4b,5,6,10b,11,12,12a-decahydrochrysen-1(2H)-one
-
(4S,5S)-5-[biphenyl-3-yl(hydroxy)methyl]-4-(2-fluorophenyl)-1-methylpyrrolidin-2-one
-
(4S,5S)-5-[biphenyl-4-yl(hydroxy)methyl]-4-(2-fluorophenyl)-1-methylpyrrolidin-2-one
-
(4S,5S)-5-[hydroxy[5-(pyridin-3-yl)thiophen-2-yl]methyl]-1-methyl-4-phenylpyrrolidin-2-one
-
(6-hydroxy-1,3-benzothiazol-2-yl)(3-hydroxyphenyl)methanone
modeling of binding to crystal structure shows five hydrogen bond interactions and a cation-pi-interaction
(6aS)-2-(benzyloxy)-6a-methyl-9-[(2E)-4-morpholin-4-yl-4-oxobut-2-en-1-yl]-5,6,6a,10,10a,10b,11,12-octahydro-4bH-naphtho[2',1':4,5]indeno[2,1-d]isoxazole
0.0001 mM, 21% inhibition
(6aS)-2-hydroxy-6a,8-dimethyl-5,6,6a,7,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazol-9(4bH)-one
0.01 mM, 32% inhibition
(6aS)-2-hydroxy-6a-methyl-5,6,6a,7,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazol-9(4bH)-one
0.01 mM, 86% inhibition
(6aS)-2-hydroxy-6a-methyl-N-(2-pyridin-3-ylethyl)-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-9-carboxamide
(6aS)-2-hydroxy-6a-methyl-N-(pyridin-2-ylmethyl)-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-9-carboxamide
(6aS)-2-hydroxy-6a-methyl-N-(pyridin-3-ylmethyl)-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-9-carboxamide
(6aS)-2-hydroxy-6a-methyl-N-[(1-methyl-1H-pyrrol-2-yl)methyl]-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-9-carboxamide
0.01 mM, 90% inhibition, IC50: 0.0023 mM
(6aS)-2-hydroxy-6a-methyl-N-[(5-methylpyrazin-2-yl)methyl]-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-9-carboxamide
0.01 mM, 80% inhibition
(6aS)-3-ethyl-2-hydroxy-6a-methyl-N-(2-pyridin-3-ylethyl)-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-9-carboxamide
-
(6aS)-6a-methyl-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazol-2-ol
-
(6aS)-6a-methyl-9-(4-morpholin-4-yl-4-oxobutyl)-4b,5,6,6a,7,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazol-2-ol
0.0001 mM, 53% inhibition
(6aS)-6a-methyl-9-(trifluoromethyl)-4b,6,6a,7,9a,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-2,6b(5H)-diol
-
(6aS)-8-(2-methoxyethyl)-6a-methyl-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazol-2-ol
-
(6aS)-9-(hydroxymethyl)-6a-methyl-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazol-2-ol
-
(6beta,17beta)-6-(hexylsulfanyl)estra-1(10),2,4-triene-3,17-diol
-
(6Z,17E)-3-hydroxyestra-1(10),2,4-triene-6,17-dione dioxime
-
(7alpha,17beta)-17-ethynyl-17-hydroxy-7-methylestr-4-en-3-one
-
1-(3'-ethyl-4'-hydroxy-biphenyl-4-yl)-ethanone
37°C, 0.01 mM, 73% inhibition, substrate: estrone, 7beta-HSD type 1
1-(3-ethyl-4'-hydroxy-biphenyl-4-yl)-ethanone
37°C, 0.01 mM, 71% inhibition, substrate: estrone, 7beta-HSD type 1
1-(4'-hydroxy-2'_methyl-biphenyl-4-yl)-ethanone
37°C, 0.01 mM, 89% inhibition, substrate: estrone, 7beta-HSD type 1
1-(4'-hydroxy-biphenyl-4-yl)-ethanone
37°C, 01 mM, 97% inhibition, substrate: estrone, 7beta-HSD type 1
1-(4-fluorophenyl)-3-[4-(1,2,3-thiadiazol-4-yl)benzyl]urea
-
1-(6-hydroxy-9H-fluoren-2-yl)-ethanone
37°C, 0.01 mM, 86% inhibition, substrate: estrone, 7beta-HSD type 1
1-bromo-6-(3-hydroxyphenyl)-2-naphthol
88% inhibition at 0.001 mM
1-[(3-hydroxyphenyl)sulfanyl]-5-oxo-4,5,7,8,9,10,11,13-octahydro-3H-indeno[2',1':4,5]pyrimido[1,2-a]azepine-2-carbaldehyde
-
1-[5-(3'-hydroxybiphenyl-3-yl)-2-thienyl]ethanone
1-[5-(3'-Hydroxybiphenyl-4-yl)-2-thienyl]ethanone
13-oxo-4-(phenylsulfanyl)-1,2,7,8,9,10,11,13-octahydro[1]benzothieno[2',3':4,5]pyrimido[1,2-a]azepine-3-carbaldehyde
0.001 mM, 80% inhibition
13-oxo-4-(propylsulfanyl)-1,2,7,8,9,10,11,13-octahydro[1]benzothieno[2',3':4,5]pyrimido[1,2-a]azepine-3-carbaldehyde
0.001 mM, 74% inhibition
16-cyano-17-oxoestra-1(10),2,4-trien-3-yl sulfamate
-
16-cyano-2-methoxy-17-oxoestra-1(10),2,4-trien-3-yl sulfamate
-
2'-methoxy-N-(3-methoxyphenyl)-N-methyl-[1,1'-biphenyl]-4-sulfonamide
-
2'-methoxy-N-methyl-N-phenyl-[1,1'-biphenyl]-4-sulfonamide
-
2,2'-diimino-7,7'-dimethyl-5,5'-bis(1-methylethyl)-2H,2'H-8,8'-binaphtho[1,8-bc]furan-3,3',4,4'-tetrol
-
2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethyl (2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoate
44% inhibition at 0.006 mM
2-(3-hydroxyphenyl)quinolin-6-ol
0.001 mM, 63% inhibition, substrate: estrone
2-chloro-3-hydroxyestra-1(10),2,4-trien-17-one
-
2-chloro-4-[5-(2,6-difluoro-3-hydroxybenzoyl)thiophen-2-yl]phenyl sulfamate
dual inhibitor, acts both on steroid sulfatase and hydroxy steroid dehydrogenase 17beta-HSD1, reverses estrogen-induced T-47D cell proliferation
2-ethyl-17-oxo-16-[2-oxo-2-[(pyridin-3-ylmethyl)amino]ethyl]estra-1(10),2,4-trien-3-yl sulfamate
-
2-hydroxy-6-(3-hydroxyphenyl)-N-(5-methyl-1,3,4-thiadiazol-2-yl)-1-naphthamide
73% inhibition at 0.001 mM
2-hydroxy-6-(3-hydroxyphenyl)-N-methyl-1-naphthamide
76% inhibition at 0.001 mM
2-hydroxy-6-(3-hydroxyphenyl)-N-phenyl-1-naphthamide
80% inhibition at 0.001 mM
2-hydroxy-N,6-bis(3-hydroxyphenyl)-1-naphthamide
70% inhibition at 0.001 mM
2-nitrophenyl (2E)-3-phenylprop-2-enoate
45% inhibition at 0.006 mM
2-[2-ethyl-3-hydroxy-17-oxoestra-1(10),2,4-trien-16-yl]-N-(pyridin-2-ylmethyl)acetamide
-
2-[2-ethyl-3-hydroxy-17-oxoestra-1(10),2,4-trien-16-yl]-N-(pyridin-3-ylmethyl)acetamide
-
2-[3-hydroxy-17-oxoestra-1(10),2,4-trien-16-yl]-N-(2-pyridin-2-ylethyl)acetamide
0.01 mM, 58% inhibition
2-[3-hydroxy-17-oxoestra-1(10),2,4-trien-16-yl]-N-(pyridin-2-ylmethyl)acetamide
0.01 mM, 82% inhibition
2-[3-hydroxy-17-oxoestra-1(10),2,4-trien-16-yl]-N-(pyridin-3-ylmethyl)acetamide
-
2-[5-(3-ethyl-4-hydroxyphenyl)-1-oxo-indan-2-yl]-N-pyridin-3-ylmethyl-acetamide
37°C, 0.001 mM, 39% inhibition, substrate: estrone, 7beta-HSD type 1
3'-(1-benzothien-2-yl)biphenyl-3-ol
3'-(2-thienyl)biphenyl-3-ol
3'-(5-chloro-2-thienyl)biphenyl-3-ol
3'-(5-methyl-2-thienyl)biphenyl-3-ol
3'-hydroxy-N-(3-hydroxybenzyl)-N-methyl-[1,10-biphenyl]-4-sulfonamide
-
3'-hydroxy-N-(3-hydroxybenzyl)-N-methylbiphenyl-4-carboxamide
-
3'-hydroxy-N-(3-hydroxyphenyl)-N-methyl-[1,10-biphenyl]-3-sulfonamide
42% inhibition at 0.001 mM
3'-hydroxy-N-(3-hydroxyphenyl)-N-methyl-[1,10-biphenyl]-4-sulfonamide
14% inhibition at 0.001 mM
3'-hydroxy-N-(3-hydroxyphenyl)-N-methylbiphenyl-4-carboxamide
-
3'-hydroxy-N-(3-methoxyphenyl)-N-methyl-[1,10-biphenyl]-4-sulfonamide
15% inhibition at 0.001 mM
3'-methoxy-N-(2-methoxyphenyl)-N-methyl-[1,1'-biphenyl]-4-sulfonamide
17% inhibition at 0.001 mM
3'-methoxy-N-(3-methoxybenzyl)-N-methyl-[1,10-biphenyl]-4-sulfonamide
45% inhibition at 0.001 mM
3'-methoxy-N-(3-methoxybenzyl)-N-methylbiphenyl-4-carboxamide
-
3'-methoxy-N-(3-methoxyphenyl)-N-methyl-[1,1'-biphenyl]-4-sulfonamide
10% inhibition at 0.001 mM
3'-methoxy-N-(3-methoxyphenyl)-N-methyl-[1,10-biphenyl]-3-sulfonamide
-
3'-methoxy-N-(3-methoxyphenyl)-N-methylbiphenyl-4-carboxamide
-
3'-methoxy-N-(4-methoxyphenyl)-N-methyl-[1,1'-biphenyl]-4-sulfonamide
-
3,3',4,4'-tetrahydroxy-7,7'-dimethyl-5,5'-bis(1-methylethyl)-2H,2'H-8,8'-binaphtho[1,8-bc]furan-2,2'-dione
-
3,4,5-trimethoxycinnamic acid
-
3-(17beta-hydroxy-3-methoxy-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide
0.01 mM, 90% inhibition, substrate: estrone
3-(17beta-hydroxy-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide
0.01 mM, 79% inhibition, substrate: estrone
3-(2-furylmethyl)-8-hydroxy-2-(2-phenylethyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
33% inhibition at 100 nM, 78% inhibition at 0.001 mM
3-(2-naphthyl)phenol
0.001 mM, 61% inhibition, substrate: estrone
3-(3,17beta-dihydroxy-2-methoxy-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide
0.01 mM, 81% inhibition, substrate: estrone
3-(3,17beta-dihydroxy-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide
0.001 mM, 94% inhibition, substrate: estrone
3-(3-hydroxy-17-oxo-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide
0.001 mM, 88% inhibition, substrate: estrone
3-(3-hydroxyphenyl)quinolin-7-ol
0.001 mM, 57% inhibition, substrate: estrone
3-(3-methoxy-17-oxo-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide
0.01 mM, 76% inhibition, substrate: estrone
3-(6-hydroxy-2-naphthyl)benzoic acid
0.001 mM, 76% inhibition, substrate: estrone
3-(hydroxymethyl)-4-(phenylsulfanyl)-2,7,8,9,10,11-hexahydro[1]benzothieno[2',3':4,5]pyrimido[1,2-a]azepin-13(1H)-one
0.001 mM, 52% inhibition
3-(quinolin-3-yl)phenol
0.001 mM, 18% inhibition, substrate: estrone
3-(trifluoromethyl)-cinnamic acid
-
3-acetyl-2-oxo-2H-chromen-7-yl trifluoromethanesulfonate
IC50 value of 360 nM against recombinant enzyme in bacterial homogenate
3-acetyl-7-(4-hydroxyphenyl)-2H-chromen-2-one
IC50 value of 270 nM against recombinant enzyme in bacterial homogenate, and high selectivity for isoform 17beta-HSD1 over 17beta-HSD2 and against the alpha and beta estrogen receptors
3-benzyl-2-(2-bromo-3,4,5-trimethoxyphenyl)-8-hydroxy[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
3-benzyl-8-hydroxy-2-(2-methylprop-1-en-1-yl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
82% inhibition at 100 nM, 97% inhibition at 0.001 mM
3-benzyl-8-hydroxy-2-(2-thienyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
83% inhibition at 100 nM, 89% inhibition at 0.001 mM
3-benzyl-8-hydroxy-2-(3,4,5-trimethoxyphenyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
3-benzyl-8-hydroxy-2-(3-methoxyphenyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
89% inhibition at 100 nM, 95% inhibition at 0.001 mM
3-butyl-8-hydroxy-2-(3,4,5-trimethoxybenzyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
0.001 mM,k 95% inhibition
3-butyl-8-hydroxy-2-(3,4,5-trimethoxyphenyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
86% inhibition at 100 nM, 95% inhibition at 0.001 mM
3-hydroxy-13alpha-D-secooxime
displays an outstanding cofactor dependence, i.e. more efficient inhibition in the presence of NADH than NADPH
3-hydroxy-13beta-D-secoalcohol
displays an outstanding cofactor dependence, i.e. more efficient inhibition in the presence of NADH than NADPH
3-hydroxy-17-oxoestra-1(10),2,4-triene-16-carboxylic acid
-
3-hydroxy-17-oxoestra-1(10),2,4-triene-2-carbonitrile
-
3-hydroxy-2-methoxy-17-oxoestra-1(10),2,4-triene-16-carbonitrile
0.01 mM, 35% inhibition
3-hydroxy-7-(3-hydroxyphenyl)-1-naphthonitrile
99% inhibition at 0.001 mM
3-hydroxy-7-(3-hydroxyphenyl)-N-methyl-2-naphthamide
18% inhibition at 0.001 mM
3-hydroxy-7-(3-hydroxyphenyl)-N-phenyl-2-naphthamide
62% inhibition at 0.001 mM
3-hydroxy-N-(3'-hydroxy-[1,1'-biphenyl]-3-yl)-N-methylbenzenesulfonamide
17% inhibition at 0.001 mM
3-hydroxy-N-(3'-hydroxy-[1,1'-biphenyl]-4-yl)-N-methylbenzenesulfonamide
22% inhibition at 0.001 mM
3-hydroxy-N-(6-hydroxy-1,3-benzothiazol-2-yl)benzamide
modeling of binding to crystal structure shows five hydrogen bond interactions and a cation-pi-interaction
3-hydroxyestra-1(10),2,4-triene-16,17-dione 16-oxime
-
3-methoxy-N-(3'-methoxy-[1,1'-biphenyl]-3-yl)-N-methylbenzenesulfonamide
68% inhibition at 0.001 mM
3-methoxy-N-(3'-methoxy-[1,10-biphenyl]-4-yl)-Nmethylbenzenesulfonamide
18% inhibition at 0.001 mM
3-phenoxybenzyl (2E)-3-(1,3-benzodioxol-5-yl)prop-2-enoate
14% inhibition at 0.006 mM
3-phenoxybenzyl (2E)-3-phenylprop-2-enoate
13% inhibition at 0.006 mM
3-[(15beta)-3-hydroxy-17-oxoestra-1(10),2,4-trien-15-yl]-N-(4-methyl-1,3-thiazol-2-yl)propanamide
-
3-[(15beta)-3-methoxy-17-oxoestra-1(10),2,4-trien-15-yl]-N-(5-methyl-1,3-thiazol-2-yl)propanamide
-
3-[(4-chlorophenyl)sulfanyl]-6-(2,4-dimethyl-1H-pyrrol-1-yl)pyridazine
-
3-[(4bS,6aS,6bR,10S,10aS,11aS,11bR)-9-hexyl-2,10a-dihydroxy-6a-methyl-8-oxo-4b,5,6,6a,6b,8,9,10,10a,11,11a,11b,12,13-tetradecahydronaphtho[20,10:4,5]indeno[2,1-][1,3]oxazin-10-yl]benzamide
-
3-[(4bS,6aS,6bR,10S,10aS,11aS,11bR)-9-octyl-2,10a-dihydroxy-6a-methyl-8-oxo-4b,5,6,6a,6b,8,9,10,10a,11,11a,11b,12,13-tetradecahydronaphtho[20,10:4,5]indeno[2,1-][1,3]oxazin-10-yl]benzamide
-
3-[(4bS,6aS,6bR,10S,11aR,11bR)-9-butyl-2-hydroxy-6a-methyl-8-oxo-4b,5,6,6a,6b,8,9,10,11a,11b,12,13-dodecahydronaphtho[20,10:4,5]indeno[2,1-e][1,3]oxazin-10-l]benzamide
-
3-[(4bS,6aS,6bR,10S,11aR,11bR)-9-ethyl-2-hydroxy-6a-methyl-8-oxo-4b,5,6,6a,6b,8,9,10,11a,11b,12,13-dodecahydronaphtho[20,10:4,5]indeno[2,1-e][1,3]oxazin-10-l]benzamide
-
3-[(4bS,6aS,6bR,10S,11aR,11bR)-9-hexyl-2-hydroxy-6a-methyl-8-oxo-4b,5,6,6a,6b,8,9,10,11a,11b,12,13-dodecahydronaphtho[20,10:4,5]indeno[2,1-e][1,3]oxazin-10-l]benzamide
-
3-[(4bS,6aS,6bR,10S,11aR,11bR)-9-octyl-2-hydroxy-6a-methyl-8-oxo-4b,5,6,6a,6b,8,9,10,11a,11b,12,13-dodecahydronaphtho[20,10:4,5]indeno[2,1-e][1,3]oxazin-10-l]benzamide
-
3-[(5-bromofuran-2-yl)methyl]-8-hydroxy-2-(3,4,5-trimethoxybenzyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
0.001 mM, 95% inhibition
3-[(5-bromofuran-2-yl)methyl]-8-hydroxy-2-(3,4,5-trimethoxyphenyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
94% inhibition at 100 nM, 99% inhibition at 0.001 mM
3-[(6aS)-2-hydroxy-6a-methyl-4b,6,6a,10,10a,10b,11,12-octahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazol-8(5H)-yl]propanenitrile
-
3-[(6aS,6bR,10S,10aS)-9-butyl-2,10a-dihydroxy-6a-methyl-8-oxo-4b,5,6,6a,6b,8,9,10,10a,11,11a,11b,12,13-tetradecahydronaphtho[2',1':4,5]indeno[2,1-e][1,3]oxazin-10-yl]benzamide
-
3-[(6aS,6bR,10S,10aS)-9-ethyl-2,10a-dihydroxy-6a-methyl-8-oxo-4b,5,6,6a,6b,8,9,10,10a,11,11a,11b,12,13-tetradecahydronaphtho[2',1':4,5]indeno[2,1-e][1,3]oxazin-10-yl]benzamide
-
3-[1-(4-hydroxyphenyl)-1H-1,2,3-triazol-4-yl]-phenol
17beta-HSD1
3-[2-(2-thienyl)pyridin-4-yl]phenol
3-[2-(5-chloro-2-thienyl)pyridin-4-yl]phenol
3-[2-hydroxy-6-(3-hydroxyphenyl)-1-naphthyl]-N-methylpropanamide
80% inhibition at 0.001 mM
3-[3-(4-hydroxyphenyl)isoxazol-5-yl]-phenol
17beta-HSD1
3-[4-(4-hydroxyphenyl)-1,3-oxazol-2-yl]-phenol
17beta-HSD1
3-[4-(4-hydroxyphenyl)-1H-1,2,3-triazol-1-yl]-phenol
17beta-HSD1
3-[4-(5-chloro-2-thienyl)pyridin-2-yl]phenol
3-[5-(4-hydroxyphenyl)-1,3-oxazol-2-yl]-phenol
very good selectivity, high cell permeability and medium CaCo-2 permeability, 17beta-HSD1
3-[5-(5-chloro-2-thienyl)pyridin-3-yl]phenol
3-[6-(5-chloro-2-thienyl)pyridin-2-yl]phenol
3-[[(16beta,17beta)-3-(2-bromoethyl)-17-hydroxyestra-1,3,5(10)-trien-16-yl]methyl] benzamide
irreversible inhibitor
4'-(2-thienyl)biphenyl-3-ol
4'-(3-furyl)biphenyl-3-ol
0.001 mM, 10 min, 17% inhibition
4'-(3-thienyl)biphenyl-3-ol
4'-(5-chloro-2-thienyl)biphenyl-3-ol
4'-(6-methoxypyridin-3-yl)biphenyl-3-ol
4'-cyanophenyl 3,4-methylenedioxycinnamate
-
4'-hydroxy-N-(3-hydroxybenzyl)-N-methylbiphenyl-3-carboxamide
-
4'-methoxy-N-(3-methoxybenzyl)-N-methylbiphenyl-3-carboxamide
-
4'-methoxy-N-(3-methoxyphenyl)-N-methyl-[1,1'-biphenyl]-4-sulfonamide
-
4-(17beta-hydroxy-3-methoxy-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide
0.01 mM, 38% inhibition, substrate: estrone
4-(3'-ethyl-4'-hydroxy-3-methyl-biphenyl)-4-oxo-N-pyridin-3-ylmethyl-butyramide
37°C, 0.001 mM, 21% inhibition, substrate: estrone,7beta-HSD type 1
4-(3'-ethyl-4'-hydroxy-biphenyl)-2,2-dimethyl-4-oxo-N-pyridin-3-ylethyl-butyramide
37°C, 0.001 mM, 15% inhibition, substrate: estrone, 7beta-HSD type 1
4-(3'-ethyl-4'-hydroxy-biphenyl)-4-oxo-N-(2-hydroxyethyl)-butyramide
37°C, 0.001 mM, 23% inhibition, substrate: estrone, 7beta-HSD type 1
4-(3'-ethyl-4'-hydroxy-biphenyl)-4-oxo-N-pyridin-3-ylethyl-butyramide
37°C, 0.001 mM, 17% inhibition, substrate: estrone, 7beta-HSD type 1
4-(3'-ethyl-4'-hydroxy-biphenyl)-4-oxo-N-pyridin-3-ylmethyl-butyramide
37°C, 0.001 mM, 24% inhibition, substrate: estrone, 7beta-HSD type 1
4-(3'-ethyl-4'-methoxy-biphenyl)-2,2-dimethyl-4-oxo-N-pyridin-3-ylmethyl-butyramide
37°C, 0.001 mM, 17% inhibition, substrate: estrone, 7beta-HSD type 1
4-(3,17beta-dihydroxy-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide
0.01 mM, 74% inhibition, substrate: estrone
4-(3-ethyl-4-hydroxy-3-methyl-biphenyl)-4-oxo-N-pyridin-3-ylethyl-butyramide
37°C, 0.001 mM, 15% inhibition, substrate: estrone, 7beta-HSD type 1
4-(3-ethyl-4-hydroxy-biphenyl)-2,2-dimethyl-4-oxo-N-pyridin-3-ylmethyl-butyramide
37°C, 0.001 mM, 38% inhibition, substrate: estrone, 7beta-HSD type 1
4-(3-Hydroxy-17-oxo-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide
0.01 mM, 76% inhibition, substrate: estrone
4-(3-methoxy-17-oxo-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide
0.01 mM, 56% inhibition, substrate: estrone
4-(octanoylamino)phenyl (2E)-3-phenylprop-2-enoate
15% inhibition at 0.006 mM
4-cyanophenyl (2E)-3-(1,3-benzodioxol-5-yl)prop-2-enoate
76% inhibition at 0.006 mM
4-fluoro-3-hydroxy-N-(3'-hydroxybiphenyl-3-yl)-N-methylbenzenesulfonamide
80% inhibition at 0.001 mM
4-fluoro-3-methoxy-N-(3'-methoxybiphenyl-3-yl)-N-methylbenzenesulfonamide
17% inhibition at 0.001 mM
4-methyl-3-(trifluoromethyl)-5-[[4-(trifluoromethyl)benzyl]sulfanyl]-4H-1,2,4-triazole
-
4-methyl-5-[6-(2,2,2-trifluoroethoxy)pyridin-3-yl]-4H-1,2,4-triazole-3-thiol
-
4-methyl-N-[4-[4-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]benzenesulfonamide
-
4-[(15beta)-3-hydroxy-17-oxo-2-propylestra-1(10),2,4-trien-15-yl]-N-[2-(7-methyl-1H-indol-2-yl)ethyl]butanamide
0.0001 mM, 69% inhibition
4-[(15beta)-3-hydroxy-17-oxoestra-1(10),2,4-trien-15-yl]-N-[2-(7-methyl-1H-indol-3-yl)ethyl]butanamide
-
5'-O-[9-[(16b,17b)-3,17-dihydroxyestra-1(10),2,4-trien-16-yl]nonanoyl]adenosine
-
5'-O-[9-[(16beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-16-yl]nonanoyl]adenosine
EM-1745, bisubstrate inhibitor of 17beta-HSD1
5-(3-ethyl-4-hydroxyphenyl)-indan-1-one
37°C, 0.01 mM, 86% inhibition, substrate: estrone, 7beta-HSD type 1
5-(3-fluoro-4-hydroxyphenyl)-indan-1-one
37°C, 0.01 mM, 75% inhibition, substrate: estrone, 7beta-HSD type 1
5-(3-fluoro-4-methoxyphenyl)-indan-1-one
37°C, 0.01 mM, 56% inhibition, substrate: estrone, 7beta-HSD type 1
5-(4-hydroxyphenyl)-indan-1-one
37°C, 0.01 mM, 81% inhibition, substrate: estrone, 7beta-HSD type 1
5-(6-hydroxy-2-naphthyl)pyridin-3-ol
0.001 mM, 58% inhibition, substrate: estrone
5-benzyl-3-(furan-2-ylmethyl)-8-hydroxy-2-(2-phenylethyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
5% inhibition at 100 nM, 26% inhibition at 0.001 mM
5-bromo-3-(2-methylpropyl)-2-(3,4,5-trimethoxyphenyl)-6,7-dihydro[1]benzothieno[2,3-d]pyrimidine-4,8(3H,5H)-dione
0.001 mM, 54% inhibition
5-butyl-3-(furan-2-ylmethyl)-8-hydroxy-2-(2-phenylethyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
9% inhibition at 100 nM, 27% inhibition at 0.001 mM
5-[(15beta)-3-methoxy-17-oxoestra-1(10),2,4-trien-15-yl]-N-(2-thiophen-2-ylethyl)pentanamide
-
6-(3-ethyl-4-hydroxyphenyl)-3,4-dihydro-2H-naphthalen-1-one
37°C, 0.01 mM, 51% inhibition, substrate: estrone, 7beta-HSD type 1
6-(3-ethyl-4-methoxyphenyl)-3,4-dihydro-2H-naphthalen-1-one
37°C, 0.01 mM, 71% inhibition, substrate: estrone, 7beta-HSD type 1
6-(3-hydroxyphenyl)-1-((4-methylphenyl)sulfonyl)-2-naphthol
75% inhibition at 0.001 mM
6-(3-hydroxyphenyl)-1-(morpholin-4-ylcarbonyl)-2-naphthol
62% inhibition at 0.001 mM
6-(3-hydroxyphenyl)-1-(phenylsulfonyl)-2-naphthol
33% inhibition at 0.001 mM
6-(3-hydroxyphenyl)-1-(piperazin-1-ylcarbonyl)-2-naphthol
45% inhibition at 0.001 mM
6-(3-hydroxyphenyl)-1-(piperidin-1-ylcarbonyl)-2-naphthol
73% inhibition at 0.001 mM
6-(3-hydroxyphenyl)-1-naphthol
0.001 mM, 23% inhibition, substrate: estrone
6-(3-hydroxyphenyl)-1-phenyl-2-naphthol
89% inhibition at 0.001 mM
6-(3-hydroxyphenyl)-2-naphthol
6-(3-hydroxyphenyl)-3,4-dihydronaphthalen-1(2H)-one
0.001 mM, 23% inhibition, substrate: estrone
6-(4-hydroxy-phenyl)-3,4-dihydro-2H-naphthalen-1-one
37°C, 0.01 mM, 89% inhibition, substrate: estrone, 7beta-HSD type 1
6-(4-hydroxyphenyl)-1-naphthol
0.001 mM, 55% inhibition, substrate: estrone
6-butyl-3-(furan-2-ylmethyl)-8-hydroxy-2-(2-phenylethyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
52% inhibition at 100 nM, 81% inhibition at 0.001 mM
6-hydroxyflavone
53.3% inhibition at 0.006 mM
6-pyridin-3-yl-2-naphthol
0.001 mM, 32% inhibition, substrate: estrone
6-[(1,3-benzothiazol-2-ylsulfanyl)methyl]-4-butoxy-2-(trifluoromethyl)quinoline
-
6-[4-(hydroxymethyl)phenyl]-2-naphthol
0.001 mM, 13% inhibition, substrate: estrone
6-[4-(trifluoromethyl)phenoxy]pyridin-3-amine
-
7,4'-Dihydroxyflavone
more than 90% inhibition at 0.006 mM
7-(3-hydroxyphenyl)-2-naphthol
0.001 mM, 62% inhibition, substrate: estrone
7-hydroxy-3-(3-hydroxyphenyl)-1-naphthonitrile
53% inhibition at 0.001 mM
8-hydroxy-3-(2-methylbutyl)-2-(3,4,5-trimethoxyphenyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
91% inhibition at 100 nM, 94% inhibition at 0.001 mM
8-hydroxy-3-(2-methylprop-1-en-1-yl)-2-(3,4,5-trimethoxyphenyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
0.001 mM, 97% inhibition
8-hydroxy-3-(2-methylpropyl)-2-(3,4,5-trimethoxyphenyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
93% inhibition at 100 nM, 98% inhibition at 0.001 mM
baicalein
i.e. 5,6,7-trihydroxyflavone, 61% inhibition at 0.006 mM
benzyl (2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoate
60% inhibition at 0.006 mM
benzyl (2E)-3-phenylprop-2-enoate
35% inhibition at 0.006 mM
chrysoeriol
i.e. 4',5,7-trihydroxy-3'-methoxyflavone, 82% inhibition at 0.006 mM
coumarin-3-carboxylic acid
-
cyclohexyl (2E)-3-phenylprop-2-enoate
25% inhibition at 0.006 mM
diosmetin
i.e. 3',5,7-trihydroxy-4'-methoxyflavone, more than 90% inhibition at 0.006 mM
Disulfiram
irreversible inhibition
Dithiocarbamate
irreversible inhibition of 17beta-HSD1, preincubation with NADPH protects from inhibition
ethyl (2Z)-hydroxy[(16Z)-3-hydroxy-17-oxoestra-1(10),2,4-trien-16-ylidene]ethanoate
-
ethyl 4-[([4-[(15alpha)-3-hydroxy-17-oxoestra-1(10),2,4-trien-15-yl]butyl]carbamoyl)amino]benzoate
-
ethyl [(6aS)-2-hydroxy-6a-methyl-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazol-9-yl]acetate
-
eupatorin
37% inhibition at 0.006 mM
fisetin
72% inhibition at 0.006 mM
genkwanin
3',5-dihydroxy-7-methoxyflavone, 81% inhibition at 0.006 mM
maneb
irreversible inhibition
methyl 3-hydroxy-17-oxoestra-1(10),2,4-triene-16-carboxylate
0.01 mM, 69% inhibition
methyl [(6aS)-2-hydroxy-6a-methyl-4b,6,6a,10,10a,10b,11,12-octahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazol-8(5H)-yl]acetate
-
myricetin
i.e. 3,3',4',5',5,7-hexahydroxyflavone, 52% inhibition at 0.006 mM
N'-[(2,4-difluorophenyl)sulfonyl]-2-pyridin-3-yl-4,5-dihydro-1,3-thiazole-4-carbohydrazide
-
N-(1,3-benzodioxol-5-ylmethyl)-5-[(15beta)-3-methoxy-17-oxoestra-1(10),2,4-trien-15-yl]pentanamide
-
N-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-methyl-1,2,3-thiadiazole-5-carboxamide
-
N-(2,4-difluorobenzyl)-4-[(15beta)-3-hydroxy-17-oxoestra-1(10),2,4-trien-15-yl]butanamide
-
N-(3-hydroxyphenyl)-3'-methoxy-N-methyl-[1,1'-biphenyl]-4-sulfonamide
-
N-(3-hydroxyphenyl)-N,3'-dimethyl-[1,1'-biphenyl]-4-sulfonamide
15% inhibition at 0.001 mM
N-(3-hydroxyphenyl)-N-methyl-4-(thiophen-2-yl)benzenesulfonamide
-
N-(3-methoxyphenyl)-N-methyl-4-(thiophen-2-yl)benzenesulfonamide
-
N-(3-methoxyphenyl)-N-methyl-4-(thiophen-3-yl)benzenesulfonamide
-
N-(4-hydroxyphenyl)-N-methyl-4-(pyridin-3-yl)benzenesulfonamide
14% inhibition at 0.001 mM
N-benzyl-4-[(15alpha)-3-hydroxy-17-oxoestra-1(10),2,4-trien-15-yl]butanamide
-
N-benzyl-4-[(15beta)-3-hydroxy-17-oxoestra-1(10),2,4-trien-15-yl]butanamide
-
N-benzyl-4-[(15beta)-3-methoxy-17-oxoestra-1(10),2,4-trien-15-yl]-N-methylbutanamide
-
N-butyl-6-[[(6beta,17beta)-17-hydroxyestra-1(10),2,4-trien-6-yl]sulfanyl]-N-methylhexanamide
-
N-butyl-6-[[(6beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-6-yl]oxy]-N-methylhexanamide
-
N-butyl-6-[[(6beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-6-yl]sulfanyl]-N-methylhexanamide
N-butyl-7-[(6beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-6-yl]-N-methylheptanamide
-
N-butyl-N-methyl-11-[16beta-(3-carbamoylbenzyl)-3,17-dihydroxy-estra-1,3,5(10)-trien-7alpha-yl]-undecanamide
0.01 mM, 61% inhibition, substrate: estrone
N-cyclohexyl-3-[(15beta)-3-hydroxy-17-oxoestra-1(10),2,4-trien-15-yl]propanimidamide
-
N-cyclohexyl-3-[(15beta)-3-methoxy-17-oxoestra-1(10),2,4-trien-15-yl]-N-methylpropanamide
-
N-cyclohexyl-3-[(15beta)-3-methoxy-17-oxoestra-1(10),2,4-trien-15-yl]propanamide
-
N-cyclooctyl-3-[(15beta)-3-methoxy-17-oxoestra-1(10),2,4-trien-15-yl]propanamide
-
N-[2-(4-hydroxyphenyl)ethyl]-3-[(15beta)-3-methoxy-17-oxoestra-1(10),2,4-trien-15-yl]propanamide
-
N-[3-(6-hydroxy-2-naphthyl)phenyl]acetamide
0.001 mM, 19% inhibition, substrate: estrone
N-[[(15alpha)-3-hydroxy-17-oxoestra-1(10),2,4-trien-15-yl]methyl]-N-methylthiophene-2-sulfonamide
-
N-[[(15alpha)-3-hydroxy-17-oxoestra-1(10),2,4-trien-15-yl]methyl]benzenesulfonamide
-
N-[[(15alpha)-3-hydroxy-17-oxoestra-1(10),2,4-trien-15-yl]methyl]thiophene-2-sulfonamide
-
naphthalen-2-yl (2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoate
56% inhibition at 0.006 mM
phenyl (2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoate
35% inhibition at 0.006 mM
S-(4-fluorophenyl) 2-methyl-4-(trifluoromethyl)benzenecarbothioate
-
scutellarein
i.e. 4',5,6,7-tetrahydroxyflavone, 88% inhibition at 0.006 mM
thiram
irreversible inhibition
zineb
irreversible inhibition
[4-[4-(2-methoxyphenyl)piperidin-1-yl]-3-nitrophenyl]methanol
-
(10R,13S,17R)-10,13-dimethyl-1,2,7,8,9,10,11,12,13,14,15,16-dodecahydro-3'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-3,5',6(4'H)-trione
-
0.003 mM, 45% inhibition, substrate: 4-androstene-3,17-dione
(10R,13S,17R)-10,13-dimethyl-1,6,7,8,9,10,11,12,13,14,15,16-dodecahydro-3'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-3,5'(2H,4'H)-dione
(13S,17R)-13-methyl-4',5',6,7,8,9,11,12,13,14,15,16-dodecahydro-3'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-3,5'-diol
-
0.003 mM, 61% inhibition, substrate: 4-androstene-3,17-dione
(13S,17R)-3-hydroxy-13-methyl-3',4',6,7,8,9,11,12,13,14,15,16-dodecahydro-5'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-5'-one
-
0.003 mM, 79% inhibition, substrate: 4-androstene-3,17-dione
(13S,17R)-3-hydroxy-13-methyl-5'-propyl-4',5',6,7,8,9,11,12,13,14,15,16-dodecahydrospiro[cyclopenta[a]phenanthrene-17,2'-pyran]-6'(3'H)-one
-
0.003 mM, 83% inhibition, substrate: 4-androstene-3,17-dione
(13S,17R)-3-hydroxy-5',13-dimethyl-4',5',6,7,8,9,11,12,13,14,15,16-dodecahydrospiro[cyclopenta[a]phenanthrene-17,2'-pyran]-6'(3'H)-one
-
0.003 mM, 94% inhibition, substrate: 4-androstene-3,17-dione
(13S,17R)-5',13-dimethyl-4',5',6,7,8,9,11,12,13,14,15,16-dodecahydrospiro[cyclopenta[a]phenanthrene-17,2'-pyran]-6'(3'H)-one
-
0.003 mM, 94% inhibition, substrate: 4-androstene-3,17-dione
(13S,17R)-5',5',13-trimethyl-4',5',6,7,8,9,11,12,13,14,15,16-dodecahydrospiro[cyclopenta[a]phenanthrene-17,2'-pyran]-6'(3'H)-one
-
0.003 mM, 95% inhibition, substrate: 4-androstene-3,17-dione
(13S,17S)-13-methyl-4',5',6,7,8,9,11,12,13,14,15,16-dodecahydrospiro[cyclopenta[a]phenanthrene-17,2'-pyran]-6'(3'H)-one
-
0.003 mM, 95% inhibition, substrate: 4-androstene-3,17-dione
(13S,17S)-3-hydroxy-13-methyl-3',4',6,7,8,9,11,12,13,14,15,16-dodecahydro-5'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-5'-one
-
0.003 mM, 45% inhibition, substrate: 4-androstene-3,17-dione
(13S,17S)-3-hydroxy-13-methyl-4',5',6,7,8,9,11,12,13,14,15,16-dodecahydrospiro[cyclopenta[a]phenanthrene-17,2'-pyran]-6'(3'H)-one
-
0.003 mM, 95% inhibition, substrate: 4-androstene-3,17-dione
(13S,17S)-3-hydroxy-13-methyl-6,7,8,9,11,12,13,14,15,16-decahydro-7'H-spiro[cyclopenta[a]phenanthrene-17,2'-oxepan]-7'-one
-
0.003 mM, 93% inhibition, substrate: 4-androstene-3,17-dione
(2'R,13S)-3-hydroxy-13-methyl-6,7,8,9,11,12,13,14,15,16-decahydrospiro[cyclopenta[a]phenanthrene-17,2'-pyran]-6'(3'H)-one
-
0.003 mM, 92% inhibition, substrate: 4-androstene-3,17-dione
(2'R,13S)-3-hydroxy-4',13-dimethyl-4',5',6,7,8,9,11,12,13,14,15,16-dodecahydrospiro[cyclopenta[a]phenanthrene-17,2'-pyran]-6'(3'H)-one
-
0.003 mM, 94% inhibition, substrate: 4-androstene-3,17-dione
(2'R,13S)-3-hydroxy-5',5',13-trimethyl-4',5',6,7,8,9,11,12,13,14,15,16-dodecahydrospiro[cyclopenta[a]phenanthrene-17,2'-pyran]-6'(3'H)-one
-
0.003 mM, 94% inhibition, substrate: 4-androstene-3,17-dione
(2'R,13S)-5'-cyclopropyl-3-hydroxy-13-methyl-4',5',6,7,8,9,11,12,13,14,15,16-dodecahydrospiro[cyclopenta[a]phenanthrene-17,2'-pyran]-6'(3'H)-one
-
0.003 mM, 91% inhibition, substrate: 4-androstene-3,17-dione
(2'R,13S)-methyl 3-hydroxy-13-methyl-6'-oxo-3',4',5',6,6',7,8,9,11,12,13,14,15,16-tetradecahydrospiro[cyclopenta[a]phenanthrene-17,2'-pyran]-5'-carboxylate
-
0.003 mM, 92% inhibition, substrate: 4-androstene-3,17-dione
(2,4-dihydroxyphenyl)-phenylmethanone
-
-
(4aR,6aS,7S)-7-[heptyl(methyl)amino]-1,4a,6a-trimethylhexadecahydro-2H-indeno[5,4-f]quinolin-2-one
-
(4aR,6aS,7S)-7-[heptyl(methyl)amino]-4a,6a-dimethylhexadecahydro-2H-indeno[5,4-f]quinolin-2-one
-
(4R,5R)-4-(2-fluorophenyl)-5-[hydroxy(5-phenylthiophen-2-yl)methyl]-1-methylpyrrolidin-2-one
-
(4R,5R)-5-[hydroxy[5-(pyridin-3-yl)thiophen-2-yl]methyl]-1-methyl-4-phenylpyrrolidin-2-one
-
(4S,5S)-5-[biphenyl-3-yl(hydroxy)methyl]-4-(2-fluorophenyl)-1-methylpyrrolidin-2-one
-
(4S,5S)-5-[biphenyl-4-yl(hydroxy)methyl]-4-(2-fluorophenyl)-1-methylpyrrolidin-2-one
-
(4S,5S)-5-[hydroxy[5-(pyridin-3-yl)thiophen-2-yl]methyl]-1-methyl-4-phenylpyrrolidin-2-one
-
(6aS,6bR,10aR)-2-hydroxy-6a-methyl-5,6,6a,6b,9,10,10a,11,11a,11b,12,13-dodecahydronaphtho[2',1':4,5]indeno[1,2-b]pyran-8(4bH)-one
-
0.003 mM, 52% inhibition, substrate: 4-androstene-3,17-dione
(6aS,6bS,10aS)-2-hydroxy-6a-methyl-5,6,6a,6b,9,10,10a,11,11a,11b,12,13-dodecahydronaphtho[2',1':4,5]indeno[1,2-b]pyran-8(4bH)-one
-
0.003 mM, 85% inhibition, substrate: 4-androstene-3,17-dione
(6aS,6bS,11aS)-2-hydroxy-6a-methyl-4b,5,6,6a,6b,9,10,11,11a,12,12a,12b,13,14-tetradecahydro-8H-naphtho[2',1':4,5]indeno[1,2-b]oxepin-8-one
-
0.003 mM, 91% inhibition, substrate: 4-androstene-3,17-dione
(6aS,6bS,9aR)-2-hydroxy-6a-methyl-4b,5,6,6a,6b,9,9a,10,10a,10b,11,12-dodecahydro-8H-naphtho[2',1':4,5]indeno[1,2-b]furan-8-one
-
0.003 mM, 62% inhibition, substrate: 4-androstene-3,17-dione
(8R,9S,13S,14S,17S)-3-hydroxy-13-methyl-4',5',6,7,8,9,11,12,13,14,15,16-dodecahydrospiro[cyclopenta[a]phenanthrene-17,2'-pyran]-6'(3'H)-one
85% inhibition at 0.001 mM
(S)-2-Methoxy-6a-methyl-5,6,6a,10,10a,10b,11,12-octahydro-4bH-7-oxa-8-aza-pentaleno[2,1-a]phenanthrene
-
-
(S)-6a-Methyl-5,6,6a,10,10a,10b,11,12-octahydro-4bH-7-oxa-8-aza-pentaleno[2,1-a]phenanthren-2-ol
-
-
([4-[(3-methoxyphenyl)methyl]piperazin-1-yl]methyl)-17alpha-methylandrostane-3alpha,17beta-diol
0.1 mM, 21.9% inhibition in the reaction with allopregnanolone. 0.3 mM, 22.6% inhibition in the reaction with 17beta-estradiol
([4-[(3-methoxyphenyl)methyl]piperazin-1-yl]methyl)-17alpha-pregn-20-yne-3alpha,17-diol
0.1 mM, 20.0% inhibition in the reaction with allopregnanolone. 0.3 mM, 44.5% inhibition in the reaction with 17beta-estradiol
1'(2')H-estra-1,3,5(10)-trieno[17,16-c]pyrazol-3-ol
-
IC50: 0.0041 mM
1,1':4',1''-terphenyl-3,3''-diol
-
-
1,2,3,4-tetrahydroquinolin-7-yl 4-(acetylamino)benzenesulfonate
-
1,2-Cyclohexanedione
-
40 mM, pH 8.5, t1/2: 4.4 h
1,3,5(10),16-estratetraen-3-ol
-
-
1,3,5(10)-estratrien-3,16beta,17beta-triol
-
-
1,3,5(10)-estratrien-3,16beta-diol
-
-
1,3,5(10)-estratrien-3,17alpha-diol
-
-
1,3,5(10)-estratrien-3-ol
-
-
1,4-dibromo-2,3-butanedione
-
40 mM, pH 8.5, t1/2: 0.02 h
1-(3'-ethyl-4'-hydroxy-biphenyl-4-yl)-ethanone
1-(3-ethyl-4'-hydroxy-biphenyl-4-yl)-ethanone
71% inhibition at 0.001 mM
1-(4'-hydroxy-2'-methyl-biphenyl-4-yl)-ethanone
89% inhibition at 0.001 mM
1-(4'-hydroxy-biphenyl-4-yl)-ethanone
97% inhibition at 0.001 mM
1-(6-hydroxy-9H-fluoren-2-yl)-ethanone
86% inhibition at 0.001 mM
1-Chloro-4-(2,2-dichloro-1-(5-Chloro-phenyl)-ethyl)-benzene
-
oxidation of estradiol
1-Chloro-4-(2,2-dichloro-1-(6-Chloro-phenyl)-ethyl)-benzene
-
oxidation of estradiol
1-phenyl-1,2-propanedione
-
40 mM, pH 8.5, t1/2: 0.19 h
1-[2-[4-(6-Methoxy-2-phenyl-3,4-dihydro-naphthalen-1-yl)-phenoxy]-ethyl]-pyrrolidine
-
oxidation of estradiol
10-((13S,16S,17S)-3,17-Dihydroxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-16-yl)-decanoic acid 5-(6-amino-purin-9-yl)-3,4-dihydroxy-tetrahydro-furan-2-ylmethyl ester
-
IC50: 140 nM
11-((13S,17R)-17-Ethynyl-3,17-dihydroxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-7-yl)-undecanoic acid butyl-methyl-amide
-
-
16-difluoro-estradiol
-
oxidation of estradiol
16-methylen-estra-1,3,5(10)-triene-3,17beta-diol
-
suicide inhibitor
16-oxo-estrone
-
40 mM, pH 8.5, t1/2: 0.8-1 h, at pH 7.2 inhibition is competitive against estradiol and non-competitive against NAD+
16alpha-bromobutyl-estradiol
-
-
16alpha-bromopropyl-estradiol
-
IC50: 0.00046 mM, reduction of estrone, the inhibitor is totally inactive against type 2 17beta-HSD and type type 1 17beta-HSD
16beta-bromobutyl-estradiol
-
-
16beta-m-pyridylmethylamidomethyl-2-methoxyoestrone
-
IC50: 0.00029 mM
17(R,S)-14,15-secoestra-1,3,5(10)-trien-15-yne-3,17-diol
-
suicide inhibitor
17,17-difluoro-3beta-([4-[(3-methoxyphenyl)methyl]piperazin-1-yl]methyl)androstan-3alpha-ol
0.1 mM, 38.6% inhibition in the reaction with allopregnanolone. 0.3 mM, 13.3% inhibition in the reaction with 17beta-estradiol
17-(1-hydroxy-prop-2-ynyl)-10,13-dimethyl-1,2,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-cyclopenta[a]phenanthren-3-one
-
suicide inhibitor
17-deoxy-estradiol
-
oxidation of estradiol
17beta-[(N-decyl)formamido]-4-aza-5alpha-androstan-3-one
-
-
17beta-[(N-decyl)formamido]-4-methyl-4-aza-5alpha-androstan-3-one
-
-
17beta-[(N-heptyl)methylamino]-4-aza-5alpha-androstan-3-one
-
-
17beta-[(N-heptyl)methylamino]-4-methyl-4-aza-5alpha-androstan-3-one
-
-
17beta-[(N-nonyl)formamido]-4-methyl-4-aza-5alpha-androstan-3-one
-
-
2',4',4-trihydroxy-4'-chalcone
-
IC50: 0.0338 mM
2',4'-dihydroxy-chalcone
-
IC50: 0.0346 mM
2'-AMP
-
competitive with respect to NAD(H) or NADP(H) and noncompetitive with respect to the steroid
2'-methoxy-N-(3-methoxyphenyl)-N-methyl-[1,1'-biphenyl]-4-sulfonamide
23% inhibition at 0.001 mM
2'-methoxy-N-methyl-N-phenyl-[1,1'-biphenyl]-4-sulfonamide
10% inhibition at 0.001 mM
2,2',4,4'-tetrahydroxybenzophenone
-
-
2,3-Butanedione
-
40 mM, pH 8.5, t1/2: 2 h
2,3-Pentanedione
-
40 mM, pH 8.5, t1/2: 5.3 h
2-(2,6-dibromo-4-methylphenoxy)-N'-[(E)-(2,4-dihydroxy-6-methylphenyl)methylidene]acetohydrazide
64% inhibition at 0.02 mM
2-(2,6-dibromo-4-methylphenoxy)-N'-[(E)-(2,4-dimethoxyphenyl)methylidene]acetohydrazide
38% inhibition at 0.02 mM
2-(2-bromo-4,6-dimethylphenoxy)-N'-[(E)-(2,4-dihydroxyphenyl)methylidene]acetohydrazide
91% inhibition at 0.02 mM
2-(2-bromo-4-methylphenoxy)-N'-[(1E)-1-(2,4-dihydroxyphenyl)ethylidene]acetohydrazide
-
2-(acetylamino)phenyl 3,4-dimethylbenzenesulfonate
-
2-ethyl-3-sulfamoyloxy-17-oxo-estra-1,3,5(10)-trien-16-methylcarboxylic acid-S-alpha-methylbenzyl amide
-
50% inhibition at 0.001 mM
2-ethyl-3-sulfamoyloxy-17-oxo-estra-1,3,5(10)-trien-16alpha/beta-methylcarboxylic acid-(5-methylpyrimidinyl-2-ylmethyl)amide
-
37% inhibition at 0.001 mM
2-ethyl-3-sulfamoyloxy-17-oxo-estra-1,3,5(10)-trien-16alpha/beta-methylcarboxylic acid-(pyridine-3-ylmethyl)amide
-
64% inhibition at 0.01 mM
2-methoxyoestrone
-
IC50: 0.0024 mM
2-methoxyphenyl 3-(acetylamino)benzenesulfonate
-
2-methoxyphenyl benzenesulfonate
51% inhibition at 0.02 mM
2-methylcinnamic acid
-
IC50: 0.0064 mM
2-[(16beta)-2-ethyl-3-hydroxy-17-oxoestra-1(10),2,4-trien-16-yl]-N-(pyridin-3-ylmethyl)acetamide
-
2-[5-(3-ethyl-4-hydroxyphenyl)-1-oxo-indan-2-yl]-N-pyridin-3-ylmethyl-acetamide
39% inhibition at 0.001 mM
3',4',5,7-tetrahydroxy-flavone
-
IC50: 0.0006 mM
3',4',7-trihydroxy-isoflavone
-
IC50: 0.0052 mM
3'-hydroxy-N-(3-hydroxybenzyl)-N-methyl-[1,10-biphenyl]-4-sulfonamide
57% inhibition at 0.001 mM
3'-hydroxy-N-(3-hydroxybenzyl)-N-methylbiphenyl-3-carboxamide
-
3'-hydroxy-N-(3-hydroxybenzyl)-N-methylbiphenyl-4-carboxamide
-
3'-hydroxy-N-(3-hydroxyphenyl)-N-methyl-[1,10-biphenyl]-3-sulfonamide
68% inhibition at 0.001 mM
3'-hydroxy-N-(3-hydroxyphenyl)-N-methyl-[1,10-biphenyl]-4-sulfonamide
50% inhibition at 0.001 mM
3'-hydroxy-N-(3-hydroxyphenyl)-N-methylbiphenyl-3-carboxamide
35% inhibition
3'-hydroxy-N-(3-hydroxyphenyl)-N-methylbiphenyl-4-carboxamide
3'-hydroxy-N-(3-methoxyphenyl)-N-methyl-[1,10-biphenyl]-4-sulfonamide
38% inhibition at 0.001 mM
3'-methoxy-N-(2-methoxyphenyl)-N-methyl-[1,1'-biphenyl]-4-sulfonamide
10% inhibition at 0.001 mM
3'-methoxy-N-(3-methoxybenzyl)-N-methyl-[1,10-biphenyl]-4-sulfonamide
-
3'-methoxy-N-(3-methoxybenzyl)-N-methylbiphenyl-3-carboxamide
11% inhibition
3'-methoxy-N-(3-methoxybenzyl)-N-methylbiphenyl-4-carboxamide
-
3'-methoxy-N-(3-methoxyphenyl)-N-methyl-[1,1'-biphenyl]-4-sulfonamide
27% inhibition at 0.001 mM
3'-methoxy-N-(3-methoxyphenyl)-N-methyl-[1,10-biphenyl]-3-sulfonamide
26% inhibition at 0.001 mM
3'-methoxy-N-(3-methoxyphenyl)-N-methylbiphenyl-3-carboxamide
-
3'-methoxy-N-(3-methoxyphenyl)-N-methylbiphenyl-4-carboxamide
35% inhibition at 0.001 mM
3'-methoxy-N-(4-methoxyphenyl)-N-methyl-[1,1'-biphenyl]-4-sulfonamide
22% inhibition at 0.001 mM
3,3',4',7-tetrahydroxy-flavone
-
-
3,3'-(1-methyl-1H-1,2,4-triazole-3,5-diyl)diphenol
-
-
3,3'-(1-phenyl-1H-1,2,4-triazole-3,5-diyl)diphenol
-
-
3,3'-(1H-1,2,3-triazole-1,4-diyl)diphenol
3,3'-pyridine-2,5-diyldiphenol
-
-
3,4,5-trimethoxycinnamic acid
-
IC50: 0.049 mM
3,5,7-trihydroxy-4'-methoxy-flavone
-
IC50: 15 mM
3,5,7-trihydroxy-flavone
-
-
3,5-dibromosalicylic acid
-
-
3-([(16beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-16-yl]methyl)benzamide
-
-
3-([(16beta,17beta)-3-(2-bromoethyl)-17-hydroxyestra-1(10),2,4-trien-16-yl]methyl)benzamide
-
a potent and steroidal nonestrogenic inhibitor of 17beta-HSD1, inhibits the transformation of estrone into estradiol by 17beta-HSD1 in T-47D cells. The comppound does not inhibit enzymes 17beta-HSD2, 17beta-HSD7, 17beta-HSD12, and CYP3A4, and does not stimulate the proliferation of estrogen-sensitive MCF-7 cells. Kinetic and molecular modeling (docking) experiments show that compound is a competitive and irreversible inhibitor of 17beta-HSD1
3-benzylidene camphor
-
-
3-bromo-5-phenylsalicylic acid
-
-
3-bromo-N-(3-hydroxy-4-methylphenyl)benzenesulfonamide
-
3-coumaric acid
-
34% inhibition at 0.05 mM
3-cyclohexylpropanoic acid
-
weak inhibition, IC50: 0.1 mM, above
3-hydroxy-1,3,5(10)-triene-[17,16-c]-(5'-carboxylic acid)-pyrazole
-
0.01 mM: 32% inhibition
3-hydroxy-1,3,5(10)-triene-[17,16-c]-(5'-hydroxymethyl)-pyrazole
-
0.01 mM: 94% inhibition, IC50: 0.00095 mM
3-hydroxy-1,3,5(10)-triene-[17,16-c]-[5'-(carboxylic acid ethyl ester)]-pyrazole
-
0.01 mM: 94% inhibition, IC50: 0.00185 mM
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(1'-isobutyl)-pyrazole
-
0.01 mM: 77% inhibition
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(1'-methoxyethyl)-pyrazole
-
0.01 mM: 95% inhibition, IC50: 0.00053 mM
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(1'-methyl acetate)-pyrazole
-
0.01 mM: 95% inhibition, IC50: 0.00092 mM
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(1'-methyl)-pyrazole
-
0.01 mM: 94% inhibition, IC50: 0.00275 mM
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(1'-propionitrile)-pyrazole
-
0.01 mM: 95% inhibition, IC50: 0.00073 mM
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(2'-isobutyl)-pyrazole
-
0.01 mM: 70% inhibition
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(2'-methoxy-ethyl)-pyrazole
-
0.01 mM: 83% inhibition
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(2'-methyl acetate)-pyrazole
-
0.01 mM: 79% inhibition
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(2'-methyl)-pyrazole
-
0.01 mM: 43% inhibition
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(5'-ethylme-thylcarbamoyl)-pyrazole
-
0.01 mM: 88% inhibition
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(5'-isopropylcarbamoyl)-pyrazole
-
0.01 mM: 57% inhibition
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(5'-methyl)-pyrazole
-
0.01 mM: 75% inhibition
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(5'-methyl-carbamoyl)-pyrazole
-
0.01 mM: 62% inhibition
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-[5'-(1''-methylpiperazin-4''-ylmethyl)carbamoyl]-pyrazole
-
0.01 mM: 50% inhibition
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-[5'-(1'-methylpyrrol-2''-ylmethyl)carbamoyl]-pyrazole
-
0.01 mM: 89% inhibition, IC50: 0.0023 mM
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-[5'-(5''-methylpyrazin-2''-ylmethyl)carbamoyl]-pyrazole
-
0.01 mM: 80% inhibition
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-[5'-(pyridin-2''-ylmethyl)carbamoyl]-pyrazole
-
0.01 mM: 93% inhibition, IC50: 0.00088 mM
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-[5'-(pyridin-3''-ylethyl)carbamoyl]-pyrazole
-
0.01 mM: 99% inhibition, IC50: 0.0003 mM
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-[5'-(pyridin-3''-ylmethyl)carbamoyl]-pyrazole
-
0.01 mM: 92% inhibition, IC50: 0.00078 mM
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-[5'-(tetrahydrofuran-2''-ylmethyl)carbamoyl]-pyrazole
-
0.01 mM: 87% inhibition
3-hydroxy-N-(3'-hydroxy-[1,1'-biphenyl]-3-yl)-N-methylbenzenesulfonamide
88% inhibition at 0.001 mM
3-hydroxy-N-(3'-hydroxy-[1,1'-biphenyl]-4-yl)-N-methylbenzenesulfonamide
66% inhibition at 0.001 mM
3-hydroxyestra-1,3,5(10),7-tetraen-17-one
-
IC50: 0.0019 mM, oxidation of estradiol
3-methoxy-1'(2')H-estra-1,3,5(10)-trieno[17,16-c]pyrazole
-
-
3-methoxy-N-(3'-methoxy-[1,1'-biphenyl]-3-yl)-N-methylbenzenesulfonamide
14% inhibition at 0.001 mM
3-methoxy-N-(3'-methoxy-[1,10-biphenyl]-4-yl)-Nmethylbenzenesulfonamide
25% inhibition at 0.001 mM
3-phenyl-5-bromosalicylic acid
-
-
3-trifluoromethylcinnamic acid
-
IC50: 0.043 mM
3-[1-(4-hydroxyphenyl)-1H-1,2,3-triazol-4-yl]-phenol
substrate: estradiol-17beta, 17beta-HSD2
3-[1-(4-hydroxyphenyl)-1H-1,2,3-triazol-4-yl]phenol
-
-
3-[2-(5-chlorothiophen-2-yl)pyridin-4-yl]phenol
-
3-[3-(4-hydroxyphenyl)-1-methyl-1H-1,2,4-triazol-5-yl]phenol
-
-
3-[3-(4-hydroxyphenyl)-1-phenyl-1H-1,2,4-triazol-5-yl]phenol
-
-
3-[3-(4-hydroxyphenyl)isoxazol-5-yl]-phenol
substrate: estradiol-17beta, 17beta-HSD2
3-[4-(4-hydroxyphenyl)-1,3-oxazol-2-yl]phenol
substrate: estradiol-17beta, 17beta-HSD2
3-[4-(4-hydroxyphenyl)-1H-1,2,3-triazol-1-yl]-phenol
substrate: estradiol-17beta, 17beta-HSD2
3-[4-(4-hydroxyphenyl)-1H-1,2,3-triazol-1-yl]phenol
-
-
3-[4-(4-hydroxyphenyl)thiophen-2-yl]phenol
-
-
3-[5-(4-hydroxyphenyl)-1,3-oxazol-2-yl]-phenol
substrate: estradiol-17beta, 17beta-HSD2, very good selectivity, high cell permeability and medium CaCo-2 permeability
3-[5-(4-hydroxyphenyl)-1-methyl-1H-1,2,4-triazol-3-yl]phenol
-
-
3-[5-(4-hydroxyphenyl)-1-phenyl-1H-1,2,4-triazol-3-yl]phenol
-
-
3-[5-(4-hydroxyphenyl)thiophen-2-yl]phenol
-
-
3-[5-(4-hydroxyphenyl)thiophen-3-yl]phenol
-
-
3alpha-hydroxy-3beta-([4-[(2-methoxy-4-methylphenyl)methyl]piperazin-1-yl]methyl)-androstan-17-one
-
-
3alpha-hydroxy-3beta-([4-[(3-methoxy-4-methylphenyl)methyl]piperazin-1-yl]methyl)-androstan-17-one
-
-
3alpha-hydroxy-3beta-([4-[(3-methoxy-4-methylphenyl)methyl]piperazin-1-yl]methyl)androstan-17-one
0.1 mM, 12.5% inhibition in the reaction with allopregnanolone. 0.3 mM, 31.0% inhibition in the reaction with 17beta-estradiol
3alpha-hydroxy-3beta-([4-[(3-methoxyphenyl)methyl]piperazin-1-yl]methyl)-16,16-dimethylandrostan-17-one
0.1 mM, 11.1% inhibition in the reaction with allopregnanolone. 0.3 mM, 24.6% inhibition in the reaction with 17beta-estradiol
3alpha-hydroxy-3beta-([4-[(3-methoxyphenyl)methyl]piperazin-1-yl]methyl)-androstan-17-one
-
-
3alpha-hydroxy-3beta-([4-[(3-methoxyphenyl)methyl]piperazin-1-yl]methyl)androstan-17-one
0.1 mM, 14.7% inhibition in the reaction with allopregnanolone. 0.3 mM, 30.0% inhibition in the reaction with 17beta-estradiol
3alpha-hydroxy-3beta-([4-[(quinolin-3-yl)methyl]piperazin-1-yl]methyl)-androstan-17-one
-
-
3alpha-hydroxy-3beta-([4-[(quinolin-3-yl)methyl]piperazin-1-yl]methyl)androstan-17-one
0.1 mM, 15.2% inhibition in the reaction with allopregnanolone. 0.3 mM, 36.1% inhibition in the reaction with 17beta-estradiol
3alpha-hydroxy-3beta-[(4-[[3-methoxy-4-(trifluoromethyl)phenyl]methyl]piperazin-1-yl)methyl]-androstan-17-one
-
-
3beta-([4-[(3-methoxyphenyl)methyl]piperazin-1-yl]methyl)androstane-3alpha,17alpha-diol
0.1 mM, 41.7% inhibition in the reaction with allopregnanolone. 0.3 mM, 31.7% inhibition in the reaction with 17beta-estradiol
3beta-([4-[(3-methoxyphenyl)methyl]piperazin-1-yl]methyl)androstane-3alpha,17beta-diol
0.1 mM, no inhibition in the reaction with allopregnanolone. 0.3 mM, 13.7% inhibition in the reaction with 17beta-estradiol
3beta-hydroxy-5,16-androstadiene
-
-
3beta-hydroxy-5-androsten-16-one
-
-
3beta-[(4-[[3-methoxy-4-(trifluoromethyl)phenyl]methyl]piperazin-1-yl)methyl]-17alpha-pregn-20-yne-3alpha,17-diol
-
metabolic stability and selectivity of inhibition for 17beta-HSD10 over 17beta-HSD3
-
3beta-[(4-[[3-methoxy-4-(trifluoromethyl)phenyl]methyl]piperazin-1-yl)methyl]-androstane-3alpha,17alpha-diol
-
metabolic stability and selectivity of inhibition for 17beta-HSD10 over 17beta-HSD3
3beta-[[4-(3,5-dimethylbenzoyl)piperazin-1-yl]methyl]-3alpha-hydroxyandrostan-17-one
3beta-[[4-(3-acetylbenzoyl)piperazin-1-yl]methyl]-3alpha-hydroxyandrostan-17-one
3beta-[[4-(4-benzoylbenzoyl)piperazin-1-yl]methyl]-3alpha-hydroxyandrostan-17-one
0.1 mM, 8.0% inhibition in the reaction with allopregnanolone. 0.3 mM, 58.8% inhibition in the reaction with 17beta-estradiol
3beta-[[4-([1,1'-biphenyl]-4-carbonyl)piperazin-1-yl]methyl]-3?-hydroxyandrostan-17-one
0.1 mM, 19.3% inhibition in the reaction with allopregnanolone. 0.3 mM, 29.4% inhibition in the reaction with 17beta-estradiol
3beta-[[4-([1,1'-biphenyl]-4-carbonyl)piperazin-1-yl]methyl]-3alpha-hydroxyandrostan-17-one
-
-
4',5,7-trihydroxy-flavanone
-
-
4',5,7-trihydroxy-flavone
-
IC50: 0.0003 mM
4',5,7-trihydroxy-isoflavone
-
IC50: 0.001 mM
4',7-dihydroxy-isoflavone
-
IC50: 0.01 mM
4'-hydroxy-N-(3-hydroxybenzyl)-N-methylbiphenyl-3-carboxamide
4'-methoxy-N-(3-methoxybenzyl)-N-methylbiphenyl-3-carboxamide
-
4'-methoxy-N-(3-methoxyphenyl)-N-methyl-[1,1'-biphenyl]-4-sulfonamide
13% inhibition at 0.001 mM
4'-methoxy-N-(3-methoxyphenyl)-N-methylbiphenyl-3-carboxamide
-
4-(3'-ethyl-4'-hydroxy-3-methyl-biphenyl)-4-oxo-N-pyridin-3-ylethyl-butyramide
15% inhibition at 0.001 mM
4-(3'-ethyl-4'-hydroxy-3-methyl-biphenyl)-4-oxo-N-pyridin-3-ylmethyl-butyramide
21% inhibition at 0.001 mM
4-(3'-ethyl-4'-hydroxy-biphenyl)-2,2-dimethyl-4-oxo-N-pyridin-3-ylethyl-butyramide
15% inhibition at 0.001 mM
4-(3'-ethyl-4'-hydroxy-biphenyl)-2,2-dimethyl-4-oxo-N-pyridin-3-ylmethyl-butyramide
38% inhibition at 0.001 mM
4-(3'-ethyl-4'-hydroxy-biphenyl)-4-oxo-N-(2-hydroxyethyl)-butyramide
23% inhibition at 0.001 mM
4-(3'-ethyl-4'-hydroxy-biphenyl)-4-oxo-N-pyridin-3-ylethyl-butyramide
17% inhibition at 0.001 mM
4-(3'-ethyl-4'-hydroxy-biphenyl)-4-oxo-N-pyridin-3-ylmethyl-butyramide
4-(3'-ethyl-4'-methoxy-biphenyl)-2,2-dimethyl-4-oxo-N-pyridin-3-ylmethyl-butyramide
17% inhibition at 0.001 mM
4-(4-[[3alpha-hydroxy-17-oxoandrostan-3beta-yl]methyl]piperazine-1-carbonyl)benzonitrile
-
-
4-(dimethylsulfamoyl)-N-(4-[[3alpha-hydroxy-17-oxoandrostan-beta?-yl]methyl]piperazin-1-yl)benzene-1-carbothioamide
0.1 mM, 13.3% inhibition in the reaction with allopregnanolone. 0.3 mM, 0.3% inhibition in the reaction with 17beta-estradiol
4-bromo-N-(3-fluorophenyl)benzenesulfonamide
-
4-chloro-N-(3-hydroxy-4-methylphenyl)benzenesulfonamide
45% inhibition at 0.02 mM
4-chloro-N-(3-hydroxyphenyl)-2,5-dimethylbenzenesulfonamide
-
4-chloro-N-(4-hydroxyphenyl)benzenesulfonamide
55% inhibition at 0.02 mM
4-chloro-N-(4-methoxyphenyl)benzenesulfonamide
-
4-chloro-N-[2-(hydroxymethyl)phenyl]benzenesulfonamide
-
4-fluoro-3-hydroxy-N-(3'-hydroxybiphenyl-3-yl)-N-methylbenzenesulfonamide
96% inhibition at 0.001 mM
4-fluoro-3-methoxy-N-(3'-methoxybiphenyl-3-yl)-N-methylbenzenesulfonamide
-
4-fluoro-N-[2-(1-hydroxyethyl)phenyl]benzenesulfonamide
-
4-hydroxychalcone
-
IC50: 0.016 mM
4-methylbenzylidene camphor
-
-
4-propanoylphenyl 3-(acetylamino)benzenesulfonate
67% inhibition at 0.02 mM
4-[5-(3-hydroxyphenyl)thiophen-2-yl]-2-methylphenol
-
-
4-[[(4-methoxy-2,5-dimethylphenyl)sulfonyl]amino]benzoic acid
-
4-[[3alpha-hydroxy-17-oxoandrostan-3beta-yl]methyl]-N-[[3-(trifluoromethyl)phenyl]methyl]piperazine-1-carbothioamide
-
-
5'-O-(10-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha-yl]-decanoyl)adenosine
-
IC50: 140 nM
5'-O-(11-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha-yl]-undecanoyl) adenosine
-
IC50: 310 nM
5'-O-(11-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha/beta-yl]-undecanoyl)adenosine
-
IC50: 90 nM
5'-O-(11-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'beta-yl]-undecanoyl)adenosine
-
IC50: 120 nM
5'-O-(12-[3',17'beta-(dihydroxy)-1',3',5'(10')-estratrien-16'alpha-yl]-dodecanoyl)adenosine
-
IC50: 1000 nM
5'-O-(6-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha/beta-yl]-hexanoyl)adenosine
-
IC50: 6900 nM
5'-O-(7-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha-yl]-heptanoyl)adenosine
-
IC50: 430 nM
5'-O-(8-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha-yl]-octanoyl)adenosine
-
IC50: 93 nM
5'-O-(9-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha-yl]-nonanoyl)adenosine
-
IC50: 52 nM
5,7-dihydroxy-4'-methoxy-flavone
-
-
5-(2-fluoro-3-methoxyphenyl)-N-(3-hydroxybenzyl)-N-methylthiophene-2-carboxamide
-
5-(2-fluoro-3-methoxyphenyl)-N-(3-methoxyphenyl)-N-methylthiophene-2-carboxamide
-
5-(2-fluoro-3-methoxyphenyl)-N-methyl-N-(3-methylphenyl)thiophene-2-carboxamide
-
5-(2-hydroxyphenyl)-N-(3-hydroxyphenyl)-N-methylthiophene-2-carboxamide
-
5-(2-methoxyphenyl)-N-(3-methoxyphenyl)-N-methylthiophene-2-carboxamide
-
5-(3-ethyl-4-hydroxyphenyl)-indan-1-one
5-(3-fluoro-4-hydroxyphenyl)-indan-1-one
5-(3-fluoro-4-methoxyphenyl)-indan-1-one
56% inhibition at 0.001 mM
5-(3-fluorophenyl)-N-(3-hydroxybenzyl)-N-methylthiophene-2-carboxamide
-
5-(3-fluorophenyl)-N-(3-methoxyphenyl)-N-methylthiophene-2-carboxamide
-
5-(4-cyanophenyl)-N-(3-hydroxybenzyl)-N-methylthiophene-2-carboxamide
-
5-(4-cyanophenyl)-N-(3-methoxyphenyl)-N-methylthiophene-2-carboxamide
5-(4-hydroxyphenyl)-indan-1-one
5-androstene-3beta,16beta-diol
-
-
6-(3-ethyl-4-hydroxyphenyl)-3,4-dihydro-2H-naphthalen-1-one
51% inhibition at 0.001 mM
6-(3-ethyl-4-methoxyphenyl)-3,4-dihydro-2H-naphthalen-1-one
71% inhibition at 0.001 mM
6-(4-hydroxy-phenyl)-3,4-dihydro-2H-naphthalen-1-one
89% inhibition at 0.001 mM
6-(4-hydroxyphenyl)naphthalen-1-ol
-
6-(hexylsulfanyl)estra-1(10),2,4-triene-3,17beta-diol
-
30% inhibition at 0.001 mM, reduction of estrone with NADH as cofactor
7-hydroxy-flavanone
-
IC50: 0.028 mM
7-hydroxy-flavone
-
IC50: 0.0009 mM
8-((13S,16S,17S)-3,17-Dihydroxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-16-yl)-octanoic acid 5-(6-amino-purin-9-yl)-3,4-dihydroxy-tetrahydro-furan-2-ylmethyl ester
-
IC50: 93 nM
9-((13S,16S,17S)-3,17-Dihydroxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-16-yl)-nonanoic acid 5-(6-amino-purin-9-yl)-3,4-dihydroxy-tetrahydro-furan-2-ylmethyl ester
-
IC50: 52 nM
9-(5-O-(9-[(16alpha,17alpha)-3,17-dihydroxyestra-1(10),2,4-trien-16-yl]nonanoyl)-alpha-L-arabinofuranosyl)-9H-purin-6-amine
-
shows key interactions with two different enzyme-binding sites, namely the substrate- and the cofactor-binding sites
arachidonic acid
-
0.018 mM, complete inhibition, oxidation of estradiol
Benzoic acid (13S,17R)-7-[10-(butyl-methyl-carbamoyl)-decyl]-17-ethynyl-17-hydroxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-3-yl ester
-
-
caffeic acid
-
18% inhibition at 0.05 mM
Cinnamic acid
-
IC50: 0.050 mM
coumarin-3-carboxylic acid
-
30% inhibition at 0.05 mM
coumestrol
-
IC50: 0.0002 mM
Cu2+
-
1 mM, 82% inhibition
enterolactone
-
0.05 mM, 84% inhibition
equilin
-
IC50: 0.0017 mM
genistein
-
0.05 mM, 59% inhibition
Glyoxal
-
40 mM, pH 8.5, t1/2: 29 h
gossypol
-
and derivatives of gossypol, competitive with respect to NAD+ in reverse reaction
indomethacin
specific inhibitor for AKR1C3
iodoacetamide
-
1 mM, 78% inhibition
linoleic acid
-
0.018 mM, 58% inhibition, oxidation of estradiol
linolenic acid
-
0.018 mM, 34% inhibition, oxidation of estradiol
medrogestone
-
although the inhibitor is not selective for the type 1 17beta-HSD, it is weakly active and has a mechanism that appears to be complex, it offers new possibilities in treatment of estrogen-dependent diseases
Mg2+
-
1 mM, 18% inhibition
N,4'-dimethyl-N-(3-methylphenyl)biphenyl-4-carboxamide
-
N,5-bis(3-hydroxyphenyl)-N-methylthiophene-2-carboxamide
33% inhibition
N,5-bis(3-methoxyphenyl)-N-methylthiophene-2-carboxamide
-
N-(2,1,3-benzothiadiazol-4-yl)-2-(pyrimidin-2-ylsulfanyl)acetamide
-
N-(2,1,3-benzothiadiazol-4-yl)-2-[(4-hydroxypyrimidin-2-yl)sulfanyl]acetamide
92% inhibition at 0.02 mM
N-(2,5-dimethoxyphenyl)-2,5-diethylbenzenesulfonamide
-
N-(2-hydroxyphenyl)-2-methyl-4-(trifluoromethyl)benzenesulfonamide
94% inhibition at 0.02 mM
N-(2-[[(2,3,5,6-tetramethylphenyl)sulfonyl]amino]phenyl)acetamide
-
N-(3-chloro-4-fluorophenyl)-4-fluorobenzenesulfonamide
45% inhibition at 0.02 mM
N-(3-chloro-4-hydroxyphenyl)-4-fluorobenzenesulfonamide
91% inhibition at 0.02 mM
N-(3-chlorophenyl)-4-fluorobenzenesulfonamide
-
N-(3-hydroxy-4-methylphenyl)-3-(trifluoromethyl)benzenesulfonamide
75% inhibition at 0.02 mM
N-(3-hydroxy-4-methylphenyl)-4-methoxybenzenesulfonamide
47% inhibition at 0.02 mM
N-(3-hydroxybenzyl)-5-(3-hydroxyphenyl)-N-methylthiophene-2-carboxamide
-
N-(3-hydroxybenzyl)-5-(4-hydroxyphenyl)-N-methylthiophene-2-carboxamide
-
N-(3-hydroxybenzyl)-5-(4-methoxyphenyl)-N-methylthiophene-2-carboxamide
-
N-(3-hydroxybenzyl)-N-methyl-5-(3-methylphenyl)thiophene-2-carboxamide
-
N-(3-hydroxyphenyl)-2,4,5-trimethylbenzenesulfonamide
47% inhibition at 0.02 mM
N-(3-hydroxyphenyl)-3'-methoxy-N-methyl-[1,1'-biphenyl]-4-sulfonamide
18% inhibition at 0.001 mM
N-(3-hydroxyphenyl)-4-methoxy-2,5-dimethylbenzenesulfonamide
85% inhibition at 0.02 mM
N-(3-hydroxyphenyl)-4-methoxy-2-methyl-5,6,7,8-tetrahydronaphthalene-1-sulfonamide
-
N-(3-hydroxyphenyl)-N,3'-dimethyl-[1,1'-biphenyl]-4-sulfonamide
22% inhibition at 0.001 mM
N-(3-hydroxyphenyl)-N-methyl-4-(thiophen-2-yl)benzenesulfonamide
31% inhibition at 0.001 mM
N-(3-hydroxyphenyl)benzenesulfonamide
-
N-(3-methoxybenzyl)-5-(3-methoxyphenyl)-N-methylthiophene-2-carboxamide
-
N-(3-methoxyphenyl)-N-methyl-4-(thiophen-2-yl)benzenesulfonamide
32% inhibition at 0.001 mM
N-(3-methoxyphenyl)-N-methyl-4-(thiophen-3-yl)benzenesulfonamide
23% inhibition at 0.001 mM
N-(3-methoxyphenyl)-N-methyl-5-(3-methylphenyl)thiophene-2-carboxamide
-
N-(4-chlorophenyl)-4-methoxy-2,5-dimethylbenzenesulfonamide
-
N-(4-hydroxy-5,6,7,8-tetrahydronaphthalen-1-yl)-4-methoxybenzenesulfonamide
-
N-(4-hydroxyphenyl)-2,4,6-trimethylbenzenesulfonamide
33% inhibition at 0.02 mM
N-(4-hydroxyphenyl)-2,5-dimethylbenzenesulfonamide
39% inhibition at 0.02 mM
N-(4-hydroxyphenyl)-N-methyl-4-(pyridin-3-yl)benzenesulfonamide
15% inhibition at 0.001 mM
N-(4-methoxyphenyl)-2,5-dimethylbenzenesulfonamide
-
N-(4-[[3alpha-hydroxy-17-oxoandrostan-3beta-yl]methyl]piperazin-1-yl)[3-(trifluoromethyl)phenyl]ethanethioamide
0.1 mM, 34.2% inhibition in the reaction with allopregnanolone. 0.3 mM, 8.5% inhibition in the reaction with 17beta-estradiol
N-(5-chloro-2-hydroxyphenyl)-4-fluoro-3-methylbenzenesulfonamide
44% inhibition at 0.02 mM
N-(5-chloro-2-methylphenyl)-4-fluorobenzenesulfonamide
-
N-butyl-6-[[(6beta,17beta)-17-hydroxyestra-1(10),2,4-trien-6-yl]sulfanyl]-N-methylhexanamide
-
38% inhibition at 0.001 mM, reduction of estrone with NADH as cofactor
N-butyl-6-[[(6beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-6-yl]oxy]-N-methylhexanamide
-
73% inhibition at 0.001 mM, IC50: 0.0008 mM, reduction of estrone with NADH as cofactor
N-butyl-6-[[(6beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-6-yl]sulfanyl]-N-methylhexanamide
-
92% inhibition at 0.001 mM, IC50: 0.00016 mM, reduction of estrone with NADH as cofactor
N-decyl-N-[(4aR,6aS,7S)-1,4a,6a-trimethyl-2-oxohexadecahydro-1H-indeno[5,4-f]quinolin-7-yl]formamide
-
N-decyl-N-[(4aR,6aS,7S)-4a,6a-dimethyl-2-oxohexadecahydro-1H-indeno[5,4-f]quinolin-7-yl]formamide
-
N-ethyl-4-[[3alpha-hydroxy-17-oxoandrostan-3beta-yl]methyl]-N-methylpiperazine-1-sulfonamide
N-methyl-N,5-bis(3-methylphenyl)thiophene-2-carboxamide
-
N-n-butyl-N-methyl-11-(16'a-bromo-3',17'b-dihydroxyestra-1',3',5'(10')-trien-7'a-yl)undecanamide
-
-
N-n-butyl-N-methyl-11-(16'a-chloro-3',17'a-dihydroxyestra-1',3',5'(10')-trien-7'a-yl)undecanamide
-
-
N-n-butyl-N-methyl-11-(16'a-chloro-3',17'b-dihydroxyestra-1',3',5'(10')-trien-7'a-yl)undecanamide
-
-
N-n-butyl-N-methyl-11-(16'a-fluoro-3',17'a-dihydroxyestra-1',3',5'(10')-trien-7'a-yl)undecanamide
-
-
N-n-butyl-N-methyl-11-(16'a-fluoro-3',17'b-dihydroxyestra-1',3',5'(10')-trien-7'a-yl)undecanamide
-
-
N-n-butyl-N-methyl-11-(16'a-iodo-3',17'b-dihydroxyestra-1',3',5'(10')-trien-7'a-yl)undecanamide
-
-
N-n-Butyl-N-methyl-11-(3,17b-dihydroxyestra-1,3,5(10)-trien-7a-yl)undecanamide
-
-
N-nonyl-N-[(4aR,6aS,7S)-1,4a,6a-trimethyl-2-oxohexadecahydro-1H-indeno[5,4-f]quinolin-7-yl]formamide
-
N-[4-(dimethylsulfamoyl)phenyl]-4-[[3alpha-hydroxy-17-oxoandrostan-3beta-yl]methyl]piperazine-1-carbothioamide
-
-
N-[[5-(2,5-dichlorophenyl)furan-2-yl]methyl]-2H-tetrazol-5-amine
71% inhibition at 0.02 mM
NADP+
-
strong inhibitor of NAD+-linked activity
nomegestrol acetate
-
although the inhibitor is not selective for the type 1 17beta-HSD, it is weakly active and has a mechanism that appears to be complex, it offers new possibilities in treatment of estrogen-dependent diseases
oleic acid
-
0.018 mM, complete inhibition, oxidation of estradiol
palm oil carotenoids
-
0.0001 mM, significant inhibition of the conversion of estradiol to estrone in the MCF-7 cell line
-
PCMB
-
1 mM, complete inhibition
Phenylglyoxal
-
40 mM, pH 8.5, t1/2: 0.33 h
S-[(7R,10R,13S,17R)-10,13-dimethyl-3,5'-dioxo-1,2,3,4',5',6,7,8,9,10,11,12,13,14,15,16-hexadecahydro-3'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-7-yl] ethanethioate
-
0.003 mM, 57% inhibition, substrate: 4-androstene-3,17-dione
tibolone
-
although the inhibitor is not selective for the type 1 17beta-HSD, it is weakly active and has a mechanism that appears to be complex, it offers new possibilities in treatment of estrogen-dependent diseases
vitamin D3
-
inhibits reductive activity in HCT8 and LoVo cells
Zn2+
-
1 mM, 33% inhibition
[6-(3,4-dihydroxyphenyl)pyridin-2-yl]-(4-fluoro-3-hydroxyphenyl)methanone
a potent nonsteroidal inhibitor, binding structure, overview
[[4-(4-benzoylbenzoyl)piperazin-1-yl]methyl]-3alpha-hydroxyandrostan-17-one
-
-
(6aS)-2-hydroxy-6a-methyl-N-(2-pyridin-3-ylethyl)-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-9-carboxamide
-
(6aS)-2-hydroxy-6a-methyl-N-(2-pyridin-3-ylethyl)-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-9-carboxamide
0.01 mM, 99% inhibition, IC50: 0.0003 mM
(6aS)-2-hydroxy-6a-methyl-N-(pyridin-2-ylmethyl)-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-9-carboxamide
-
(6aS)-2-hydroxy-6a-methyl-N-(pyridin-2-ylmethyl)-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-9-carboxamide
0.01 mM, 93% inhibition, IC50: 0.00088 mM
(6aS)-2-hydroxy-6a-methyl-N-(pyridin-3-ylmethyl)-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-9-carboxamide
-
(6aS)-2-hydroxy-6a-methyl-N-(pyridin-3-ylmethyl)-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-9-carboxamide
0.01 mM, 92% inhibition, IC50: 0.00078 mM
1-[5-(3'-hydroxybiphenyl-3-yl)-2-thienyl]ethanone
0.001 mM, 10 min, 22% inhibition
1-[5-(3'-hydroxybiphenyl-3-yl)-2-thienyl]ethanone
0.001 mM, 10 min, 23% inhibition
1-[5-(3'-Hydroxybiphenyl-4-yl)-2-thienyl]ethanone
0.001 mM, 10 min, 10% inhibition
1-[5-(3'-Hydroxybiphenyl-4-yl)-2-thienyl]ethanone
0.001 mM, 10 min, 38% inhibition
3'-(1-benzothien-2-yl)biphenyl-3-ol
0.001 mM, 10 min, 39% inhibition
3'-(1-benzothien-2-yl)biphenyl-3-ol
0.001 mM, 10 min, 49% inhibition
3'-(2-thienyl)biphenyl-3-ol
0.001 mM, 10 min, 40% inhibition
3'-(2-thienyl)biphenyl-3-ol
0.001 mM, 10 min, 48% inhibition
3'-(5-chloro-2-thienyl)biphenyl-3-ol
0.001 mM, 10 min, 31% inhibition
3'-(5-chloro-2-thienyl)biphenyl-3-ol
0.001 mM, 10 min, 71% inhibition
3'-(5-methyl-2-thienyl)biphenyl-3-ol
0.001 mM, 10 min, 32% inhibition
3'-(5-methyl-2-thienyl)biphenyl-3-ol
0.001 mM, 10 min, 36% inhibition
3-benzyl-2-(2-bromo-3,4,5-trimethoxyphenyl)-8-hydroxy[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
0.001 mM, 95% inhibition
3-benzyl-2-(2-bromo-3,4,5-trimethoxyphenyl)-8-hydroxy[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
87% inhibition at 100 nM, 95% inhibition at 0.001 mM. IC50: 5 nM
3-benzyl-8-hydroxy-2-(3,4,5-trimethoxyphenyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
94% inhibition at 100 nM, 99% inhibition at 0.001 mM. IC50: 5 nM
3-benzyl-8-hydroxy-2-(3,4,5-trimethoxyphenyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
0.001 mM, 99% inhibition
3-[2-(2-thienyl)pyridin-4-yl]phenol
0.001 mM, 10 min, 33% inhibition
3-[2-(2-thienyl)pyridin-4-yl]phenol
0.001 mM, 10 min, 62% inhibition
3-[2-(5-chloro-2-thienyl)pyridin-4-yl]phenol
0.001 mM, 10 min, 39% inhibition
3-[2-(5-chloro-2-thienyl)pyridin-4-yl]phenol
0.001 mM, 10 min, 63% inhibition
3-[4-(5-chloro-2-thienyl)pyridin-2-yl]phenol
0.001 mM, 10 min, 25% inhibition
3-[4-(5-chloro-2-thienyl)pyridin-2-yl]phenol
0.001 mM, 10 min, 61% inhibition
3-[5-(5-chloro-2-thienyl)pyridin-3-yl]phenol
0.001 mM, 10 min, 40% inhibition
3-[5-(5-chloro-2-thienyl)pyridin-3-yl]phenol
0.001 mM, 10 min, 46% inhibition
3-[6-(5-chloro-2-thienyl)pyridin-2-yl]phenol
0.001 mM, 10 min, 21% inhibition
3-[6-(5-chloro-2-thienyl)pyridin-2-yl]phenol
0.001 mM, 10 min, 40% inhibition
4'-(2-thienyl)biphenyl-3-ol
0.001 mM, 10 min, 22% inhibition
4'-(2-thienyl)biphenyl-3-ol
0.001 mM, 10 min, 36% inhibition
4'-(3-thienyl)biphenyl-3-ol
0.001 mM, 10 min, 36% inhibition
4'-(3-thienyl)biphenyl-3-ol
0.001 mM, 10 min, 41% inhibition
4'-(5-chloro-2-thienyl)biphenyl-3-ol
-
4'-(5-chloro-2-thienyl)biphenyl-3-ol
0.001 mM, 10 min, 48% inhibition
4'-(6-methoxypyridin-3-yl)biphenyl-3-ol
0.001 mM, 10 min, 35% inhibition
4'-(6-methoxypyridin-3-yl)biphenyl-3-ol
0.001 mM, 10 min, 58% inhibition
6-(3-hydroxyphenyl)-2-naphthol
0.0001 mM, 91% inhibition, substrate: estrone
6-(3-hydroxyphenyl)-2-naphthol
94% inhibition at 0.001 mM
EM-1745
strong competitive inhibitor, inhibition reversible, 50% inhibition at 52 nM
EM-1745
bisubstrate inhibitor of 17beta-HSD1
estrone
substrate inhibition
estrone
0.001 mM, 85% inhibition
N-butyl-6-[[(6beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-6-yl]sulfanyl]-N-methylhexanamide
-
N-butyl-6-[[(6beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-6-yl]sulfanyl]-N-methylhexanamide
EM-678
N-ethylmaleimide
irreversible inhibition
N-ethylmaleimide
irreversible inhibition of 17beta-HSD1, preincubation with NADPH protects from inhibition
(10R,13S,17R)-10,13-dimethyl-1,6,7,8,9,10,11,12,13,14,15,16-dodecahydro-3'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-3,5'(2H,4'H)-dione
-
0.003 mM, 61% inhibition, substrate: 4-androstene-3,17-dione
(10R,13S,17R)-10,13-dimethyl-1,6,7,8,9,10,11,12,13,14,15,16-dodecahydro-3'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-3,5'(2H,4'H)-dione
-
0.003 mM, 63% inhibition, substrate: 4-androstene-3,17-dione
1-(3'-ethyl-4'-hydroxy-biphenyl-4-yl)-ethanone
37°C, 0.01 mM, 51% inhibition, substrate: estradiol-17beta, 7beta-HSD type 2
1-(3'-ethyl-4'-hydroxy-biphenyl-4-yl)-ethanone
73% inhibition at 0.001 mM
3'-hydroxy-N-(3-hydroxyphenyl)-N-methylbiphenyl-4-carboxamide
-
3'-hydroxy-N-(3-hydroxyphenyl)-N-methylbiphenyl-4-carboxamide
13% inhibition at 0.001 mM
3,3'-(1H-1,2,3-triazole-1,4-diyl)diphenol
-
-
3,3'-(1H-1,2,3-triazole-1,4-diyl)diphenol
-
17% inhibition at 0.001 mM
3beta-[[4-(3,5-dimethylbenzoyl)piperazin-1-yl]methyl]-3alpha-hydroxyandrostan-17-one
-
-
3beta-[[4-(3,5-dimethylbenzoyl)piperazin-1-yl]methyl]-3alpha-hydroxyandrostan-17-one
0.1 mM, 1.5% inhibition in the reaction with allopregnanolone
3beta-[[4-(3-acetylbenzoyl)piperazin-1-yl]methyl]-3alpha-hydroxyandrostan-17-one
-
-
3beta-[[4-(3-acetylbenzoyl)piperazin-1-yl]methyl]-3alpha-hydroxyandrostan-17-one
0.1 mM, 5.0% inhibition in the reaction with allopregnanolone
4'-hydroxy-N-(3-hydroxybenzyl)-N-methylbiphenyl-3-carboxamide
-
4'-hydroxy-N-(3-hydroxybenzyl)-N-methylbiphenyl-3-carboxamide
-
4-(3'-ethyl-4'-hydroxy-biphenyl)-4-oxo-N-pyridin-3-ylmethyl-butyramide
37°C, 0.01 mM, 12% inhibition, substrate: estradiol-17beta, 7beta-HSD type 2
4-(3'-ethyl-4'-hydroxy-biphenyl)-4-oxo-N-pyridin-3-ylmethyl-butyramide
24% inhibition at 0.001 mM
5-(3-ethyl-4-hydroxyphenyl)-indan-1-one
37°C, 0.01 mM, 48% inhibition, substrate: estradiol-17beta, 7beta-HSD type 2
5-(3-ethyl-4-hydroxyphenyl)-indan-1-one
86% inhibition at 0.001 mM
5-(3-fluoro-4-hydroxyphenyl)-indan-1-one
75% inhibition at 0.001 mM
5-(3-fluoro-4-hydroxyphenyl)-indan-1-one
37°C, 0.01 mM, 24% inhibition, substrate: estradiol-17beta, 7beta-HSD type 2
5-(4-cyanophenyl)-N-(3-methoxyphenyl)-N-methylthiophene-2-carboxamide
-
5-(4-cyanophenyl)-N-(3-methoxyphenyl)-N-methylthiophene-2-carboxamide
48% inhibition
5-(4-hydroxyphenyl)-indan-1-one
37°C, 0.01 mM, 17% inhibition, substrate: estradiol-17beta, 7beta-HSD type 2
5-(4-hydroxyphenyl)-indan-1-one
81% inhibition at 0.001 mM
cholest-4-ene-3,6-dione
cholest-4-ene-3,6-dione arrests the enzymatic conversion of estrone to 17-beta estradiol, by inhibiting AKR1C3 in intact MCF-7 cells. It can be used as a molecular scaffold for further development of l small-molecules with better specificity towards AKR1C3
cholest-4-ene-3,6-dione
the inhibitor occupies the binding region of AKR1C3 with almost similar orientation as indomethacin, thereby acting as an antagonistic agent for AKR1C3. It induces inhibition of AKR1C3 and cell death in MCF-7 cells. IT can be used as a molecular scaffold for development of novel small-molecules with better specificity towards AKR1C3
diethylstilbestrol
-
-
diethylstilbestrol
-
strong inhibition
diethylstilbestrol
-
oxidation of estradiol
EM-139
-
-
EM-139
-
antigen, dual-site inhibitor
estrone
-
-
estrone
-
oxidation of estradiol
estrone
-
92% inhibition at 0.001 mM, IC50: 0.00009 mM
estrone
-
IC50: 600-810 nM, depending on assay method
N-ethyl-4-[[3alpha-hydroxy-17-oxoandrostan-3beta-yl]methyl]-N-methylpiperazine-1-sulfonamide
-
-
N-ethyl-4-[[3alpha-hydroxy-17-oxoandrostan-3beta-yl]methyl]-N-methylpiperazine-1-sulfonamide
0.1 mM, no inhibition in the reaction with allopregnanolone. 0.3 mM, 10.2% inhibition in the reaction with 17beta-estradiol
additional information
not inhibited by 2-hydroxy-6-(3-hydroxyphenyl)-N-pyridin-2-yl-1-naphthamide and 2-hydroxy-6-(3-hydroxyphenyl)-N-(pyrimidin-2-yl)-1-naphthamide
-
additional information
fused 16beta,17beta-oxazinone-estradiol derivatives act as a family of non-estrogenic 17beta-hydroxysteroid dehydrogenase type 1 inhibitors, activities in T-47D breast cancer cells, molecular docking, structure-activity relationships, overview
-
additional information
inhibitory effects of 13-epimeric estrones, D-secooxime and D-secoalcohol estrone compounds on placental enzyme 17beta-HSD1
-
additional information
synthesis, physicochemical properties, and biological evaluation of novel N-methylsulfonamide and retro-N-methylsulfonamide derivatives as 17beta-HSD2 (the isoenzyme responsible of the reverse reaction) inhibitors showing high potency with a good selectivity toward 17beta-HSD1, and a likely good in vitro ADME profile, overview. No inhibition by 9b, 9c, 9e, 9f, 9g, 9h, 9k, 9o, and 10a
-
additional information
synthesis, physicochemical properties, and biological evaluation of novel N-methylsulfonamide and retro-N-methylsulfonamide derivatives as 17beta-HSD2 (the isoenzyme responsible of the reverse reaction) inhibitors showing high potency with a good selectivity toward 17beta-HSD1, and a likely good in vitro ADME profile, overview. No inhibition by 9b, 9c, 9e, 9f, 9g, 9h, 9k, 9o, and 10a
-
additional information
the enzyme shows sensitivity towards sulfhydryl modifying chemicals. 17beta-HSD1 is irreversibly inhibited by the sulfhydrylmodifying agents N-ethylmaleimide and dithiocarbamates. Preincubation with increasing concentrations of NADPH protects 17beta-HSD1 from inhibition by these chemicals
-
additional information
17beta-HSD1 and 17beta-HSD2 inhibitor structures and their biological activities are reviewed
-
additional information
17beta-HSD1 and 17beta-HSD2 inhibitor structures and their biological activities are reviewed
-
additional information
the status of inhibitors against 17beta-hydroxysteroid dehydrogenases 1 is reviewed
-
additional information
the status of inhibitors against 17beta-hydroxysteroid dehydrogenases 1 is reviewed
-
additional information
-
activity with estradiol-17beta is not inhibited by high concentrations of C19-steroids or C21-steroids
-
additional information
-
steroids which inhibit conversion of estrone to estradiol in normal breast tissue fail to do so when added to growing monolayers in the breast cancer cell lines T47D and MCF-7
-
additional information
-
modulation of local synthesis of estradiol is one potential mechanism through which genistein, enterolactone and enterodiol may protect against breast cancer
-
additional information
-
not inhibited by 1-(4'-methoxy-biphenyl-4-yl)-ethanone, 1-(4-benzo[1,3]dioxol-5-yl-phenyl)-ethanone, 1-(3'-ethyl-4'-methoxy-biphenyl-4-yl)-ethanone, 1-(4'-methoxy-2'-methyl-biphenyl-4-yl)-ethanone, 1-(4'-methoxy-2-methyl-biphenyl-4-yl)-ethanone, 1-(4'-hydroxy-2-methyl-biphenyl-4-yl)-ethanone, 1-(7-methoxy-9H-fluoren-2-yl)-ethanone, 5-(4-methoxyphenyl)-indan-1-one, 5-(3-ethyl-4-methoxyphenyl)-indan-1-one, 2,3-dihydro-5-phenylinden-1-one, 6-(4-methoxy-phenyl)-3,4-dihydro-2H-naphthalen-1-one, 4-(3'-ethyl-4'-hydroxy-biphenyl)-4-oxo-N-pyridin-2-ylmethyl-butyramide, 2-[5-(3-ethyl-4-hydroxyphenyl)-1-oxo-indan-2-yl]-N-pyridin-2-ylmethyl-acetamide, and 2-[5-(3-ethyl-4-hydroxyphenyl)-1-oxo-indan-2-yl]-N-(5-methyl-pyrazin-2-ylmethyl)-acetamide
-
additional information
not inhibited by 1-(4'-methoxy-biphenyl-4-yl)-ethanone, 1-(4-benzo[1,3]dioxol-5-yl-phenyl)-ethanone, 1-(3'-ethyl-4'-methoxy-biphenyl-4-yl)-ethanone, 1-(4'-methoxy-2'-methyl-biphenyl-4-yl)-ethanone, 1-(4'-methoxy-2-methyl-biphenyl-4-yl)-ethanone, 1-(4'-hydroxy-2-methyl-biphenyl-4-yl)-ethanone, 1-(7-methoxy-9H-fluoren-2-yl)-ethanone, 5-(4-methoxyphenyl)-indan-1-one, 5-(3-ethyl-4-methoxyphenyl)-indan-1-one, 2,3-dihydro-5-phenylinden-1-one, 6-(4-methoxy-phenyl)-3,4-dihydro-2H-naphthalen-1-one, 4-(3'-ethyl-4'-hydroxy-biphenyl)-4-oxo-N-pyridin-2-ylmethyl-butyramide, 2-[5-(3-ethyl-4-hydroxyphenyl)-1-oxo-indan-2-yl]-N-pyridin-2-ylmethyl-acetamide, and 2-[5-(3-ethyl-4-hydroxyphenyl)-1-oxo-indan-2-yl]-N-(5-methyl-pyrazin-2-ylmethyl)-acetamide
-
additional information
-
not inhibited by 3,3'-(1-methyl-1H-1,2,4-triazole-3,5-diyl)diphenol, 3-[5-(4-hydroxyphenyl)-1-methyl-1H-1,2,4-triazol-3-yl]phenol, 3-[3-(4-hydroxyphenyl)-1-methyl-1H-1,2,4-triazol-5-yl]phenol, 3,3'-(1-phenyl-1H-1,2,4-triazole-3,5-diyl)diphenol, 3-[5-(4-hydroxyphenyl)-1-phenyl-1H-1,2,4-triazol-3-yl]phenol, and 3-[3-(4-hydroxyphenyl)-1-phenyl-1H-1,2,4-triazol-5-yl]phenol
-
additional information
-
design of a series of estradiol-derivatives from potent inhibitor 16beta-(m-carbamoylbenzyl)-E2 to eliminate estrogenic activity, evaluation as 17beta-HSD1 inhibitors, and their proliferative (estrogenic) activity on estrogen-sensitive cells, structure-activity relationship study, overview
-
additional information
design of inhibitors displaying h17beta-HSD2 inhibitory activity and selectivity toward h17beta-HSD1. No inhibition by 5-(4-cyanophenyl)-N-(3-hydroxybenzyl)-N-methylthiophene-2-carboxamide
-
additional information
ligand-based pharmacophore models for 17beta-HSD2 inhibitors are constructed and employed for virtual screening, structure-activity relationships, overview. No inhibition by 18, 25, 26, 27, 28, 33, 34, 36, 37, 38, 41, 42, 43, 44, 45, and 47
-
additional information
synthesis, physicochemical properties, and biological evaluation of novel N-methylsulfonamide and retro-N-methylsulfonamide derivatives as 17beta-HSD2 inhibitors showing high potency with a good selectivity toward 17beta-HSD1 (the isoenzyme responsible of the reverse reaction), and a likely good in vitro ADME profile, overview
-
additional information
synthesis, physicochemical properties, and biological evaluation of novel N-methylsulfonamide and retro-N-methylsulfonamide derivatives as 17beta-HSD2 inhibitors showing high potency with a good selectivity toward 17beta-HSD1 (the isoenzyme responsible of the reverse reaction), and a likely good in vitro ADME profile, overview
-
additional information
17beta-HSD1 and 17beta-HSD2 inhibitor structures and their biological activities are reviewed. Dual 17beta-HSD1/STS inhibitors and inhibitors are covered
-
additional information
17beta-HSD1 and 17beta-HSD2 inhibitor structures and their biological activities are reviewed. Dual 17beta-HSD1/STS inhibitors and inhibitors are covered
-
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17beta-estradiol 17-dehydrogenase deficiency
Deleterious missense mutations and silent polymorphism in the human 17beta-hydroxysteroid dehydrogenase 3 gene (HSD17B3).
17beta-estradiol 17-dehydrogenase deficiency
Hydroxysteroid (17?) dehydrogenase 12 is essential for metabolic homeostasis in adult mice.
17beta-estradiol 17-dehydrogenase deficiency
Stromal cells of endometriosis fail to produce paracrine factors that induce epithelial 17beta-hydroxysteroid dehydrogenase type 2 gene and its transcriptional regulator Sp1: a mechanism for defective estradiol metabolism.
3(or 17)beta-hydroxysteroid dehydrogenase deficiency
3beta-hydroxysteroid dehydrogenase/delta5-->4-isomerase activity associated with the human 17beta-hydroxysteroid dehydrogenase type 2 isoform.
Adenocarcinoma
The Expression of HSD17B12 Is Associated with COX-2 Expression and Is Increased in High-Grade Epithelial Ovarian Cancer.
Adenoma
17Beta-hydroxysteroid dehydrogenase type 1, 2, 3, and 4 expression and enzyme activity in human anterior pituitary adenomas.
Adenomyosis
Adenomyosis: the pathophysiology of an oestrogen-dependent disease.
Adrenal Insufficiency
Four patients with D-bifunctional protein (DBP) deficiency: Expanding the phenotypic spectrum of a highly variable disease.
Adrenocortical Carcinoma
Overexpression of HSD17B4 exerts tumor suppressive function in adrenocortical carcinoma and is not associated with hormone excess.
Ataxia
Autonomous Purkinje cell axonal dystrophy causes ataxia in peroxisomal multifunctional protein-2 deficiency.
Ataxia
Mutations in the DBP-deficiency protein HSD17B4 cause ovarian dysgenesis, hearing loss, and ataxia of Perrault Syndrome.
Ataxia
Next generation sequencing with copy number variant detection expands the phenotypic spectrum of HSD17B4-deficiency.
Ataxia
Severe manifestation of Leber's hereditary optic neuropathy due to 11778G>A mtDNA mutation in a female with hypoestrogenism due to Perrault syndrome.
Breast Diseases
New development in intracrinology of breast carcinoma.
Breast Neoplasms
1-[(Benzofuran-2-yl)phenylmethyl]triazoles as steroidogenic inhibitors: synthesis and in vitro inhibition of human placental CYP19 aromatase.
Breast Neoplasms
17-beta-Hydroxysteroid dehydrogenase type 1: computational design of active site inhibitors targeted to the Rossmann fold.
Breast Neoplasms
17beta-hydroxysteroid dehydrogenase 14 affects estradiol levels in breast cancer cells and is a prognostic marker in estrogen receptor-positive breast cancer.
Breast Neoplasms
17Beta-hydroxysteroid dehydrogenase enzymes and breast cancer.
Breast Neoplasms
17Beta-hydroxysteroid dehydrogenase type 1 and type 2 in human breast carcinoma: a correlation to clinicopathological parameters.
Breast Neoplasms
17beta-hydroxysteroid dehydrogenase type 1 is an independent prognostic marker in breast cancer.
Breast Neoplasms
17beta-hydroxysteroid dehydrogenase Type 1, and not Type 12, is a target for endocrine therapy of hormone-dependent breast cancer.
Breast Neoplasms
17Beta-hydroxysteroid dehydrogenase type 12 in human breast carcinoma: a prognostic factor via potential regulation of fatty acid synthesis.
Breast Neoplasms
17ss-Hydroxysteroid dehydrogenase type 1 as predictor of tamoxifen response in premenopausal breast cancer.
Breast Neoplasms
A concerted, rational design of type 1 17beta-hydroxysteroid dehydrogenase inhibitors: estradiol-adenosine hybrids with high affinity.
Breast Neoplasms
A new polymorphism in the coding region of exon four in HSD17B2 in relation to risk of sporadic and hereditary breast cancer.
Breast Neoplasms
Abnormal expression of 17beta-hydroxysteroid dehydrogenases in breast cancer predicts late recurrence.
Breast Neoplasms
Acetylation targets HSD17B4 for degradation via the CMA pathway in response to estrone.
Breast Neoplasms
Analysis of 17beta-hydroxysteroid dehydrogenase types 5, 7, and 12 genetic sequence variants in breast cancer cases from French Canadian Families with high risk of breast and ovarian cancer.
Breast Neoplasms
Binary and ternary crystal structure analyses of a novel inhibitor with 17beta-HSD type 1: a lead compound for breast cancer therapy.
Breast Neoplasms
Dietary isoflavone intake, polymorphisms in the CYP17, CYP19, 17beta-HSD1, and SHBG genes, and risk of breast cancer in case-control studies in Japanese, Japanese Brazilians, and non-Japanese Brazilians.
Breast Neoplasms
DNA methylation marker to estimate the breast cancer cell fraction in DNA samples.
Breast Neoplasms
Effect of retinoic acid and palm oil carotenoids on oestrone sulphatase and oestradiol-17beta hydroxysteroid dehydrogenase activities in MCF-7 and MDA-MB-231 breast cancer cell lines.
Breast Neoplasms
Estradiol and estrone C-16 derivatives as inhibitors of type 1 17beta-hydroxysteroid dehydrogenase: blocking of ER+ breast cancer cell proliferation induced by estrone.
Breast Neoplasms
Evaluation of inhibitors for 17beta-hydroxysteroid dehydrogenase type 1 in vivo in immunodeficient mice inoculated with MCF-7 cells stably expressing the recombinant human enzyme.
Breast Neoplasms
Expression of 17beta-hydroxysteroid dehydrogenase type 2 and type 5 in breast cancer and adjacent non-malignant tissue: a correlation to clinicopathological parameters.
Breast Neoplasms
Expression of aromatase and 17beta-hydroxysteroid dehydrogenase types 1, 7 and 12 in breast cancer An immunocytochemical study.
Breast Neoplasms
Expression of COX-2 and steroid converting enzymes in breast cancer.
Breast Neoplasms
Gene-body hypermethylation of ATM in peripheral blood DNA of bilateral breast cancer patients.
Breast Neoplasms
Hormonal carcinogenesis.
Breast Neoplasms
Hormone replacement therapy and cancers: the biological roles of estrogen and progestin in tumorigenesis are different between the endometrium and breast.
Breast Neoplasms
Human hydroxysteroid (17-beta) dehydrogenase 1 expression enhances estrogen sensitivity of MCF-7 breast cancer cell xenografts.
Breast Neoplasms
Identification of Hydroxysteroid (17?) dehydrogenase type 12 (HSD17B12) as a CD8(+) T-cell-defined human tumor antigen of human carcinomas.
Breast Neoplasms
In vivo and in vitro expression of steroid-converting enzymes in human breast tumours: associations with interleukin-6.
Breast Neoplasms
Increased intratumoral androgens in human breast carcinoma following aromatase inhibitor exemestane treatment.
Breast Neoplasms
Interactions between exposure to polycyclic aromatic hydrocarbons and xenobiotic metabolism genes, and risk of breast cancer.
Breast Neoplasms
Multi-omics analyses identify HSD17B4 methylation-silencing as a predictive and response marker of HER2-positive breast cancer to HER2-directed therapy.
Breast Neoplasms
Mutation analysis and characterization of HSD17B2 sequence variants in breast cancer cases from French Canadian families with high risk of breast and ovarian cancer.
Breast Neoplasms
New development in intracrinology of breast carcinoma.
Breast Neoplasms
Pathological complete response of HER2-positive breast cancer to trastuzumab and chemotherapy can be predicted by HSD17B4 methylation.
Breast Neoplasms
PDGFRA, HSD17B4 and HMGB2 are potential therapeutic targets in polycystic ovarian syndrome and breast cancer.
Breast Neoplasms
Polymorphism Thr160Thr in SRD5A1, involved in the progesterone metabolism, modifies postmenopausal breast cancer risk associated with menopausal hormone therapy.
Breast Neoplasms
Predictive value of genetic analysis for pathological complete response to preoperative treatment in HER2 positive, HR negative early breast cancer (PASSION trial).
Breast Neoplasms
Progestins and cancer.
Breast Neoplasms
Ratio of 17HSD1 to 17HSD2 Protein Expression Predicts the Outcome of Tamoxifen Treatment in Postmenopausal Breast Cancer Patients.
Breast Neoplasms
Role of BRCA1, HSD17B1 and HSD17B2 methylation in breast cancer tissue.
Breast Neoplasms
Sex steroid-producing enzymes in human breast cancer.
Breast Neoplasms
Structure and function of 17beta-hydroxysteroid dehydrogenase type 1 and type 2.
Breast Neoplasms
Structure of the ternary complex of human 17beta-hydroxysteroid dehydrogenase type 1 with 3-hydroxyestra-1,3,5,7-tetraen-17-one (equilin) and NADP+.
Breast Neoplasms
The gene for 17 beta-hydroxysteroid dehydrogenase maps to human chromosome 17, bands q12-q21, and shows an RFLP with ScaI.
Breast Neoplasms
The regulation of hydroxysteroid 17?-dehydrogenase type 1 and 2 gene expression in breast cancer cell lines by estradiol, dihydrotestosterone, microRNAs, and genes related to breast cancer.
Breast Neoplasms
Type 5 17-hydroxysteroid dehydrogenase/prostaglandin F synthase (AKR1C3) inhibition and potential anti-proliferative activity of cholest-4-ene-3,6-dione in MCF-7 breast cancer cells.
Carcinoma
17? hydroxysteroid dehydrogenase type 12 (HSD17B12) is a marker of poor prognosis in ovarian carcinoma.
Carcinoma
17Beta-hydroxysteroid dehydrogenase type 1 and type 2 in human breast carcinoma: a correlation to clinicopathological parameters.
Carcinoma
17Beta-hydroxysteroid dehydrogenases in human endometrium and its disorders.
Carcinoma
Characteristics of a highly labile human type 5 17beta-hydroxysteroid dehydrogenase.
Carcinoma
High Expression of 17?-hydroxysteroid Dehydrogenase Type 2 is Associated with a Better Prognosis in Urothelial Carcinoma of the Urinary Tract.
Carcinoma
Identification of Hydroxysteroid (17?) dehydrogenase type 12 (HSD17B12) as a CD8(+) T-cell-defined human tumor antigen of human carcinomas.
Carcinoma
Immunological analysis of 17 beta-hydroxysteroid dehydrogenase in benign and malignant human breast tissue.
Carcinoma
Mefenamic acid enhances anticancer drug sensitivity via inhibition of aldo-keto reductase 1C enzyme activity.
Carcinoma
Overexpression of HSD17B4 exerts tumor suppressive function in adrenocortical carcinoma and is not associated with hormone excess.
Carcinoma
[Altered expression of the HSD17B4 gene in esophageal squamous cell carcinoma and loss of heterozygosity analysis]
Carcinoma, Ductal
17Beta-hydroxysteroid dehydrogenase type 1 and type 2 in human breast carcinoma: a correlation to clinicopathological parameters.
Carcinoma, Ductal
New development in intracrinology of breast carcinoma.
Carcinoma, Endometrioid
The analyses of 17beta-hydroxysteroid dehydrogenase isozymes in human endometrial hyperplasia and carcinoma.
Carcinoma, Hepatocellular
Association of Genetic Polymorphisms in HSD17B1, HSD17B2 and SHBG Genes with Hepatocellular Carcinoma Risk.
Carcinoma, Hepatocellular
NF-?B increased expression of 17?-hydroxysteroid dehydrogenase 4 promotes HepG2 proliferation via inactivating estradiol.
Carcinoma, Intraductal, Noninfiltrating
New development in intracrinology of breast carcinoma.
Carcinoma, Non-Small-Cell Lung
HSD17B4, ACAA1, and PXMP4 in Peroxisome Pathway Are Down-Regulated and Have Clinical Significance in Non-small Cell Lung Cancer.
Carcinoma, Ovarian Epithelial
The Expression of HSD17B12 Is Associated with COX-2 Expression and Is Increased in High-Grade Epithelial Ovarian Cancer.
Carcinoma, Small Cell
Overexpression of HSD17B4 exerts tumor suppressive function in adrenocortical carcinoma and is not associated with hormone excess.
Carcinoma, Squamous Cell
Identification of Hydroxysteroid (17?) dehydrogenase type 12 (HSD17B12) as a CD8(+) T-cell-defined human tumor antigen of human carcinomas.
Carcinoma, Squamous Cell
Intracellular regulation of 17 beta-hydroxysteroid dehydrogenase type 2 catalytic activity in A431 cells.
Carcinoma, Squamous Cell
Mefenamic acid enhances anticancer drug sensitivity via inhibition of aldo-keto reductase 1C enzyme activity.
Cerebellar Ataxia
Slowly progressive d-bifunctional protein deficiency with survival to adulthood diagnosed by whole-exome sequencing.
CHARGE Syndrome
Laser-capture micro dissection combined with next-generation sequencing analysis of cell type-specific deafness gene expression in the mouse cochlea.
Choriocarcinoma
Characterization of 17 beta-hydroxysteroid dehydrogenase type 1 in choriocarcinoma cells: regulation by basic fibroblast growth factor.
Choriocarcinoma
Endocrine disruption induced by organotin compounds; organotins function as a powerful agonist for nuclear receptors rather than an aromatase inhibitor.
Choriocarcinoma
Organotin compounds enhance 17beta-hydroxysteroid dehydrogenase type I activity in human choriocarcinoma JAr cells: potential promotion of 17beta-estradiol biosynthesis in human placenta.
Colonic Neoplasms
17Beta-hydroxysteroid dehydrogenase type 2: independent prognostic significance and evidence of estrogen protection in female patients with colon cancer.
Colonic Neoplasms
Developing antineoplastic agents that target peroxisomal enzymes: cytisine-linked isoflavonoids as inhibitors of hydroxysteroid 17-beta-dehydrogenase-4 (HSD17B4).
Colorectal Neoplasms
Functional genetic variant of HSD17B12 in the fatty acid biosynthesis pathway predicts the outcome of colorectal cancer.
Colorectal Neoplasms
Genetic variation in sex-steroid receptors and synthesizing enzymes and colorectal cancer risk in women.
Dengue
Very-long-chain fatty acid metabolic capacity of 17-beta-hydroxysteroid dehydrogenase type 12 (HSD17B12) promotes replication of hepatitis C virus and related flaviviruses.
Diabetes Mellitus
[Serum levels of 17-beta estradiol dehydrogenase in pregnancies complicated by diabetes mellitus]
Diabetes Mellitus, Type 2
An Integrative Phenotype-Genotype Approach Using Phenotypic Characteristics from the UAE National Diabetes Study Identifies HSD17B12 as a Candidate Gene for Obesity and Type 2 Diabetes.
Disorder of Sex Development, 46,XY
Deleterious missense mutations and silent polymorphism in the human 17beta-hydroxysteroid dehydrogenase 3 gene (HSD17B3).
Dyslipidemias
Role of dipeptidyl peptidase IV (DPP4) in the development of dyslipidemia: DPP4 contributes to the steroid metabolism pathway.
Endometrial Hyperplasia
The analyses of 17beta-hydroxysteroid dehydrogenase isozymes in human endometrial hyperplasia and carcinoma.
Endometrial Neoplasms
17Beta-hydroxysteroid dehydrogenases in human endometrium and its disorders.
Endometrial Neoplasms
Divergent effects of retinoic acids on the expression of ERalpha and 17beta-hydroxysteroid dehydrogenase type 2 in endometrial carcinoma cells (RL 95-2).
Endometrial Neoplasms
Failure of progestins to induce estradiol dehydrogenase activity in endometrial carcinoma, in vitro.
Endometrial Neoplasms
Hormone replacement therapy and cancers: the biological roles of estrogen and progestin in tumorigenesis are different between the endometrium and breast.
Endometrial Neoplasms
Menopausal endocrinology and management.
Endometrial Neoplasms
Progestins and cancer.
Endometrial Neoplasms
The analyses of 17beta-hydroxysteroid dehydrogenase isozymes in human endometrial hyperplasia and carcinoma.
Endometrial Neoplasms
The correlation between the response to progestogen treatment and the expression of progesterone receptor B and 17beta-hydroxysteroid dehydrogenase type 2 in human endometrial carcinoma.
Endometrial Neoplasms
[Studies on estradiol dehydrogenase activity in the human uterine endometrium]
Endometriosis
Adenomyosis: the pathophysiology of an oestrogen-dependent disease.
Endometriosis
Analysis of aromatase and 17beta-hydroxysteroid dehydrogenase type 2 messenger ribonucleic acid expression in deep endometriosis and eutopic endometrium using laser capture microdissection.
Endometriosis
Deficient 17beta-hydroxysteroid dehydrogenase type 2 expression in endometriosis: failure to metabolize 17beta-estradiol.
Endometriosis
Differential expression of genes in eutopic and ectopic endometrium from patients with ovarian endometriosis.
Endometriosis
Effects of progestins on local estradiol biosynthesis and action in the Z-12 endometriotic epithelial cell line.
Endometriosis
Estrogen biosynthesis in endometriosis: molecular basis and clinical relevance.
Endometriosis
Estrogen metabolizing enzymes in endometrium and endometriosis.
Endometriosis
Expression of 17beta-hydroxysteroid dehydrogenase type 2 in pelvic endometriosis.
Endometriosis
HSD3B2, HSD17B1, HSD17B2, ESR1, ESR2 and AR expression in infertile women with endometriosis.
Endometriosis
Induction of endometriosis in the marmoset monkey (Callithrix jacchus).
Endometriosis
Mechanisms of excessive estrogen formation in endometriosis.
Endometriosis
Role of aromatase in endometrial disease.
Endometriosis
Steroidogenic enzyme and key decidualization marker dysregulation in endometrial stromal cells from women with versus without endometriosis.
Endometriosis
Stromal cells of endometriosis fail to produce paracrine factors that induce epithelial 17beta-hydroxysteroid dehydrogenase type 2 gene and its transcriptional regulator Sp1: a mechanism for defective estradiol metabolism.
Esophageal Squamous Cell Carcinoma
[Altered expression of the HSD17B4 gene in esophageal squamous cell carcinoma and loss of heterozygosity analysis]
Flaviviridae Infections
Very-long-chain fatty acid metabolic capacity of 17-beta-hydroxysteroid dehydrogenase type 12 (HSD17B12) promotes replication of hepatitis C virus and related flaviviruses.
Hearing Loss
Laser-capture micro dissection combined with next-generation sequencing analysis of cell type-specific deafness gene expression in the mouse cochlea.
Hearing Loss
Mutations in the DBP-deficiency protein HSD17B4 cause ovarian dysgenesis, hearing loss, and ataxia of Perrault Syndrome.
Hearing Loss
Next generation sequencing with copy number variant detection expands the phenotypic spectrum of HSD17B4-deficiency.
Hearing Loss, Sensorineural
Four patients with D-bifunctional protein (DBP) deficiency: Expanding the phenotypic spectrum of a highly variable disease.
Hepatitis C
Very-long-chain fatty acid metabolic capacity of 17-beta-hydroxysteroid dehydrogenase type 12 (HSD17B12) promotes replication of hepatitis C virus and related flaviviruses.
Hydatidiform Mole
[Serum and tissue 17 beta hydroxysteroid dehydrogenase and estrogens in hydatidiform mole]
Hydatidiform Mole
[Serum levels of 17-beta estradiol dehydrogenase in pregnancies complicated by hydatidiform mole and in twin pregnancies]
Hypospadias
Fine mapping analysis confirms and strengthens linkage of four chromosomal regions in familial hypospadias.
Hypospadias
Lack of defects in androgen production in children with hypospadias.
Infertility
The hydroxysteroid (17?) dehydrogenase family gene HSD17B12 is involved in the prostaglandin synthesis pathway, the ovarian function, and regulation of fertility.
Infertility
Transgenic male mice expressing human hydroxysteroid dehydrogenase 2 indicate a role for the enzyme independent of its action on sex steroids.
Intellectual Disability
Severe manifestation of Leber's hereditary optic neuropathy due to 11778G>A mtDNA mutation in a female with hypoestrogenism due to Perrault syndrome.
Kallmann Syndrome
Laser-capture micro dissection combined with next-generation sequencing analysis of cell type-specific deafness gene expression in the mouse cochlea.
Leiomyoma
Adenomyosis: the pathophysiology of an oestrogen-dependent disease.
Leiomyoma
Increased expression of type I 17beta-hydroxysteroid dehydrogenase enhances in situ production of estradiol in uterine leiomyoma.
Leiomyoma
Polymorphisms in genes HSD17B1 and HSD17B2 and uterine leiomyoma risk in Chinese women.
Leukemia
T cell recognition of Moloney leukemia virus proteins. III. T cell proliferative responses against gp70 are associated with the production of a lymphokine inducing 20 alpha-hydroxysteroid dehydrogenase in splenic lymphocytes.
Liver Diseases, Alcoholic
Major differences exist in the function and tissue-specific expression of human aflatoxin B1 aldehyde reductase and the principal human aldo-keto reductase AKR1 family members.
Liver Neoplasms
17??hydroxysteroid dehydrogenase 4 induces liver cancer proliferation?associated genes via STAT3 activation.
Liver Neoplasms
AKR1C1-3, notably AKR1C3, are distinct biomarkers for liver cancer diagnosis and prognosis: Database mining in malignancies.
Liver Neoplasms
Comment on: Correlation between HSD17B4 expression in rat liver cancer tissues and inflammation or proliferation.
Liver Neoplasms
Correlation between HSD17B4 expression in rat liver cancer tissues and inflammation or proliferation.
Liver Neoplasms
NF-?B increased expression of 17?-hydroxysteroid dehydrogenase 4 promotes HepG2 proliferation via inactivating estradiol.
Lung Neoplasms
Altered expression of 17???hydroxysteroid dehydrogenase type 2 and its prognostic significance in non?small cell lung cancer.
Lung Neoplasms
HSD17B4, ACAA1, and PXMP4 in Peroxisome Pathway Are Down-Regulated and Have Clinical Significance in Non-small Cell Lung Cancer.
Lymphatic Metastasis
Expression of 17?-hydroxysteroid dehydrogenase type 2 is associated with some clinicopathological features in gastric cancer.
Lymphoma
Influence of genotype and the organ of origin on the subtype of T-cell in Moloney lymphomas induced by transfer of preleukemic cells from athymic and thymus-bearing mice.
Mandibulofacial Dysostosis
Laser-capture micro dissection combined with next-generation sequencing analysis of cell type-specific deafness gene expression in the mouse cochlea.
Mania
Polymorphisms in AKR1C4 and HSD3B2 and differences in serum DHEAS and progesterone are associated with paranoid ideation during mania or hypomania in bipolar disorder.
Megalencephaly
Four patients with D-bifunctional protein (DBP) deficiency: Expanding the phenotypic spectrum of a highly variable disease.
Muscle Hypotonia
Four patients with D-bifunctional protein (DBP) deficiency: Expanding the phenotypic spectrum of a highly variable disease.
Neoplasm Metastasis
Expression of 17?-hydroxysteroid dehydrogenase type 2 is associated with some clinicopathological features in gastric cancer.
Neoplasm Metastasis
High Expression of 17?-hydroxysteroid Dehydrogenase Type 2 is Associated with a Better Prognosis in Urothelial Carcinoma of the Urinary Tract.
Neoplasm Metastasis
Steroid-converting enzymes in human ovarian carcinomas.
Neoplasms
17? hydroxysteroid dehydrogenase type 12 (HSD17B12) is a marker of poor prognosis in ovarian carcinoma.
Neoplasms
17??hydroxysteroid dehydrogenase 4 induces liver cancer proliferation?associated genes via STAT3 activation.
Neoplasms
17Beta-hydroxysteroid dehydrogenase enzymes and breast cancer.
Neoplasms
17Beta-hydroxysteroid dehydrogenase type 1 and type 2 in human breast carcinoma: a correlation to clinicopathological parameters.
Neoplasms
17beta-hydroxysteroid dehydrogenase type 1 is an independent prognostic marker in breast cancer.
Neoplasms
17Beta-hydroxysteroid dehydrogenase type 1, 2, 3, and 4 expression and enzyme activity in human anterior pituitary adenomas.
Neoplasms
17Beta-hydroxysteroid dehydrogenase type 12 in human breast carcinoma: a prognostic factor via potential regulation of fatty acid synthesis.
Neoplasms
17ss-Hydroxysteroid dehydrogenase type 1 as predictor of tamoxifen response in premenopausal breast cancer.
Neoplasms
20 alpha-hydroxysteroid dehydrogenase activity in canine spontaneous neoplasms.
Neoplasms
A low carbohydrate, high protein diet suppresses intratumoral androgen synthesis and slows castration-resistant prostate tumor growth in mice.
Neoplasms
Altered expression of 17???hydroxysteroid dehydrogenase type 2 and its prognostic significance in non?small cell lung cancer.
Neoplasms
Alternative Acts: Oncogenic Splicing of Steroidogenic Enzymes in Prostate Cancer.
Neoplasms
Breast cancer DNA methylation profiles in cancer cells and tumor stroma: association with HER-2/neu status in primary breast cancer.
Neoplasms
Correlation between HSD17B4 expression in rat liver cancer tissues and inflammation or proliferation.
Neoplasms
Cytosol and nuclear estrogen and progestin receptors and 17 beta-hydroxysteroid dehydrogenase activity in non-diseased tissue and in benign and malignant tumors of the human ovary.
Neoplasms
Cytosolic 20 alpha-hydroxysteroid dehydrogenase activity in spontaneous neoplasms in the dog and cat.
Neoplasms
Developing antineoplastic agents that target peroxisomal enzymes: cytisine-linked isoflavonoids as inhibitors of hydroxysteroid 17-beta-dehydrogenase-4 (HSD17B4).
Neoplasms
Differential expression of 17beta-hydroxysteroid dehydrogenase isozyme genes in prostate cancer and noncancer tissues.
Neoplasms
DNA methylation marker to estimate the breast cancer cell fraction in DNA samples.
Neoplasms
Estradiol-adenosine hybrid compounds designed to inhibit type 1 17beta-hydroxysteroid dehydrogenase.
Neoplasms
Expression of 17?-hydroxysteroid dehydrogenase type 2 is associated with some clinicopathological features in gastric cancer.
Neoplasms
Expression of 17beta-hydroxysteroid dehydrogenase type 2 and type 5 in breast cancer and adjacent non-malignant tissue: a correlation to clinicopathological parameters.
Neoplasms
Expression of 17beta-hydroxysteroid dehydrogenases and other estrogen-metabolizing enzymes in different cancer cell lines.
Neoplasms
Expression of aromatase and 17beta-hydroxysteroid dehydrogenase types 1, 7 and 12 in breast cancer An immunocytochemical study.
Neoplasms
Functional silencing of HSD17B2 in prostate cancer promotes disease progression.
Neoplasms
Functional validation of metabolic genes that distinguish Gleason 3 from Gleason 4 prostate cancer foci.
Neoplasms
Gene expression of androgen metabolising enzymes in benign prostatic hyperplasia.
Neoplasms
High mRNA levels of 17?-hydroxysteroid dehydrogenase type 1 correlate with poor prognosis in endometrial cancer.
Neoplasms
Identification of a 17beta-hydroxysteroid dehydrogenase type 12 pseudogene as the source of a highly restricted BALB/c Meth A tumor rejection peptide.
Neoplasms
Identification of Hydroxysteroid (17?) dehydrogenase type 12 (HSD17B12) as a CD8(+) T-cell-defined human tumor antigen of human carcinomas.
Neoplasms
Immunological analysis of 17 beta-hydroxysteroid dehydrogenase in benign and malignant human breast tissue.
Neoplasms
In vivo and in vitro expression of steroid-converting enzymes in human breast tumours: associations with interleukin-6.
Neoplasms
Involvement of H-cadherin (CDH13) on 16q in the region of frequent deletion in ovarian cancer.
Neoplasms
Mammalian lignans and genistein decrease the activities of aromatase and 17beta-hydroxysteroid dehydrogenase in MCF-7 cells.
Neoplasms
Mefenamic acid enhances anticancer drug sensitivity via inhibition of aldo-keto reductase 1C enzyme activity.
Neoplasms
Multi-omics analyses identify HSD17B4 methylation-silencing as a predictive and response marker of HER2-positive breast cancer to HER2-directed therapy.
Neoplasms
NF-?B increased expression of 17?-hydroxysteroid dehydrogenase 4 promotes HepG2 proliferation via inactivating estradiol.
Neoplasms
Overexpression of HSD17B4 exerts tumor suppressive function in adrenocortical carcinoma and is not associated with hormone excess.
Neoplasms
Pathological complete response of HER2-positive breast cancer to trastuzumab and chemotherapy can be predicted by HSD17B4 methylation.
Neoplasms
Predictive value of genetic analysis for pathological complete response to preoperative treatment in HER2 positive, HR negative early breast cancer (PASSION trial).
Neoplasms
Quantitative analysis of the human AKR family members in cancer cell lines using the mTRAQ/MRM approach.
Neoplasms
Ratio of 17HSD1 to 17HSD2 Protein Expression Predicts the Outcome of Tamoxifen Treatment in Postmenopausal Breast Cancer Patients.
Neoplasms
Reductive 17beta-hydroxysteroid dehydrogenases in the sulfatase pathway: critical in the cell proliferation of breast cancer.
Neoplasms
Role of BRCA1, HSD17B1 and HSD17B2 methylation in breast cancer tissue.
Neoplasms
Steroid metabolism and steroid receptors in dimethylbenz(a)anthracene-induced rat mammary tumors.
Neoplasms
Steroid metabolism in normal mammary gland and in the dimethylbenzanthracene-induced mammary tumor of rats.
Neoplasms
Steroid-converting enzymes in human ovarian carcinomas.
Neoplasms
The Expression of HSD17B12 Is Associated with COX-2 Expression and Is Increased in High-Grade Epithelial Ovarian Cancer.
Neoplasms
The prognostic impact of lipid biosynthesis-associated markers, HSD17B2 and HMGCS2, in rectal cancer treated with neoadjuvant concurrent chemoradiotherapy.
Neoplasms
Unusual charge stabilization of NADP+ in 17beta-hydroxysteroid dehydrogenase.
Neoplasms
[Altered expression of the HSD17B4 gene in esophageal squamous cell carcinoma and loss of heterozygosity analysis]
Nephritis, Hereditary
Laser-capture micro dissection combined with next-generation sequencing analysis of cell type-specific deafness gene expression in the mouse cochlea.
Neuroblastoma
Common genetic variants in NEFL influence gene expression and neuroblastoma risk.
Neuroblastoma
HSD17B12 gene rs11037575 C>T polymorphism confers neuroblastoma susceptibility in a Southern Chinese population.
Neuroblastoma
Replication of GWAS-identified neuroblastoma risk loci strengthens the role of BARD1 and affirms the cumulative effect of genetic variations on disease susceptibility.
Obesity
An Integrative Phenotype-Genotype Approach Using Phenotypic Characteristics from the UAE National Diabetes Study Identifies HSD17B12 as a Candidate Gene for Obesity and Type 2 Diabetes.
Osteosarcoma
Effects of 20 alpha-hydroxysteroid dehydrogenase and its inhibitors on canine osteosarcoma cell growth in vitro.
Ovarian Neoplasms
Mutation analysis and characterization of HSD17B2 sequence variants in breast cancer cases from French Canadian families with high risk of breast and ovarian cancer.
Ovarian Neoplasms
The Expression of HSD17B12 Is Associated with COX-2 Expression and Is Increased in High-Grade Epithelial Ovarian Cancer.
Peripheral Nervous System Diseases
Four patients with D-bifunctional protein (DBP) deficiency: Expanding the phenotypic spectrum of a highly variable disease.
Peripheral Nervous System Diseases
Slowly progressive d-bifunctional protein deficiency with survival to adulthood diagnosed by whole-exome sequencing.
Pituitary Neoplasms
17Beta-hydroxysteroid dehydrogenase type 1, 2, 3, and 4 expression and enzyme activity in human anterior pituitary adenomas.
Polycystic Ovary Syndrome
PDGFRA, HSD17B4 and HMGB2 are potential therapeutic targets in polycystic ovarian syndrome and breast cancer.
Precursor Cell Lymphoblastic Leukemia-Lymphoma
Multi-omics analyses identify HSD17B4 methylation-silencing as a predictive and response marker of HER2-positive breast cancer to HER2-directed therapy.
Pregnancy, Tubal
Expression of P450 aromatase and 17beta-hydroxysteroid dehydrogenase type 1 at fetal-maternal interface during tubal pregnancy.
Primary Ovarian Insufficiency
Epistasis between the HSD17B4 and TG polymorphisms is associated with premature ovarian failure.
Prolactinoma
17Beta-hydroxysteroid dehydrogenase type 1, 2, 3, and 4 expression and enzyme activity in human anterior pituitary adenomas.
Prostatic Neoplasms
Acetylation-mediated degradation of HSD17B4 regulates the progression of prostate cancer.
Prostatic Neoplasms
Allelic loss of the loci containing the androgen synthesis gene, StAR, is prognostic for relapse in intermediate-risk prostate cancer.
Prostatic Neoplasms
Alternative Acts: Oncogenic Splicing of Steroidogenic Enzymes in Prostate Cancer.
Prostatic Neoplasms
Characteristics of a highly labile human type 5 17beta-hydroxysteroid dehydrogenase.
Prostatic Neoplasms
Differential but Concerted Expression of HSD17B2, HSD17B3, SHBG and SRD5A1 Testosterone Tetrad Modulate Therapy Response and Susceptibility to Disease Relapse in Patients with Prostate Cancer.
Prostatic Neoplasms
Differential expression of 17beta-hydroxysteroid dehydrogenase isozyme genes in prostate cancer and noncancer tissues.
Prostatic Neoplasms
Expression of different 17beta-hydroxysteroid dehydrogenase types and their activities in human prostate cancer cells.
Prostatic Neoplasms
Functional silencing of HSD17B2 in prostate cancer promotes disease progression.
Prostatic Neoplasms
Functional validation of metabolic genes that distinguish Gleason 3 from Gleason 4 prostate cancer foci.
Prostatic Neoplasms
HSD17B4 overexpression, an independent biomarker of poor patient outcome in prostate cancer.
Prostatic Neoplasms
Loss of an Androgen-Inactivating and Isoform-Specific HSD17B4 Splice Form Enables Emergence of Castration-Resistant Prostate Cancer.
Prostatic Neoplasms
Regulation of 17beta-hydroxysteroid dehydrogenase type 2, type 4 and type 5 by calcitriol, LXR agonist and 5alpha-dihydrotestosterone in human prostate cancer cells.
Prostatic Neoplasms
Steroidogenic enzymes and stem cell markers are up-regulated during androgen deprivation in prostate cancer.
Protein Deficiency
D-bifunctional protein deficiency: a cause of neonatal onset seizures and hypotonia.
Protein Deficiency
Diagnosis of D-Bifunctional Protein Deficiency through Whole-Genome Sequencing: Implications for Cost-Effective Care.
Protein Deficiency
First Case of Peroxisomal D-bifunctional Protein Deficiency with Novel HSD17B4 Mutations and Progressive Neuropathy in Korea.
Protein Deficiency
Heterozygous mutations in HSD17B4 cause juvenile peroxisomal D-bifunctional protein deficiency.
Protein Deficiency
Next generation sequencing with copy number variant detection expands the phenotypic spectrum of HSD17B4-deficiency.
Protein Deficiency
Rapid whole-genome sequencing identifies a homozygous novel variant, His540Arg, in HSD17B4 resulting in D-bifunctional protein deficiency disorder diagnosis.
Protein Deficiency
Two Novel HSD17B4 Heterozygous Mutations in Association With D-Bifunctional Protein Deficiency: A Case Report and Literature Review.
Puberty, Precocious
Identification and Characterization of lncRNA and mRNA in Testes of Landrace and Hezuo Boars.
Rectal Neoplasms
The prognostic impact of lipid biosynthesis-associated markers, HSD17B2 and HMGCS2, in rectal cancer treated with neoadjuvant concurrent chemoradiotherapy.
Sarcoma
Identification of a 17beta-hydroxysteroid dehydrogenase type 12 pseudogene as the source of a highly restricted BALB/c Meth A tumor rejection peptide.
Seizures
Diagnosis of D-Bifunctional Protein Deficiency through Whole-Genome Sequencing: Implications for Cost-Effective Care.
Spasms, Infantile
Four patients with D-bifunctional protein (DBP) deficiency: Expanding the phenotypic spectrum of a highly variable disease.
Spinocerebellar Ataxias
Biallelic mutation of HSD17B4 induces middle age-onset spinocerebellar ataxia.
Squamous Cell Carcinoma of Head and Neck
Prediction of future metastasis and molecular characterization of head and neck squamous-cell carcinoma based on transcriptome and genome analysis by microarrays.
Stomach Neoplasms
Genetic susceptibility factors on genes involved in the steroid hormone biosynthesis pathway and progesterone receptor for gastric cancer risk.
Testicular Neoplasms
Effect modification of endocrine disruptors and testicular germ cell tumour risk by hormone-metabolizing genes.
Thymoma
Estrogen inhibits cell proliferation through in situ production in human thymoma.
Uremia
Different vitamin D receptor agonists exhibit differential effects on endothelial function and aortic gene expression in 5/6 nephrectomized rats.
Usher Syndromes
Laser-capture micro dissection combined with next-generation sequencing analysis of cell type-specific deafness gene expression in the mouse cochlea.
Uterine Hemorrhage
Menopausal endocrinology and management.
Waardenburg Syndrome
Laser-capture micro dissection combined with next-generation sequencing analysis of cell type-specific deafness gene expression in the mouse cochlea.
Zellweger Syndrome
Unique multifunctional HSD17B4 gene product: 17beta-hydroxysteroid dehydrogenase 4 and D-3-hydroxyacyl-coenzyme A dehydrogenase/hydratase involved in Zellweger syndrome.
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0.0012
(13alpha)-3-hydroxyestra-1(10),2,4-trien-17-one
Homo sapiens
pH and temperature not specified in the publication
0.000101
(16alpha)-2-chloro-16-fluoro-3-hydroxyestra-1(10),2,4-trien-17-one
Homo sapiens
-
0.00032
(16beta)-16-(ethoxymethyl)-3-hydroxyestra-1(10),2,4-trien-17-one
Homo sapiens
-
0.000035
(16beta)-2-chloro-16-fluoro-3-hydroxyestra-1(10),2,4-trien-17-one
Homo sapiens
-
0.01
(16beta)-3-hydroxy-16-methyl-17-oxoestra-1(10),2,4-triene-16-carbonitrile
Homo sapiens
-
0.00011
(16Z)-3-hydroxy-16-(hydroxymethylidene)estra-1(10),2,4-trien-17-one
Homo sapiens
-
0.00051
(17beta)-3,17-dihydroxy-N-(pyridin-3-ylmethyl)estra-1(10),2,4-triene-16-carboxamide
Homo sapiens
-
0.000087
(2R,4aS,4bR,10bS,12aS)-9-chloro-2-fluoro-8-hydroxy-12a-methyl-3,4,4a,4b,5,6,10b,11,12,12a-decahydrochrysen-1(2H)-one
Homo sapiens
-
0.000126
(2S,4aS,4bR,10bS,12aS)-9-chloro-2-fluoro-8-hydroxy-12a-methyl-3,4,4a,4b,5,6,10b,11,12,12a-decahydrochrysen-1(2H)-one
Homo sapiens
-
0.00203
(3alpha,7alpha,17beta)-17-ethynyl-7-methylestr-5(10)-ene-3,17-diol
Homo sapiens
-
0.00483
(3beta,7alpha,17beta)-17-ethynyl-7-methylestr-5(10)-ene-3,17-diol
Homo sapiens
-
0.000015
(4aS,4bR,10bS,12aS)-8-hydroxy-12a-methyl-9-(2-phenylethyl)-3,4,4a,4b,5,6,10b,11,12,12a-decahydrochrysen-1(2H)-one
Homo sapiens
-
0.000024
(4aS,4bR,10bS,12aS)-8-hydroxy-12a-methyl-9-prop-2-en-1-yl-3,4,4a,4b,5,6,10b,11,12,12a-decahydrochrysen-1(2H)-one
Homo sapiens
-
0.000052
(4aS,4bR,10bS,12aS)-8-hydroxy-9-iodo-12a-methyl-3,4,4a,4b,5,6,10b,11,12,12a-decahydrochrysen-1(2H)-one
Homo sapiens
-
0.000085
(4aS,4bR,10bS,12aS)-8-hydroxy-9-methoxy-12a-methyl-3,4,4a,4b,5,6,10b,11,12,12a-decahydrochrysen-1(2H)-one
Homo sapiens
-
0.000052
(4aS,4bR,10bS,12aS)-9-bromo-8-hydroxy-12a-methyl-3,4,4a,4b,5,6,10b,11,12,12a-decahydrochrysen-1(2H)-one
Homo sapiens
-
0.000077
(4aS,4bR,10bS,12aS)-9-chloro-8-hydroxy-12a-methyl-3,4,4a,4b,5,6,10b,11,12,12a-decahydrochrysen-1(2H)-one
Homo sapiens
-
0.000044
(6-hydroxy-1,3-benzothiazol-2-yl)(3-hydroxyphenyl)methanone
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0003
(6aS)-2-hydroxy-6a-methyl-N-(2-pyridin-3-ylethyl)-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-9-carboxamide
Homo sapiens
0.01 mM, 99% inhibition, IC50: 0.0003 mM
0.00088
(6aS)-2-hydroxy-6a-methyl-N-(pyridin-2-ylmethyl)-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-9-carboxamide
Homo sapiens
0.01 mM, 93% inhibition, IC50: 0.00088 mM
0.00078
(6aS)-2-hydroxy-6a-methyl-N-(pyridin-3-ylmethyl)-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-9-carboxamide
Homo sapiens
0.01 mM, 92% inhibition, IC50: 0.00078 mM
0.0023
(6aS)-2-hydroxy-6a-methyl-N-[(1-methyl-1H-pyrrol-2-yl)methyl]-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-9-carboxamide
Homo sapiens
0.01 mM, 90% inhibition, IC50: 0.0023 mM
0.0007
(6aS)-3-ethyl-2-hydroxy-6a-methyl-N-(2-pyridin-3-ylethyl)-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-9-carboxamide
Homo sapiens
-
0.00053
(6aS)-8-(2-methoxyethyl)-6a-methyl-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazol-2-ol
Homo sapiens
-
0.00095
(6aS)-9-(hydroxymethyl)-6a-methyl-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazol-2-ol
Homo sapiens
-
0.0019
(6Z,17E)-3-hydroxyestra-1(10),2,4-triene-6,17-dione dioxime
Homo sapiens
-
0.00144
(7alpha,17beta)-17-ethynyl-17-hydroxy-7-methylestr-4-en-3-one
Homo sapiens
-
0.0054
1-(3'-ethyl-4'-hydroxy-biphenyl-4-yl)-ethanone
Homo sapiens
-
0.0099
1-(3-ethyl-4'-hydroxy-biphenyl-4-yl)-ethanone
Homo sapiens
-
0.0037
1-(4'-hydroxy-2'_methyl-biphenyl-4-yl)-ethanone
Homo sapiens
-
0.0037
1-(4'-hydroxy-biphenyl-4-yl)-ethanone
Homo sapiens
-
0.0048
1-(6-hydroxy-9H-fluoren-2-yl)-ethanone
Homo sapiens
-
0.00004
1-bromo-6-(3-hydroxyphenyl)-2-naphthol
Homo sapiens
in 20 mM KH2PO4, pH 7.4, at 25°C
0.01
16-cyano-17-oxoestra-1(10),2,4-trien-3-yl sulfamate
Homo sapiens
-
0.0021
16-cyano-2-methoxy-17-oxoestra-1(10),2,4-trien-3-yl sulfamate
Homo sapiens
-
0.0043
2,2'-diimino-7,7'-dimethyl-5,5'-bis(1-methylethyl)-2H,2'H-8,8'-binaphtho[1,8-bc]furan-3,3',4,4'-tetrol
Homo sapiens
-
0.00014
2-chloro-3-hydroxyestra-1(10),2,4-trien-17-one
Homo sapiens
-
0.0000222
2-chloro-4-[5-(2,6-difluoro-3-hydroxybenzoyl)thiophen-2-yl]phenyl sulfamate
Homo sapiens
whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.0051
2-ethyl-17-oxo-16-[2-oxo-2-[(pyridin-3-ylmethyl)amino]ethyl]estra-1(10),2,4-trien-3-yl sulfamate
Homo sapiens
-
0.00000362 - 0.000165
2-[2-ethyl-3-hydroxy-17-oxoestra-1(10),2,4-trien-16-yl]-N-(pyridin-2-ylmethyl)acetamide
0.000027
2-[2-ethyl-3-hydroxy-17-oxoestra-1(10),2,4-trien-16-yl]-N-(pyridin-3-ylmethyl)acetamide
Homo sapiens
-
0.000037
2-[3-hydroxy-17-oxoestra-1(10),2,4-trien-16-yl]-N-(pyridin-3-ylmethyl)acetamide
Homo sapiens
-
0.0047
2-[5-(3-ethyl-4-hydroxyphenyl)-1-oxo-indan-2-yl]-N-pyridin-3-ylmethyl-acetamide
Homo sapiens
-
0.00137 - 0.00194
3'-(1-benzothien-2-yl)biphenyl-3-ol
0.00056 - 0.00237
3'-(5-chloro-2-thienyl)biphenyl-3-ol
0.004299
3'-hydroxy-N-(3-hydroxybenzyl)-N-methyl-[1,10-biphenyl]-4-sulfonamide
Homo sapiens
pH 7.4, 37°C
0.002031
3'-hydroxy-N-(3-hydroxyphenyl)-N-methyl-[1,10-biphenyl]-4-sulfonamide
Homo sapiens
pH 7.4, 37°C
0.0022
3,3',4,4'-tetrahydroxy-7,7'-dimethyl-5,5'-bis(1-methylethyl)-2H,2'H-8,8'-binaphtho[1,8-bc]furan-2,2'-dione
Homo sapiens
-
0.000044
3-(3,17beta-dihydroxy-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide
Homo sapiens
-
0.000171
3-(3-hydroxy-17-oxo-estra-1,3,5(10)-trien-16beta-ylmethyl)-benzamide
Homo sapiens
-
0.000005
3-benzyl-2-(2-bromo-3,4,5-trimethoxyphenyl)-8-hydroxy[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
Homo sapiens
87% inhibition at 100 nM, 95% inhibition at 0.001 mM. IC50: 5 nM
0.000005
3-benzyl-8-hydroxy-2-(3,4,5-trimethoxyphenyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
0.00007
3-hydroxy-13alpha-D-secooxime
Homo sapiens
pH and temperature not specified in the publication
0.00094
3-hydroxy-17-oxoestra-1(10),2,4-triene-16-carboxylic acid
Homo sapiens
-
0.000168
3-hydroxy-17-oxoestra-1(10),2,4-triene-2-carbonitrile
Homo sapiens
-
0.000243
3-hydroxy-N-(6-hydroxy-1,3-benzothiazol-2-yl)benzamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0011
3-hydroxyestra-1(10),2,4-triene-16,17-dione 16-oxime
Homo sapiens
-
0.00073
3-[(6aS)-2-hydroxy-6a-methyl-4b,6,6a,10,10a,10b,11,12-octahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazol-8(5H)-yl]propanenitrile
Homo sapiens
-
0.00132
3-[1-(4-hydroxyphenyl)-1H-1,2,3-triazol-4-yl]-phenol
Homo sapiens
substrate: estrone, 17beta-HSD1
0.00047 - 0.00238
3-[2-(5-chloro-2-thienyl)pyridin-4-yl]phenol
0.00161
3-[3-(4-hydroxyphenyl)isoxazol-5-yl]-phenol
Homo sapiens
substrate: estrone, 17beta-HSD1
0.00185
3-[4-(4-hydroxyphenyl)-1,3-oxazol-2-yl]-phenol
Homo sapiens
substrate: estrone, 17beta-HSD1
0.00084
3-[4-(4-hydroxyphenyl)-1H-1,2,3-triazol-1-yl]-phenol
Homo sapiens
substrate: estrone, 17beta-HSD1
0.00085 - 0.00364
3-[4-(5-chloro-2-thienyl)pyridin-2-yl]phenol
0.00031
3-[5-(4-hydroxyphenyl)-1,3-oxazol-2-yl]-phenol
Homo sapiens
substrate: estrone, 17beta-HSD1
0.00139 - 0.00711
3-[6-(5-chloro-2-thienyl)pyridin-2-yl]phenol
0.00102 - 0.01
4'-(5-chloro-2-thienyl)biphenyl-3-ol
0.00069 - 0.00297
4'-(6-methoxypyridin-3-yl)biphenyl-3-ol
0.0018
4-(3-ethyl-4-hydroxy-biphenyl)-2,2-dimethyl-4-oxo-N-pyridin-3-ylmethyl-butyramide
Homo sapiens
-
0.000052
5'-O-[9-[(16b,17b)-3,17-dihydroxyestra-1(10),2,4-trien-16-yl]nonanoyl]adenosine
Homo sapiens
-
0.002
5-(3-ethyl-4-hydroxyphenyl)-indan-1-one
Homo sapiens
-
0.0029
5-(3-fluoro-4-hydroxyphenyl)-indan-1-one
Homo sapiens
-
0.0017
5-(4-hydroxyphenyl)-indan-1-one
Homo sapiens
-
0.0083
6-(3-ethyl-4-methoxyphenyl)-3,4-dihydro-2H-naphthalen-1-one
Homo sapiens
-
0.00002
6-(3-hydroxyphenyl)-1-phenyl-2-naphthol
Homo sapiens
in 20 mM KH2PO4, pH 7.4, at 25°C
0.000116
6-(3-hydroxyphenyl)-2-naphthol
Homo sapiens
in 20 mM KH2PO4, pH 7.4, at 25°C
0.0156
6-(4-hydroxy-phenyl)-3,4-dihydro-2H-naphthalen-1-one
Homo sapiens
-
0.000218
estrone
Homo sapiens
-
0.00185
ethyl [(6aS)-2-hydroxy-6a-methyl-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazol-9-yl]acetate
Homo sapiens
-
0.00092
methyl [(6aS)-2-hydroxy-6a-methyl-4b,6,6a,10,10a,10b,11,12-octahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazol-8(5H)-yl]acetate
Homo sapiens
-
0.00016
N-butyl-6-[[(6beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-6-yl]sulfanyl]-N-methylhexanamide
Homo sapiens
-
0.000027
STX1040
Homo sapiens
-
0.000049
(13S,17R)-3-hydroxy-13-methyl-6,7,8,9,11,12,13,14,15,16-decahydrospiro[cyclopenta[a]phenanthrene-17,2'-pyran]-6'(3'H)-one
Homo sapiens
-
-
0.000019
(13S,17R)-3-hydroxy-4',13-dimethyl-4',5',6,7,8,9,11,12,13,14,15,16-dodecahydrospiro[cyclopenta[a]phenanthrene-17,2'-pyran]-6'(3'H)-one
Homo sapiens
-
-
0.000016
(13S,17R)-3-hydroxy-5',13-dimethyl-4',5',6,7,8,9,11,12,13,14,15,16-dodecahydrospiro[cyclopenta[a]phenanthrene-17,2'-pyran]-6'(3'H)-one
Homo sapiens
-
-
0.000028
(13S,17R)-3-hydroxy-5',5',13-trimethyl-4',5',6,7,8,9,11,12,13,14,15,16-dodecahydrospiro[cyclopenta[a]phenanthrene-17,2'-pyran]-6'(3'H)-one
Homo sapiens
-
-
0.000107
(13S,17R)-5'-cyclopropyl-3-hydroxy-13-methyl-4',5',6,7,8,9,11,12,13,14,15,16-dodecahydrospiro[cyclopenta[a]phenanthrene-17,2'-pyran]-6'(3'H)-one
Homo sapiens
-
-
0.00002
(13S,17S)-3-hydroxy-13-methyl-4',5',6,7,8,9,11,12,13,14,15,16-dodecahydrospiro[cyclopenta[a]phenanthrene-17,2'-pyran]-6'(3'H)-one
Homo sapiens
-
-
0.000042
(13S,17S)-3-hydroxy-13-methyl-6,7,8,9,11,12,13,14,15,16-decahydro-7'H-spiro[cyclopenta[a]phenanthrene-17,2'-oxepan]-7'-one
Homo sapiens
-
-
0.00041 - 0.0006
(4aR,6aS,7S)-7-[heptyl(methyl)amino]-1,4a,6a-trimethylhexadecahydro-2H-indeno[5,4-f]quinolin-2-one
0.00096
(4aR,6aS,7S)-7-[heptyl(methyl)amino]-4a,6a-dimethylhexadecahydro-2H-indeno[5,4-f]quinolin-2-one
Homo sapiens
pH and temperature not specified in the publication
0.00001
(4R,5R)-4-(2-fluorophenyl)-5-[hydroxy(5-phenylthiophen-2-yl)methyl]-1-methylpyrrolidin-2-one
Homo sapiens
pH 7.4, 37°C
0.00005
(4R,5R)-5-[hydroxy[5-(pyridin-3-yl)thiophen-2-yl]methyl]-1-methyl-4-phenylpyrrolidin-2-one
Homo sapiens
pH 7.4, 37°C
0.00042
(4S,5S)-5-[biphenyl-3-yl(hydroxy)methyl]-4-(2-fluorophenyl)-1-methylpyrrolidin-2-one
Homo sapiens
pH 7.4, 37°C
0.00102
(4S,5S)-5-[biphenyl-4-yl(hydroxy)methyl]-4-(2-fluorophenyl)-1-methylpyrrolidin-2-one
Homo sapiens
pH 7.4, 37°C
0.00005
(4S,5S)-5-[hydroxy[5-(pyridin-3-yl)thiophen-2-yl]methyl]-1-methyl-4-phenylpyrrolidin-2-one
Homo sapiens
pH 7.4, 37°C
0.000066
(6aS,6bS,11aS)-2-hydroxy-6a-methyl-4b,5,6,6a,6b,9,10,11,11a,12,12a,12b,13,14-tetradecahydro-8H-naphtho[2',1':4,5]indeno[1,2-b]oxepin-8-one
Homo sapiens
-
-
0.0041
1'(2')H-estra-1,3,5(10)-trieno[17,16-c]pyrazol-3-ol
Homo sapiens
-
IC50: 0.0041 mM
0.000173
1,1':4',1''-terphenyl-3,3''-diol
Homo sapiens
-
at 37°C in phosphate buffer (50 mM) with 20% (v/v) glycerol and 1 mM EDTA
0.0054
1-(3'-ethyl-4'-hydroxy-biphenyl-4-yl)-ethanone
Homo sapiens
-
0.0099
1-(3-ethyl-4'-hydroxy-biphenyl-4-yl)-ethanone
Homo sapiens
-
0.0037
1-(4'-hydroxy-2'-methyl-biphenyl-4-yl)-ethanone
Homo sapiens
-
0.0037
1-(4'-hydroxy-biphenyl-4-yl)-ethanone
Homo sapiens
-
0.0048
1-(6-hydroxy-9H-fluoren-2-yl)-ethanone
Homo sapiens
-
0.00014
10-((13S,16S,17S)-3,17-Dihydroxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-16-yl)-decanoic acid 5-(6-amino-purin-9-yl)-3,4-dihydroxy-tetrahydro-furan-2-ylmethyl ester
Homo sapiens
-
IC50: 140 nM
0.00046
16alpha-bromopropyl-estradiol
Homo sapiens
-
IC50: 0.00046 mM, reduction of estrone, the inhibitor is totally inactive against type 2 17beta-HSD and type type 1 17beta-HSD
0.00029
16beta-m-pyridylmethylamidomethyl-2-methoxyoestrone
Homo sapiens
-
IC50: 0.00029 mM
0.00291 - 0.00424
17beta-[(N-decyl)formamido]-4-methyl-4-aza-5alpha-androstan-3-one
-
0.00578 - 0.00601
17beta-[(N-heptyl)methylamino]-4-aza-5alpha-androstan-3-one
-
0.00041 - 0.00119
17beta-[(N-heptyl)methylamino]-4-methyl-4-aza-5alpha-androstan-3-one
-
0.0007 - 0.00332
17beta-[(N-nonyl)formamido]-4-methyl-4-aza-5alpha-androstan-3-one
-
0.0338
2',4',4-trihydroxy-4'-chalcone
Homo sapiens
-
IC50: 0.0338 mM
0.0346
2',4'-dihydroxy-chalcone
Homo sapiens
-
IC50: 0.0346 mM
0.0103 - 0.042
2,2',4,4'-tetrahydroxybenzophenone
0.023
2-(2-bromo-4,6-dimethylphenoxy)-N'-[(E)-(2,4-dihydroxyphenyl)methylidene]acetohydrazide
Homo sapiens
pH 7.4, 37°C
0.0024
2-methoxyoestrone
Homo sapiens
-
IC50: 0.0024 mM
0.0064
2-methylcinnamic acid
Homo sapiens
-
IC50: 0.0064 mM
0.0047
2-[5-(3-ethyl-4-hydroxyphenyl)-1-oxo-indan-2-yl]-N-pyridin-3-ylmethyl-acetamide
Homo sapiens
-
0.0006
3',4',5,7-tetrahydroxy-flavone
Homo sapiens
-
IC50: 0.0006 mM
0.0052
3',4',7-trihydroxy-isoflavone
Homo sapiens
-
IC50: 0.0052 mM
0.000934
3'-hydroxy-N-(3-hydroxybenzyl)-N-methyl-[1,10-biphenyl]-4-sulfonamide
Homo sapiens
pH 7.4, 37°C
0.00064
3'-hydroxy-N-(3-hydroxybenzyl)-N-methylbiphenyl-3-carboxamide
Homo sapiens
pH 7.4, 37°C
0.000594
3'-hydroxy-N-(3-hydroxybenzyl)-N-methylbiphenyl-4-carboxamide
Homo sapiens
pH 7.4, 37°C
0.00054
3'-hydroxy-N-(3-hydroxyphenyl)-N-methyl-[1,10-biphenyl]-3-sulfonamide
Homo sapiens
pH 7.4, 37°C
0.001179
3'-hydroxy-N-(3-hydroxyphenyl)-N-methyl-[1,10-biphenyl]-4-sulfonamide
Homo sapiens
pH 7.4, 37°C
0.000061
3'-hydroxy-N-(3-hydroxyphenyl)-N-methylbiphenyl-4-carboxamide
Homo sapiens
pH 7.4, 37°C
0.000494
3'-methoxy-N-(3-methoxybenzyl)-N-methylbiphenyl-4-carboxamide
Homo sapiens
pH 7.4, 37°C
0.00052
3'-methoxy-N-(3-methoxyphenyl)-N-methylbiphenyl-3-carboxamide
Homo sapiens
pH 7.4, 37°C
0.000517
3'-methoxy-N-(3-methoxyphenyl)-N-methylbiphenyl-4-carboxamide
Homo sapiens
pH 7.4, 37°C
0.041
3,3'-(1-phenyl-1H-1,2,4-triazole-3,5-diyl)diphenol
Homo sapiens
-
37°C, pH not specified in the publication
0.017
3,3'-(1H-1,2,3-triazole-1,4-diyl)diphenol
0.000101
3,3'-pyridine-2,5-diyldiphenol
Homo sapiens
-
at 37°C in phosphate buffer (50 mM) with 20% (v/v) glycerol and 1 mM EDTA
0.049
3,4,5-trimethoxycinnamic acid
Homo sapiens
-
IC50: 0.049 mM
15
3,5,7-trihydroxy-4'-methoxy-flavone
Homo sapiens
-
IC50: 15 mM
0.000042
3-([(16beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-16-yl]methyl)benzamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000083
3-([(16beta,17beta)-3-(2-bromoethyl)-17-hydroxyestra-1(10),2,4-trien-16-yl]methyl)benzamide
Homo sapiens
-
pH and temperature not specified in the publication
0.006 - 0.072
3-benzylidene camphor
0.00046
3-bromo-5-phenylsalicylic acid
Homo sapiens
-
pH not specified in the publication, 25°C
0.0063
3-bromo-N-(3-hydroxy-4-methylphenyl)benzenesulfonamide
Homo sapiens
pH 7.4, 37°C
0.1
3-cyclohexylpropanoic acid
Homo sapiens
-
weak inhibition, IC50: 0.1 mM, above
0.00095
3-hydroxy-1,3,5(10)-triene-[17,16-c]-(5'-hydroxymethyl)-pyrazole
Homo sapiens
-
0.01 mM: 94% inhibition, IC50: 0.00095 mM
0.00185
3-hydroxy-1,3,5(10)-triene-[17,16-c]-[5'-(carboxylic acid ethyl ester)]-pyrazole
Homo sapiens
-
0.01 mM: 94% inhibition, IC50: 0.00185 mM
0.00053
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(1'-methoxyethyl)-pyrazole
Homo sapiens
-
0.01 mM: 95% inhibition, IC50: 0.00053 mM
0.00092
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(1'-methyl acetate)-pyrazole
Homo sapiens
-
0.01 mM: 95% inhibition, IC50: 0.00092 mM
0.00275
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(1'-methyl)-pyrazole
Homo sapiens
-
0.01 mM: 94% inhibition, IC50: 0.00275 mM
0.00073
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(1'-propionitrile)-pyrazole
Homo sapiens
-
0.01 mM: 95% inhibition, IC50: 0.00073 mM
0.0023
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-[5'-(1'-methylpyrrol-2''-ylmethyl)carbamoyl]-pyrazole
Homo sapiens
-
0.01 mM: 89% inhibition, IC50: 0.0023 mM
0.00088
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-[5'-(pyridin-2''-ylmethyl)carbamoyl]-pyrazole
Homo sapiens
-
0.01 mM: 93% inhibition, IC50: 0.00088 mM
0.0003
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-[5'-(pyridin-3''-ylethyl)carbamoyl]-pyrazole
Homo sapiens
-
0.01 mM: 99% inhibition, IC50: 0.0003 mM
0.00078
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-[5'-(pyridin-3''-ylmethyl)carbamoyl]-pyrazole
Homo sapiens
-
0.01 mM: 92% inhibition, IC50: 0.00078 mM
0.000159
3-hydroxy-N-(3'-hydroxy-[1,1'-biphenyl]-3-yl)-N-methylbenzenesulfonamide
Homo sapiens
pH 7.4, 37°C
0.000511
3-hydroxy-N-(3'-hydroxy-[1,1'-biphenyl]-4-yl)-N-methylbenzenesulfonamide
Homo sapiens
pH 7.4, 37°C
0.0019
3-hydroxyestra-1,3,5(10),7-tetraen-17-one
Homo sapiens
-
IC50: 0.0019 mM, oxidation of estradiol
0.043
3-trifluoromethylcinnamic acid
Homo sapiens
-
IC50: 0.043 mM
0.00812
3-[1-(4-hydroxyphenyl)-1H-1,2,3-triazol-4-yl]-phenol
Homo sapiens
substrate: estradiol-17beta, 17beta-HSD2
0.00084 - 40.88
3-[1-(4-hydroxyphenyl)-1H-1,2,3-triazol-4-yl]phenol
0.00047
3-[2-(5-chlorothiophen-2-yl)pyridin-4-yl]phenol
Homo sapiens
pH 7.4, 37°C
0.021
3-[3-(4-hydroxyphenyl)-1-methyl-1H-1,2,4-triazol-5-yl]phenol
Homo sapiens
-
37°C, pH not specified in the publication
0.00027
3-[3-(4-hydroxyphenyl)isoxazol-5-yl]-phenol
Homo sapiens
substrate: estradiol-17beta, 17beta-HSD2
0.00025
3-[4-(4-hydroxyphenyl)-1,3-oxazol-2-yl]-phenol
Homo sapiens
substrate: estradiol-17beta, 17beta-HSD2
0.00728
3-[4-(4-hydroxyphenyl)-1H-1,2,3-triazol-1-yl]-phenol
Homo sapiens
substrate: estradiol-17beta, 17beta-HSD2
0.00084 - 46.94
3-[4-(4-hydroxyphenyl)-1H-1,2,3-triazol-1-yl]phenol
0.000077
3-[4-(4-hydroxyphenyl)thiophen-2-yl]phenol
Homo sapiens
-
at 37°C in phosphate buffer (50 mM) with 20% (v/v) glycerol and 1 mM EDTA
0.0175
3-[5-(4-hydroxyphenyl)-1,3-oxazol-2-yl]-phenol
Homo sapiens
substrate: estrone, 17beta-HSD2
0.02
3-[5-(4-hydroxyphenyl)-1-methyl-1H-1,2,4-triazol-3-yl]phenol
Homo sapiens
-
37°C, pH not specified in the publication
0.044
3-[5-(4-hydroxyphenyl)-1-phenyl-1H-1,2,4-triazol-3-yl]phenol
Homo sapiens
-
37°C, pH not specified in the publication
0.000069
3-[5-(4-hydroxyphenyl)thiophen-2-yl]phenol
Homo sapiens
-
at 37°C in phosphate buffer (50 mM) with 20% (v/v) glycerol and 1 mM EDTA
0.000151
3-[5-(4-hydroxyphenyl)thiophen-3-yl]phenol
Homo sapiens
-
at 37°C in phosphate buffer (50 mM) with 20% (v/v) glycerol and 1 mM EDTA
0.0031
3alpha-hydroxy-3beta-([4-[(2-methoxy-4-methylphenyl)methyl]piperazin-1-yl]methyl)-androstan-17-one
Homo sapiens
-
pH and temperature not specified in the publication, transformation of E2 to E1 by HEK-293[17beta-HSD10] cells
0.00042
3alpha-hydroxy-3beta-([4-[(3-methoxy-4-methylphenyl)methyl]piperazin-1-yl]methyl)-androstan-17-one
Homo sapiens
-
pH and temperature not specified in the publication, transformation of E2 to E1 by HEK-293[17beta-HSD10] cells
0.0026
3alpha-hydroxy-3beta-([4-[(3-methoxyphenyl)methyl]piperazin-1-yl]methyl)-androstan-17-one
Homo sapiens
-
pH and temperature not specified in the publication, transformation of E2 to E1 by HEK-293[17beta-HSD10] cells
0.00097
3alpha-hydroxy-3beta-([4-[(quinolin-3-yl)methyl]piperazin-1-yl]methyl)-androstan-17-one
Homo sapiens
-
pH and temperature not specified in the publication, transformation of E2 to E1 by HEK-293[17beta-HSD10] cells
0.00014
3alpha-hydroxy-3beta-[(4-[[3-methoxy-4-(trifluoromethyl)phenyl]methyl]piperazin-1-yl)methyl]-androstan-17-one
Homo sapiens
-
pH and temperature not specified in the publication, transformation of E2 to E1 by HEK-293[17beta-HSD10] cells
0.00126
3beta-[(4-[[3-methoxy-4-(trifluoromethyl)phenyl]methyl]piperazin-1-yl)methyl]-17alpha-pregn-20-yne-3alpha,17-diol
Homo sapiens
-
pH and temperature not specified in the publication, transformation of E2 to E1 by HEK-293[17beta-HSD10] cells
-
0.00095
3beta-[(4-[[3-methoxy-4-(trifluoromethyl)phenyl]methyl]piperazin-1-yl)methyl]-androstane-3alpha,17alpha-diol
Homo sapiens
-
pH and temperature not specified in the publication, transformation of E2 to E1 by HEK-293[17beta-HSD10] cells
0.00205
3beta-[[4-(3,5-dimethylbenzoyl)piperazin-1-yl]methyl]-3alpha-hydroxyandrostan-17-one
Homo sapiens
-
pH and temperature not specified in the publication, transformation of E2 to E1 by HEK-293[17beta-HSD10] cells
0.0023
3beta-[[4-(3-acetylbenzoyl)piperazin-1-yl]methyl]-3alpha-hydroxyandrostan-17-one
Homo sapiens
-
pH and temperature not specified in the publication, transformation of E2 to E1 by HEK-293[17beta-HSD10] cells
0.0026
3beta-[[4-([1,1'-biphenyl]-4-carbonyl)piperazin-1-yl]methyl]-3alpha-hydroxyandrostan-17-one
Homo sapiens
-
pH and temperature not specified in the publication, transformation of E2 to E1 by HEK-293[17beta-HSD10] cells
0.0003
4',5,7-trihydroxy-flavone
Homo sapiens
-
IC50: 0.0003 mM
0.001
4',5,7-trihydroxy-isoflavone
Homo sapiens
-
IC50: 0.001 mM
0.01
4',7-dihydroxy-isoflavone
Homo sapiens
-
IC50: 0.01 mM
0.00048 - 0.000482
4'-hydroxy-N-(3-hydroxybenzyl)-N-methylbiphenyl-3-carboxamide
0.0012
4'-methoxy-N-(3-methoxyphenyl)-N-methylbiphenyl-3-carboxamide
Homo sapiens
pH 7.4, 37°C
0.0018
4-(3'-ethyl-4'-hydroxy-biphenyl)-2,2-dimethyl-4-oxo-N-pyridin-3-ylmethyl-butyramide
Homo sapiens
-
0.0037
4-(3'-ethyl-4'-hydroxy-biphenyl)-4-oxo-N-pyridin-3-ylmethyl-butyramide
Homo sapiens
-
0.0017
4-(4-[[3alpha-hydroxy-17-oxoandrostan-3beta-yl]methyl]piperazine-1-carbonyl)benzonitrile
Homo sapiens
-
pH and temperature not specified in the publication, transformation of E2 to E1 by HEK-293[17beta-HSD10] cells
0.001
4-chloro-N-(3-hydroxyphenyl)-2,5-dimethylbenzenesulfonamide
Homo sapiens
pH 7.4, 37°C
0.000023
4-fluoro-3-hydroxy-N-(3'-hydroxybiphenyl-3-yl)-N-methylbenzenesulfonamide
Homo sapiens
pH 7.4, 37°C
0.016
4-hydroxychalcone
Homo sapiens
-
IC50: 0.016 mM
0.0059 - 0.07
4-methylbenzylidene camphor
0.000046
4-[5-(3-hydroxyphenyl)thiophen-2-yl]-2-methylphenol
Homo sapiens
-
at 37°C in phosphate buffer (50 mM) with 20% (v/v) glycerol and 1 mM EDTA
0.0014
4-[[3alpha-hydroxy-17-oxoandrostan-3beta-yl]methyl]-N-[[3-(trifluoromethyl)phenyl]methyl]piperazine-1-carbothioamide
Homo sapiens
-
pH and temperature not specified in the publication, transformation of E2 to E1 by HEK-293[17beta-HSD10] cells
0.00014
5'-O-(10-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha-yl]-decanoyl)adenosine
Homo sapiens
-
IC50: 140 nM
0.00031
5'-O-(11-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha-yl]-undecanoyl) adenosine
Homo sapiens
-
IC50: 310 nM
0.00009
5'-O-(11-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha/beta-yl]-undecanoyl)adenosine
Homo sapiens
-
IC50: 90 nM
0.00012
5'-O-(11-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'beta-yl]-undecanoyl)adenosine
Homo sapiens
-
IC50: 120 nM
0.001
5'-O-(12-[3',17'beta-(dihydroxy)-1',3',5'(10')-estratrien-16'alpha-yl]-dodecanoyl)adenosine
Homo sapiens
-
IC50: 1000 nM
0.0069
5'-O-(6-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha/beta-yl]-hexanoyl)adenosine
Homo sapiens
-
IC50: 6900 nM
0.00043
5'-O-(7-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha-yl]-heptanoyl)adenosine
Homo sapiens
-
IC50: 430 nM
0.000093
5'-O-(8-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha-yl]-octanoyl)adenosine
Homo sapiens
-
IC50: 93 nM
0.000052
5'-O-(9-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha-yl]-nonanoyl)adenosine
Homo sapiens
-
IC50: 52 nM
0.000061
5-(2-fluoro-3-methoxyphenyl)-N-(3-hydroxybenzyl)-N-methylthiophene-2-carboxamide
Homo sapiens
pH 7.4, 37°C
0.000062
5-(2-fluoro-3-methoxyphenyl)-N-(3-methoxyphenyl)-N-methylthiophene-2-carboxamide
Homo sapiens
pH 7.4, 37°C
0.000062
5-(2-fluoro-3-methoxyphenyl)-N-methyl-N-(3-methylphenyl)thiophene-2-carboxamide
Homo sapiens
pH 7.4, 37°C
0.00041
5-(2-hydroxyphenyl)-N-(3-hydroxyphenyl)-N-methylthiophene-2-carboxamide
Homo sapiens
pH 7.4, 37°C
0.00049
5-(2-methoxyphenyl)-N-(3-methoxyphenyl)-N-methylthiophene-2-carboxamide
Homo sapiens
pH 7.4, 37°C
0.002
5-(3-ethyl-4-hydroxyphenyl)-indan-1-one
Homo sapiens
-
0.0029
5-(3-fluoro-4-hydroxyphenyl)-indan-1-one
Homo sapiens
-
0.00033
5-(3-fluorophenyl)-N-(3-hydroxybenzyl)-N-methylthiophene-2-carboxamide
Homo sapiens
pH 7.4, 37°C
0.00017
5-(3-fluorophenyl)-N-(3-methoxyphenyl)-N-methylthiophene-2-carboxamide
Homo sapiens
pH 7.4, 37°C
0.00051
5-(4-cyanophenyl)-N-(3-methoxyphenyl)-N-methylthiophene-2-carboxamide
Homo sapiens
pH 7.4, 37°C
0.0017
5-(4-hydroxyphenyl)-indan-1-one
Homo sapiens
-
0.0083
6-(3-ethyl-4-methoxyphenyl)-3,4-dihydro-2H-naphthalen-1-one
Homo sapiens
-
0.0156
6-(4-hydroxy-phenyl)-3,4-dihydro-2H-naphthalen-1-one
Homo sapiens
-
0.000302
6-(4-hydroxyphenyl)naphthalen-1-ol
Homo sapiens
pH 7.4, 37°C
0.028
7-hydroxy-flavanone
Homo sapiens
-
IC50: 0.028 mM
0.0009
7-hydroxy-flavone
Homo sapiens
-
IC50: 0.0009 mM
0.000093
8-((13S,16S,17S)-3,17-Dihydroxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-16-yl)-octanoic acid 5-(6-amino-purin-9-yl)-3,4-dihydroxy-tetrahydro-furan-2-ylmethyl ester
Homo sapiens
-
IC50: 93 nM
0.000052
9-((13S,16S,17S)-3,17-Dihydroxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-16-yl)-nonanoic acid 5-(6-amino-purin-9-yl)-3,4-dihydroxy-tetrahydro-furan-2-ylmethyl ester
Homo sapiens
-
IC50: 52 nM
0.05
Cinnamic acid
Homo sapiens
-
IC50: 0.050 mM
0.0002
coumestrol
Homo sapiens
-
IC50: 0.0002 mM
0.0017
equilin
Homo sapiens
-
IC50: 0.0017 mM
0.00009 - 0.00081
estrone
0.000072
methyl (13S,17R)-3-hydroxy-13-methyl-6'-oxo-3',4',5',6,6',7,8,9,11,12,13,14,15,16-tetradecahydrospiro[cyclopenta[a]phenanthrene-17,2'-pyran]-5'-carboxylate
Homo sapiens
-
-
0.0011
N,4'-dimethyl-N-(3-methylphenyl)biphenyl-4-carboxamide
Homo sapiens
pH 7.4, 37°C
0.000068
N,5-bis(3-methoxyphenyl)-N-methylthiophene-2-carboxamide
Homo sapiens
pH 7.4, 37°C
0.0011
N-(2,1,3-benzothiadiazol-4-yl)-2-[(4-hydroxypyrimidin-2-yl)sulfanyl]acetamide
Homo sapiens
pH 7.4, 37°C
0.24 - 0.52
N-(2-hydroxyphenyl)-2-methyl-4-(trifluoromethyl)benzenesulfonamide
Homo sapiens
pH 7.4, 37°C
0.003 - 0.01
N-(3-chloro-4-hydroxyphenyl)-4-fluorobenzenesulfonamide
Homo sapiens
pH 7.4, 37°C
0.0071
N-(3-hydroxy-4-methylphenyl)-3-(trifluoromethyl)benzenesulfonamide
Homo sapiens
pH 7.4, 37°C
0.00039
N-(3-hydroxybenzyl)-5-(3-hydroxyphenyl)-N-methylthiophene-2-carboxamide
Homo sapiens
pH 7.4, 37°C
0.00033
N-(3-hydroxybenzyl)-5-(4-hydroxyphenyl)-N-methylthiophene-2-carboxamide
Homo sapiens
pH 7.4, 37°C
0.000161
N-(3-hydroxybenzyl)-5-(4-methoxyphenyl)-N-methylthiophene-2-carboxamide
Homo sapiens
pH 7.4, 37°C
0.00016 - 0.000164
N-(3-hydroxybenzyl)-N-methyl-5-(3-methylphenyl)thiophene-2-carboxamide
0.0033
N-(3-hydroxyphenyl)-2,4,5-trimethylbenzenesulfonamide
Homo sapiens
pH 7.4, 37°C
0.0069
N-(3-hydroxyphenyl)-4-methoxy-2,5-dimethylbenzenesulfonamide
Homo sapiens
pH 7.4, 37°C
0.015
N-(3-hydroxyphenyl)-4-methoxy-2-methyl-5,6,7,8-tetrahydronaphthalene-1-sulfonamide
Homo sapiens
pH 7.4, 37°C
0.0049
N-(3-hydroxyphenyl)benzenesulfonamide
Homo sapiens
pH 7.4, 37°C
0.00037
N-(3-methoxybenzyl)-5-(3-methoxyphenyl)-N-methylthiophene-2-carboxamide
Homo sapiens
pH 7.4, 37°C
0.000058
N-(3-methoxyphenyl)-N-methyl-5-(3-methylphenyl)thiophene-2-carboxamide
Homo sapiens
pH 7.4, 37°C
0.0096
N-(4-hydroxy-5,6,7,8-tetrahydronaphthalen-1-yl)-4-methoxybenzenesulfonamide
Homo sapiens
pH 7.4, 37°C
0.0008
N-butyl-6-[[(6beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-6-yl]oxy]-N-methylhexanamide
Homo sapiens
-
73% inhibition at 0.001 mM, IC50: 0.0008 mM, reduction of estrone with NADH as cofactor
0.00016
N-butyl-6-[[(6beta,17beta)-3,17-dihydroxyestra-1(10),2,4-trien-6-yl]sulfanyl]-N-methylhexanamide
Homo sapiens
-
92% inhibition at 0.001 mM, IC50: 0.00016 mM, reduction of estrone with NADH as cofactor
0.00291 - 0.00396
N-decyl-N-[(4aR,6aS,7S)-1,4a,6a-trimethyl-2-oxohexadecahydro-1H-indeno[5,4-f]quinolin-7-yl]formamide
0.00112 - 0.00578
N-decyl-N-[(4aR,6aS,7S)-4a,6a-dimethyl-2-oxohexadecahydro-1H-indeno[5,4-f]quinolin-7-yl]formamide
0.0016
N-ethyl-4-[[3alpha-hydroxy-17-oxoandrostan-3beta-yl]methyl]-N-methylpiperazine-1-sulfonamide
Homo sapiens
-
pH and temperature not specified in the publication, transformation of E2 to E1 by HEK-293[17beta-HSD10] cells
0.000052
N-methyl-N,5-bis(3-methylphenyl)thiophene-2-carboxamide
Homo sapiens
pH 7.4, 37°C
0.0007 - 0.00332
N-nonyl-N-[(4aR,6aS,7S)-1,4a,6a-trimethyl-2-oxohexadecahydro-1H-indeno[5,4-f]quinolin-7-yl]formamide
0.00107
N-[4-(dimethylsulfamoyl)phenyl]-4-[[3alpha-hydroxy-17-oxoandrostan-3beta-yl]methyl]piperazine-1-carbothioamide
Homo sapiens
-
pH and temperature not specified in the publication, transformation of E2 to E1 by HEK-293[17beta-HSD10] cells
0.00285
[[4-(4-benzoylbenzoyl)piperazin-1-yl]methyl]-3alpha-hydroxyandrostan-17-one
Homo sapiens
-
pH and temperature not specified in the publication, transformation of E2 to E1 by HEK-293[17beta-HSD10] cells
additional information
(2,4-dihydroxyphenyl)-phenylmethanone
0.00000362
2-[2-ethyl-3-hydroxy-17-oxoestra-1(10),2,4-trien-16-yl]-N-(pyridin-2-ylmethyl)acetamide
Homo sapiens
-
0.000165
2-[2-ethyl-3-hydroxy-17-oxoestra-1(10),2,4-trien-16-yl]-N-(pyridin-2-ylmethyl)acetamide
Homo sapiens
-
0.00137
3'-(1-benzothien-2-yl)biphenyl-3-ol
Homo sapiens
37°C, pH not specified in the publication
0.00194
3'-(1-benzothien-2-yl)biphenyl-3-ol
Homo sapiens
37°C, pH not specified in the publication
0.00056
3'-(5-chloro-2-thienyl)biphenyl-3-ol
Homo sapiens
37°C, pH not specified in the publication
0.00237
3'-(5-chloro-2-thienyl)biphenyl-3-ol
Homo sapiens
37°C, pH not specified in the publication
0.000005
3-benzyl-8-hydroxy-2-(3,4,5-trimethoxyphenyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
Homo sapiens
-
0.000005
3-benzyl-8-hydroxy-2-(3,4,5-trimethoxyphenyl)[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
Homo sapiens
94% inhibition at 100 nM, 99% inhibition at 0.001 mM. IC50: 5 nM
0.00047
3-[2-(5-chloro-2-thienyl)pyridin-4-yl]phenol
Homo sapiens
37°C, pH not specified in the publication
0.00238
3-[2-(5-chloro-2-thienyl)pyridin-4-yl]phenol
Homo sapiens
37°C, pH not specified in the publication
0.00085
3-[4-(5-chloro-2-thienyl)pyridin-2-yl]phenol
Homo sapiens
37°C, pH not specified in the publication
0.00364
3-[4-(5-chloro-2-thienyl)pyridin-2-yl]phenol
Homo sapiens
37°C, pH not specified in the publication
0.00139
3-[6-(5-chloro-2-thienyl)pyridin-2-yl]phenol
Homo sapiens
37°C, pH not specified in the publication
0.00711
3-[6-(5-chloro-2-thienyl)pyridin-2-yl]phenol
Homo sapiens
37°C, pH not specified in the publication
0.00102
4'-(5-chloro-2-thienyl)biphenyl-3-ol
Homo sapiens
37°C, pH not specified in the publication
0.01
4'-(5-chloro-2-thienyl)biphenyl-3-ol
Homo sapiens
value higher than 0.01, 37°C, pH not specified in the publication
0.00069
4'-(6-methoxypyridin-3-yl)biphenyl-3-ol
Homo sapiens
37°C, pH not specified in the publication
0.00297
4'-(6-methoxypyridin-3-yl)biphenyl-3-ol
Homo sapiens
37°C, pH not specified in the publication
0.00041
(4aR,6aS,7S)-7-[heptyl(methyl)amino]-1,4a,6a-trimethylhexadecahydro-2H-indeno[5,4-f]quinolin-2-one
Homo sapiens
pH and temperature not specified in the publication
0.0006
(4aR,6aS,7S)-7-[heptyl(methyl)amino]-1,4a,6a-trimethylhexadecahydro-2H-indeno[5,4-f]quinolin-2-one
Homo sapiens
pH and temperature not specified in the publication, substrate: progesterone
0.00291
17beta-[(N-decyl)formamido]-4-methyl-4-aza-5alpha-androstan-3-one
Homo sapiens
pH 7.4, 37°C, reduction of estrone
-
0.00396
17beta-[(N-decyl)formamido]-4-methyl-4-aza-5alpha-androstan-3-one
Homo sapiens
pH 7.4, 37°C, reduction of dihydrotestosterone
-
0.00424
17beta-[(N-decyl)formamido]-4-methyl-4-aza-5alpha-androstan-3-one
Homo sapiens
pH 7.4, 37°C, reduction of progesterone
-
0.00578
17beta-[(N-heptyl)methylamino]-4-aza-5alpha-androstan-3-one
Homo sapiens
pH 7.4, 37°C, reduction of dihydrotestosterone
-
0.00601
17beta-[(N-heptyl)methylamino]-4-aza-5alpha-androstan-3-one
Homo sapiens
pH 7.4, 37°C, reduction of progesterone
-
0.00041
17beta-[(N-heptyl)methylamino]-4-methyl-4-aza-5alpha-androstan-3-one
Homo sapiens
pH 7.4, 37°C, reduction of estrone
-
0.0006
17beta-[(N-heptyl)methylamino]-4-methyl-4-aza-5alpha-androstan-3-one
Homo sapiens
pH 7.4, 37°C, reduction of progesterone
-
0.00119
17beta-[(N-heptyl)methylamino]-4-methyl-4-aza-5alpha-androstan-3-one
Homo sapiens
pH 7.4, 37°C, reduction of dihydrotestosterone
-
0.0007
17beta-[(N-nonyl)formamido]-4-methyl-4-aza-5alpha-androstan-3-one
Homo sapiens
pH 7.4, 37°C, reduction of estrone
-
0.00316
17beta-[(N-nonyl)formamido]-4-methyl-4-aza-5alpha-androstan-3-one
Homo sapiens
pH 7.4, 37°C, reduction of progesterone
-
0.00332
17beta-[(N-nonyl)formamido]-4-methyl-4-aza-5alpha-androstan-3-one
Homo sapiens
pH 7.4, 37°C, reduction of dihydrotestosterone
-
0.0103
2,2',4,4'-tetrahydroxybenzophenone
Homo sapiens
-
pH 7.4, 37°C
0.042
2,2',4,4'-tetrahydroxybenzophenone
Homo sapiens
-
pH 7.4, 37°C
0.017
3,3'-(1H-1,2,3-triazole-1,4-diyl)diphenol
Homo sapiens
-
-
0.017
3,3'-(1H-1,2,3-triazole-1,4-diyl)diphenol
Homo sapiens
-
37°C, pH not specified in the publication
0.006
3-benzylidene camphor
Homo sapiens
-
pH 7.4, 37°C
0.072
3-benzylidene camphor
Homo sapiens
-
pH 7.4, 37°C
0.00084
3-[1-(4-hydroxyphenyl)-1H-1,2,3-triazol-4-yl]phenol
Homo sapiens
-
-
0.00132
3-[1-(4-hydroxyphenyl)-1H-1,2,3-triazol-4-yl]phenol
Homo sapiens
-
-
0.00132
3-[1-(4-hydroxyphenyl)-1H-1,2,3-triazol-4-yl]phenol
Homo sapiens
-
37°C, pH not specified in the publication
40.88
3-[1-(4-hydroxyphenyl)-1H-1,2,3-triazol-4-yl]phenol
Homo sapiens
-
37°C, pH not specified in the publication
0.00084
3-[4-(4-hydroxyphenyl)-1H-1,2,3-triazol-1-yl]phenol
Homo sapiens
-
-
0.00084
3-[4-(4-hydroxyphenyl)-1H-1,2,3-triazol-1-yl]phenol
Homo sapiens
-
37°C, pH not specified in the publication
46.94
3-[4-(4-hydroxyphenyl)-1H-1,2,3-triazol-1-yl]phenol
Homo sapiens
-
37°C, pH not specified in the publication
0.00048
4'-hydroxy-N-(3-hydroxybenzyl)-N-methylbiphenyl-3-carboxamide
Homo sapiens
pH 7.4, 37°C
0.000482
4'-hydroxy-N-(3-hydroxybenzyl)-N-methylbiphenyl-3-carboxamide
Homo sapiens
pH 7.4, 37°C
0.0059
4-methylbenzylidene camphor
Homo sapiens
-
pH 7.4, 37°C
0.07
4-methylbenzylidene camphor
Homo sapiens
-
pH 7.4, 37°C
0.00009
estrone
Homo sapiens
-
92% inhibition at 0.001 mM, IC50: 0.00009 mM
0.0006 - 0.00081
estrone
Homo sapiens
-
IC50: 600-810 nM, depending on assay method
0.00016
N-(3-hydroxybenzyl)-N-methyl-5-(3-methylphenyl)thiophene-2-carboxamide
Homo sapiens
pH 7.4, 37°C
0.000164
N-(3-hydroxybenzyl)-N-methyl-5-(3-methylphenyl)thiophene-2-carboxamide
Homo sapiens
pH 7.4, 37°C
0.00291
N-decyl-N-[(4aR,6aS,7S)-1,4a,6a-trimethyl-2-oxohexadecahydro-1H-indeno[5,4-f]quinolin-7-yl]formamide
Homo sapiens
pH and temperature not specified in the publication, substrate: progesterone
0.00396
N-decyl-N-[(4aR,6aS,7S)-1,4a,6a-trimethyl-2-oxohexadecahydro-1H-indeno[5,4-f]quinolin-7-yl]formamide
Homo sapiens
pH and temperature not specified in the publication, substrate: progesterone
0.00112
N-decyl-N-[(4aR,6aS,7S)-4a,6a-dimethyl-2-oxohexadecahydro-1H-indeno[5,4-f]quinolin-7-yl]formamide
Homo sapiens
pH and temperature not specified in the publication
0.00578
N-decyl-N-[(4aR,6aS,7S)-4a,6a-dimethyl-2-oxohexadecahydro-1H-indeno[5,4-f]quinolin-7-yl]formamide
Homo sapiens
pH and temperature not specified in the publication, substrate: progesterone
0.0007
N-nonyl-N-[(4aR,6aS,7S)-1,4a,6a-trimethyl-2-oxohexadecahydro-1H-indeno[5,4-f]quinolin-7-yl]formamide
Homo sapiens
pH and temperature not specified in the publication
0.00332
N-nonyl-N-[(4aR,6aS,7S)-1,4a,6a-trimethyl-2-oxohexadecahydro-1H-indeno[5,4-f]quinolin-7-yl]formamide
Homo sapiens
pH and temperature not specified in the publication, substrate: progesterone
additional information
(2,4-dihydroxyphenyl)-phenylmethanone
Homo sapiens
-
value higher than 0.02, pH 7.4, 37°C
additional information
(2,4-dihydroxyphenyl)-phenylmethanone
Homo sapiens
-
value higher than 0.065, pH 7.4, 37°C
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Strickler, R.C.; Tobias, B.; Covey, D.F.
Human placental 17beta-estradiol dehydrogenase and 20alpha-hydroxysteroid dehydrogenase. Two activities at a single enzyme active site
J. Biol. Chem.
256
316-321
1981
Homo sapiens
brenda
Blomquist, C.H.; Lindemann, N.J.; Hakanson, E.Y.
17beta-Hydroxysteroid and 20alpha-hydroxysteroid dehydrogenase activities of human placental microsomes: kinetic evidence for two enzymes differing in substrate specificity
Arch. Biochem. Biophys.
239
206-215
1985
Homo sapiens
brenda
Murdock, G.L.; Warren, J.C.; Sweet, F.
Human placental estradiol 17beta-dehydrogenase: evidence for inverted substrate orientation (wrong-way binding) at the active site
Biochemistry
27
4452-4458
1988
Homo sapiens
brenda
Mendoza-Hernandez, G.; Lopez-Solache, I.; Diaz-Zagoya, J.C.
Periodate-oxidized NADP+ is a powerful inhibitor of human placental estradiol-17beta dehydrogenase
Biochem. Biophys. Res. Commun.
146
645-651
1987
Homo sapiens
brenda
Mendoza-Hernandez, G.; Rendon, J.L.; Diaz-Zagoya, J.C.
A single step procedure for purification of estradiol 17beta-dehydrogenase from human placenta
Biochem. Biophys. Res. Commun.
126
477-481
1985
Homo sapiens
brenda
Mendoza-Hernandez, G.; Calcagno, M.; Sanchez-Nuncio, H.R.; Diaz-Zagoya, J.C.
Dehydroepiandrosterone is a substrate for estradiol 17beta-dehydrogenase from human placenta
Biochem. Biophys. Res. Commun.
119
83-87
1984
Homo sapiens
brenda
Pollow, K.; Luebbert, H.; Pollow, B.
On the mitochondrial 17beta-hydroxysteroid dehydrogenase from human endometrium and endometrial carcinoma: characterization and intramitochondrial distribution
J. Steroid Biochem.
7
45-50
1976
Homo sapiens
brenda
Nicolas, J.C.
Purification of an enzyme containing a NADP-protected cysteine on organomercuri-agarose 17beta-estradiol dehydrogenase
Methods Enzymol.
34
552-554
1974
Homo sapiens
brenda
Nicolas, J.C.
The soluble 17beta-estradiol dehydrogenase of human placenta
Methods Enzymol.
34
555-557
1974
Homo sapiens
brenda
Nicolas, J.C.; Harris, J.I.
Human placental 17-oestradiol dehydrogenase. Sequence of a tryptic peptide containing an essential cysteine
FEBS Lett.
29
173-176
1973
Homo sapiens
brenda
Nicolas, J.C.; Pons, M.; Descomps, B.; de Paulet, A.C
Affinity chromatography: large-scale purification of the soluble oestradiol-17-dehydrogenase of human placenta
FEBS Lett.
23
175-179
1972
Homo sapiens
brenda
Burns, D.J.W.; Engel, L.L.; Bethune, J.L.
Amino acid composition and subunit structure. Human placental 17-estradiol dehydrogenase
Biochemistry
11
2699-2703
1972
Homo sapiens
brenda
Langer, L.J.; Alexander, J.A.; Engel, L.L.
Human placental estradiol-17beta dehydrogenase
J. Biol. Chem.
234
2609-2614
1959
Homo sapiens
brenda
Luebbert, H.
Effects of ethanol and other organic solvents on the kinetic behaviour of purified human placental oestradiol-17beta-dehydrogenase
Acta Endocrinol.
99
448-453
1982
Homo sapiens
brenda
Engel, L.L.; Inano, H.
Some kinetic properties of human placental 17beta-estradiol dehydrogenase: patterns of inhibition by adenine nucleotides
Adv. Enzyme Regul.
17
363-371
1979
Homo sapiens
brenda
Pollow, K.; Luebbert, H.; Jeske, R.; Pollow, B.
Studies on 17beta-hydroxysteroid dehydrogenase in human endometrium and endometrial carcinoma
Acta Endocrinol.
79
146-156
1975
Homo sapiens
brenda
Murdock, G.L.; Chin, C.C.; Warren, J.C.
Human placental estradiol 17beta-dehydrogenase: sequence of a histidine-bearing peptide in the catalytic region
Biochemistry
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Homo sapiens
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Homo sapiens
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1995
Homo sapiens
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Effect of retinoic acid and palm oil carotenoids on oestrone sulphatase and oestradiol-17beta hydroxysteroid dehydrogenase activities in MCF-7 and MDA-MB-231 breast cancer cell lines
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2000
Homo sapiens
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17beta-Estradiol dehydrogenase (E2DH) activity in T47D cells
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Oestradiol synthesis from oestrone in malignant breast epithelial cells: studies on a high affinity, 80 kDa form of oestradiol dehydrogenase
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Homo sapiens
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Sawicki, M.W.; Erman, M.; Puranen, T.; Vihko, P.; Ghosh, D.
Structure of the ternary complex of human 17beta-hydroxysteroid dehydrogenase type 1 with 3-hydroxyestra-1,3,5,7-tetraen-17-one (equilin) and NADP+
Proc. Natl. Acad. Sci. USA
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Homo sapiens (P14061), Homo sapiens
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Ghosh, D.; Pletnev, V.Z.; Zhu, D.W.; Wawrzak, Z.; Duax, W.L.; Pangborn, W.; Labrie, F.; Lin, S.X.
Structure of human estrogenic 17beta-hydroxysteroid dehydrogenase at 2.20 A resolution
Structure
3
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1995
Homo sapiens
brenda
Reed, M.J.; Rea, D.; Duncan, L.J.; Parker, M.G.
Regulation of estradiol 17beta-hydroxysteroid dehydrogenase expression and activity by retinoic acid in T47D breast cancer cells
Endocrinology
135
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1994
Homo sapiens
brenda
Puranen, T.J.; Poutanen, M.H.; Peltoketo, H.E.; Vihko, P.T.; Vihko, R.K.
Site-directed mutagenesis of the putative active site of human 17beta-hydroxysteroid dehydrogenase type 1
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Brown, W.M.; Metzger, L.E.; Barlow, J.P.; Hunsaker, L.A.; Deck, L.M.; Royer, R.E.; Vander Jagt, D.L.
17-beta-Hydroxysteroid dehydrogenase type 1: computational design of active site inhibitors targeted to the Rossmann fold
Chem. Biol. Interact.
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2003
Homo sapiens
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Qiu, W.; Campbell, R.L.; Gangloff, A.; Dupuis, P.; Boivin, R.P.; Tremblay, M.R.; Poirier, D.; Lin, S.X.
A concerted, rational design of type 1 17beta-hydroxysteroid dehydrogenase inhibitors: estradiol-adenosine hybrids with high affinity
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Homo sapiens (P14061), Homo sapiens
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Zhu, S.J.; Li, Y.; Li, H.; Wang, Y.L.; Xiao, Z.J.; Vihko, P.; Piao, Y.S.
Retinoic acids promote the action of aromatase and 17beta-hydroxysteroid dehydrogenase type 1 on the biosynthesis of 17beta-estradiol in placental cells
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2002
Homo sapiens
brenda
Fiorelli, G.; Picariello, L.; Martineti, V.; Tognarini, I.; Tonelli, F.; Brandi, M.L.
Estrogen metabolism in human colorectal cancer cells
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81
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2002
Homo sapiens
brenda
Blomquist, C.H.; Bonenfant, M.; McGinley, D.M.; Posalaky, Z.; Lakatua, D.J.; Tuli-Puri, S.; Bealka, D.G.; Tremblay, Y.
Androgenic and estrogenic 17beta-hydroxysteroid dehydrogenase/17-ketosteroid reductase in human ovarian epithelial tumors: evidence for the type 1, 2 and 5 isoforms
J. Steroid Biochem. Mol. Biol.
81
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2002
Homo sapiens
brenda
Steckelbroeck, S.; Watzka, M.; Reissinger, A.; Wegener-Toper, P.; Bidlingmaier, F.; Bliesener, N.; Hans, V.H.; Clusmann, H.; Ludwig, M.; Siekmann, L.; Klingmuller, D.
Characterisation of estrogenic 17beta-hydroxysteroid dehydrogenase (17beta-HSD) activity in the human brain
J. Steroid Biochem. Mol. Biol.
86
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2003
Homo sapiens
brenda
Khan, N.; Sharma, K.K.; Andersson, S.; Auchus, R.J.
Human 17beta-hydroxysteroid dehydrogenases types 1, 2, and 3 catalyze bi-directional equilibrium reactions, rather than unidirectional metabolism, in HEK-293 cells
Arch. Biochem. Biophys.
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2004
Homo sapiens
brenda
Poirier, D.
Inhibitors of 17beta-hydroxysteroid dehydrogenases
Curr. Med. Chem.
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2003
Homo sapiens
brenda
Li, Y.; Qin, L.; Xiao, Z.J.; Wang, Y.L.; Herva, R.; Leng, J.H.; Lang, J.H.; Isomaa, V.; Piao, Y.S.
Expression of P450 aromatase and 17beta-hydroxysteroid dehydrogenase type 1 at fetal-maternal interface during tubal pregnancy
J. Steroid Biochem. Mol. Biol.
87
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2003
Homo sapiens
brenda
Nakanishi, T.; Hiromori, Y.; Yokoyama, H.; Koyanagi, M.; Itoh, N.; Nishikawa, J.; Tanaka, K.
Organotin compounds enhance 17beta-hydroxysteroid dehydrogenase type I activity in human choriocarcinoma JAr cells: potential promotion of 17beta-estradiol biosynthesis in human placenta
Biochem. Pharmacol.
71
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2006
Homo sapiens
brenda
Vicker, N.; Lawrence, H.R.; Allan, G.M.; Bubert, C.; Smith, A.; Tutill, H.J.; Purohit, A.; Day, J.M.; Mahon, M.F.; Reed, M.J.; Potter, B.V.
Focused libraries of 16-substituted estrone derivatives and modified e-ring steroids: inhibitors of 17beta-hydroxysteroid dehydrogenase type 1
ChemMedChem
1
464-481
2006
Homo sapiens
brenda
Husen, B.; Huhtinen, K.; Saloniemi, T.; Messinger, J.; Thole, H.H.; Poutanen, M.
Human hydroxysteroid (17-beta) dehydrogenase 1 expression enhances estrogen sensitivity of MCF-7 breast cancer cell xenografts
Endocrinology
147
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2006
Homo sapiens
brenda
Tremblay, M.R.; Boivin, R.P.; Luu-The, V.; Poirier, D.
Inhibitors of type 1 17beta-hydroxysteroid dehydrogenase with reduced estrogenic activity: modifications of the positions 3 and 6 of estradiol
J. Enzyme Inhib. Med. Chem.
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2005
Homo sapiens
brenda
Fischer, D.S.; Allan, G.M.; Bubert, C.; Vicker, N.; Smith, A.; Tutill, H.J.; Purohit, A.; Wood, L.; Packham, G.; Mahon, M.F.; Reed, M.J.; Potter, B.V.
E-ring modified steroids as novel potent inhibitors of 17beta-hydroxysteroid dehydrogenase type 1
J. Med. Chem.
48
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2005
Homo sapiens
brenda
Poirier, D.; Boivin, R.P.; Tremblay, M.R.; Berube, M.; Qiu, W.; Lin, S.X.
Estradiol-adenosine hybrid compounds designed to inhibit type 1 17beta-hydroxysteroid dehydrogenase
J. Med. Chem.
48
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2005
Homo sapiens
brenda
Song, D.; Liu, G.; Luu-The, V.; Zhao, D.; Wang, L.; Zhang, H.; Xueling, G.; Li, S.; Desy, L.; Labrie, F.; Pelletier, G.
Expression of aromatase and 17beta-hydroxysteroid dehydrogenase types 1, 7 and 12 in breast cancer. An immunocytochemical study
J. Steroid Biochem. Mol. Biol.
101
136-144
2006
Homo sapiens
brenda
Liu, H.; Robert, A.; Luu-The, V.
Cloning and characterization of human form 2 type 7 17beta-hydroxysteroid dehydrogenase, a primarily 3beta-keto reductase and estrogen activating and androgen inactivating enzyme
J. Steroid Biochem. Mol. Biol.
94
173-179
2005
Homo sapiens (Q5MGS6)
brenda
Brooks, J.D.; Thompson, L.U.
Mammalian lignans and genistein decrease the activities of aromatase and 17beta-hydroxysteroid dehydrogenase in MCF-7 cells
J. Steroid Biochem. Mol. Biol.
94
461-467
2005
Homo sapiens
brenda
Otsuka, M.; Kato, N.; Ichimura, T.; Abe, S.; Tanaka, Y.; Taniguchi, H.; Hoshida, Y.; Moriyama, M.; Wang, Y.; Shao, R.X.; Narayan, D.; Muroyama, R.; Kanai, F.; Kawabe, T.; Isobe, T.; Omata, M.
Vitamin K2 binds 17beta-hydroxysteroid dehydrogenase 4 and modulates estrogen metabolism
Life Sci.
76
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2005
Homo sapiens
brenda
Messinger, J.; Hirvelae, L.; Husen, B.; Kangas, L.; Koskimies, P.; Pentikaeinen, O.; Saarenketo, P.; Thole, H.
New inhibitors of 17beta-hydroxysteroid dehydrogenase type 1
Mol. Cell. Endocrinol.
248
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2006
Homo sapiens (P14061), Homo sapiens
brenda
Purohit, A.; Tutill, H.J.; Day, J.M.; Chander, S.K.; Lawrence, H.R.; Allan, G.M.; Fischer, D.S.; Vicker, N.; Newman, S.P.; Potter, B.V.; Reed, M.J.
The regulation and inhibition of 17beta-hydroxysteroid dehydrogenase in breast cancer
Mol. Cell. Endocrinol.
248
199-203
2006
Homo sapiens
brenda
Allan, G.M.; Bubert, C.; Vicker, N.; Smith, A.; Tutill, H.J.; Purohit, A.; Reed, M.J.; Potter, B.V.
Novel, potent inhibitors of 17beta-hydroxysteroid dehydrogenase type 1
Mol. Cell. Endocrinol.
248
204-207
2006
Homo sapiens (P14061)
brenda
Alho-Richmond, S.; Lilienkampf, A.; Waehaelae, K.
Active site analysis of 17beta-hydroxysteroid dehydrogenase type 1 enzyme complexes with SPROUT
Mol. Cell. Endocrinol.
248
208-213
2006
Homo sapiens (P14061)
brenda
Poirier, D.; Chang, H.J.; Azzi, A.; Boivin, R.P.; Lin, S.X.
Estrone and estradiol C-16 derivatives as inhibitors of type 1 17beta-hydroxysteroid dehydrogenase
Mol. Cell. Endocrinol.
248
236-238
2006
Homo sapiens (P14061)
brenda
Day, J.M.; Tutill, H.J.; Newman, S.P.; Purohit, A.; Lawrence, H.R.; Vicker, N.; Potter, B.V.; Reed, M.J.
17beta-Hydroxysteroid dehydrogenase type 1 and type 2: association between mRNA expression and activity in cell lines
Mol. Cell. Endocrinol.
248
246-249
2006
Homo sapiens
brenda
Lin, S.X.; Shi, R.; Qiu, W.; Azzi, A.; Zhu, D.W.; Dabbagh, H.A.; Zhou, M.
Structural basis of the multispecificity demonstrated by 17beta-hydroxysteroid dehydrogenase types 1 and 5
Mol. Cell. Endocrinol.
248
38-46
2006
Homo sapiens
brenda
Luu-The, V.; Tremblay, P.; Labrie, F.
Characterization of type 12 17beta-hydroxysteroid dehydrogenase, an isoform of type 3 17beta-hydroxysteroid dehydrogenase responsible for estradiol formation in women
Mol. Endocrinol.
20
437-443
2006
Homo sapiens (Q53GQ0), Homo sapiens
brenda
Nagayoshi, Y.; Ohba, T.; Yamamoto, H.; Miyahara, Y.; Tashiro, H.; Katabuchi, H.; Okamura, H.
Characterization of 17beta-hydroxysteroid dehydrogenase type 4 in human ovarian surface epithelial cells
Mol. Hum. Reprod.
11
615-621
2005
Homo sapiens
brenda
Brozic, P.; Golob, B.; Gomboc, N.; Rizner, T.L.; Gobec, S.
Cinnamic acids as new inhibitors of 17beta-hydroxysteroid dehydrogenase type 5 (AKR1C3)
Mol. Cell. Endocrinol.
248
233-235
2006
Homo sapiens
brenda
Moeller, G.; Adamski, J.
Multifunctionality of human 17beta-hydroxysteroid dehydrogenases
Mol. Cell. Endocrinol.
248
47-55
2006
Homo sapiens
brenda
Lukacik, P.; Kavanagh, K.L.; Oppermann, U.
Structure and function of human 17beta-hydroxysteroid dehydrogenases
Mol. Cell. Endocrinol.
248
61-71
2006
Homo sapiens
brenda
Laplante, Y.; Cadot, C.; Fournier, M.A.; Poirier, D.
Estradiol and estrone C-16 derivatives as inhibitors of type 1 17beta-hydroxysteroid dehydrogenase: blocking of ER+ breast cancer cell proliferation induced by estrone
Bioorg. Med. Chem.
16
1849-1860
2008
Homo sapiens (P14061), Homo sapiens
brenda
Allan, G.M.; Vicker, N.; Lawrence, H.R.; Tutill, H.J.; Day, J.M.; Huchet, M.; Ferrandis, E.; Reed, M.J.; Purohit, A.; Potter, B.V.
Novel inhibitors of 17beta-hydroxysteroid dehydrogenase type 1: templates for design
Bioorg. Med. Chem.
16
4438-4456
2008
Homo sapiens, Homo sapiens (P14061)
brenda
Bey, E.; Marchais-Oberwinkler, S.; Kruchten, P.; Frotscher, M.; Werth, R.; Oster, A.; Alguel, O.; Neugebauer, A.; Hartmann, R.W.
Design, synthesis and biological evaluation of bis(hydroxyphenyl) azoles as potent and selective non-steroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent diseases
Bioorg. Med. Chem.
16
6423-6435
2008
Homo sapiens, Homo sapiens (P14061)
brenda
Brozic, P.; Lanisnik Risner, T.; Gobec, S.
Inhibitors of 17beta-hydroxysteroid dehydrogenase type 1
Curr. Med. Chem.
15
137-150
2008
Homo sapiens (P14061)
brenda
Bydal, P.; Luu-The, V.; Labrie, F.; Poirier, D.
Steroidal lactones as inhibitors of 17beta-hydroxysteroid dehydrogenase type 5: Chemical synthesis, enzyme inhibitory activity, and assessment of estrogenic and androgenic activities
Eur. J. Med. Chem.
44
632-644
2008
Homo sapiens
brenda
Day, J.M.; Foster, P.A.; Tutill, H.J.; Parsons, M.F.; Newman, S.P.; Chander, S.K.; Allan, G.M.; Lawrence, H.R.; Vicker, N.; Potter, B.V.; Reed, M.J.; Purohit, A.
17beta-Hydroxysteroid dehydrogenase type 1, and not type 12, is a target for endocrine therapy of hormone-dependent breast cancer
Int. J. Cancer
122
1931-1940
2008
Homo sapiens (P14061), Homo sapiens
brenda
Frotscher, M.; Ziegler, E.; Marchais-Oberwinkler, S.; Kruchten, P.; Neugebauer, A.; Fetzer, L.; Scherer, C.; Mueller-Vieira, U.; Messinger, J.; Thole, H.; Hartmann, R.W.
Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent disease
J. Med. Chem.
51
2158-2169
2008
Homo sapiens (P14061)
brenda
Luu-The, V.; Ferraris, C.; Duche, D.; Belanger, P.; Leclaire, J.; Labrie, F.
Steroid metabolism and profile of steroidogenic gene expression in Episkin: high similarity with human epidermis
J. Steroid Biochem. Mol. Biol.
107
30-36
2007
Homo sapiens
brenda
Ohno, S.; Nishikawa, K.; Honda, Y.; Nakajin, S.
Expression in E. coli and tissue distribution of the human homologue of the mouse Ke 6 gene, 17beta-hydroxysteroid dehydrogenase type 8
Mol. Cell. Biochem.
309
209-215
2008
Homo sapiens
brenda
Saloniemi, T.; Lamminen, T.; Huhtinen, K.; Welsh, M.; Saunders, P.; Kujari, H.; Poutanen, M.
Activation of androgens by hydroxysteroid (17beta) dehydrogenase 1 in vivo as a cause of prenatal masculinization and ovarian benign serous cystadenomas
Mol. Endocrinol.
21
2627-2636
2007
Homo sapiens (P14016)
brenda
Fournier, D.; Poirier, D.; Mazumdar, M.; Lin, S.X.
Design and synthesis of bisubstrate inhibitors of type 1 17beta-hydroxysteroid dehydrogenase: overview and perspectives
Eur. J. Med. Chem.
43
2298-2306
2008
Homo sapiens (P14061)
brenda
Marchais-Oberwinkler, S.; Kruchten, P.; Frotscher, M.; Ziegler, E.; Neugebauer, A.; Bhoga, U.; Bey, E.; Mueller-Vieira, U.; Messinger, J.; Thole, H.; Hartmann, R.W.
Substituted 6-phenyl-2-naphthols. Potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1): design, synthesis, biological evaluation, and pharmacokinetics
J. Med. Chem.
51
4685-4698
2008
Homo sapiens (P14061)
brenda
El-Kabbani, O.; Scammells, P.J.; Gosling, J.; Dhagat, U.; Endo, S.; Matsunaga, T.; Soda, M.; Hara, A.
Structure-guided design, synthesis, and evaluation of salicylic acid-based inhibitors targeting a selectivity pocket in the active site of human 20alpha-hydroxysteroid dehydrogenase (AKR1C1)
J. Med. Chem.
52
3259-3264
2009
Homo sapiens
brenda
Bellemare, V.; Laberge, P.; Noel, S.; Tchernof, A.; Luu-The, V.
Differential estrogenic 17beta-hydroxysteroid dehydrogenase activity and type 12 17beta-hydroxysteroid dehydrogenase expression levels in preadipocytes and differentiated adipocytes
J. Steroid Biochem. Mol. Biol.
114
129-134
2009
Homo sapiens
brenda
Kruchten, P.; Werth, R.; Bey, E.; Oster, A.; Marchais-Oberwinkler, S.; Frotscher, M.; Hartmann, R.W.
Selective inhibition of 17beta-hydroxysteroid dehydrogenase type 1 (17betaHSD1) reduces estrogen responsive cell growth of T47-D breast cancer cells
J. Steroid Biochem. Mol. Biol.
114
200-206
2009
Homo sapiens
brenda
Al-Soud, Y.A.; Bey, E.; Oster, A.; Marchais-Oberwinkler, S.; Werth, R.; Kruchten, P.; Frotscher, M.; Hartmann, R.W.
The role of the heterocycle in bis(hydroxyphenyl)triazoles for inhibition of 17beta-hydroxysteroid dehydrogenase (17beta-HSD) type 1 and type 2
Mol. Cell. Endocrinol.
301
212-215
2009
Homo sapiens
brenda
Messinger, J.; Husen, B.; Koskimies, P.; Hirvelae, L.; Kallio, L.; Saarenketo, P.; Thole, H.
Estrone C15 derivatives--a new class of 17beta-hydroxysteroid dehydrogenase type 1 inhibitors
Mol. Cell. Endocrinol.
301
216-224
2009
Homo sapiens (P14061), Homo sapiens
brenda
Karkola, S.; Alho-Richmond, S.; Wahala, K.
Pharmacophore modelling of 17beta-HSD1 enzyme based on active inhibitors and enzyme structure
Mol. Cell. Endocrinol.
301
225-228
2009
Homo sapiens (P14061)
brenda
Brozic, P.; Kocbek, P.; Sova, M.; Kristl, J.; Martens, S.; Adamski, J.; Gobec, S.; Lanisnik Rizner, T.
Flavonoids and cinnamic acid derivatives as inhibitors of 17beta-hydroxysteroid dehydrogenase type 1
Mol. Cell. Endocrinol.
301
229-234
2009
Homo sapiens (P14061)
brenda
Nashev, L.G.; Schuster, D.; Laggner, C.; Sodha, S.; Langer, T.; Wolber, G.; Odermatt, A.
The UV-filter benzophenone-1 inhibits 17beta-hydroxysteroid dehydrogenase type 3: Virtual screening as a strategy to identify potential endocrine disrupting chemicals
Biochem. Pharmacol.
79
1189-1199
2010
Homo sapiens
brenda
Oster, A.; Klein, T.; Werth, R.; Kruchten, P.; Bey, E.; Negri, M.; Marchais-Oberwinkler, S.; Frotscher, M.; Hartmann, R.W.
Novel estrone mimetics with high 17beta-HSD1 inhibitory activity
Bioorg. Med. Chem.
18
3494-3505
2010
Homo sapiens (P14061)
brenda
Chanplakorn, N.; Chanplakorn, P.; Suzuki, T.; Ono, K.; Chan, M.; Miki, Y.; Saji, S.; Ueno, T.; Toi, M.; Sasano, H.
Increased estrogen sulfatase (STS) and 17hydroxysteroid dehydrogenase type l(17-HSD1) following neoadjuvant aromatase inhibitor therapy in breast cancer patients
Breast Cancer Res. Treat.
120
639-648
2010
Homo sapiens
brenda
Hong, Y.; Chen, S.
Aromatase, estrone sulfatase, and 17beta-hydroxysteroid dehydrogenase: Structure-function studies and inhibitor development
Mol. Cell. Endocrinol.
340
120-126
2011
Homo sapiens
brenda
Negri, M.; Recanatini, M.; Hartmann, R.W.
Insights in 17beta-HSD1 enzyme kinetics and ligand binding by dynamic motion investigation
PLoS ONE
5
e12026
2010
Homo sapiens (P14061)
brenda
Starcevic, S.; Brozic, P.; Turk, S.; Cesar, J.; Lanisnik Rizner, T.; Gobec, S.
Synthesis and biological evaluation of (6- and 7-Phenyl) coumarin derivatives as selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1
J. Med. Chem.
54
248-261
2011
Homo sapiens (P14061)
brenda
Beranic, N.; Rizner, T.L.
Effects of progestins on local estradiol biosynthesis and action in the Z-12 endometriotic epithelial cell line
J. Steroid Biochem. Mol. Biol.
132
303-310
2012
Homo sapiens (P14061), Homo sapiens (P37059), Homo sapiens
brenda
Spadaro, A.; Negri, M.; Marchais-Oberwinkler, S.; Bey, E.; Frotscher, M.
Hydroxybenzothiazoles as new nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1)
PLoS ONE
7
e29252
2012
Homo sapiens (P14061)
brenda
Zhang, C.; Chen, J.; Yin, D.; Lin, S.
The contribution of 17beta-hydroxysteroid dehydrogenase type 1 to the estradiol-estrone ratio in estrogen-sensitive breast cancer cells
PLoS ONE
7
e29835
2012
Homo sapiens (P14061), Homo sapiens (P37059)
brenda
Sivik, T.; Gunnarsson, C.; Fornander, T.; Nordenskjoeld, B.; Skoog, L.; Stal, O.; Jansson, A.
17beta-Hydroxysteroid dehydrogenase type 14 is a predictive marker for tamoxifen response in oestrogen receptor positive breast cancer
PLoS ONE
7
e40568
2012
Homo sapiens (Q9BPX1)
brenda
Muthusamy, S.; Andersson, S.; Kim, H.J.; Butler, R.; Waage, L.; Bergerheim, U.; Gustafsson, J.A.
Estrogen receptor beta and 17beta-hydroxysteroid dehydrogenase type 6, a growth regulatory pathway that is lost in prostate cancer
Proc. Natl. Acad. Sci. USA
108
20090-20094
2011
Homo sapiens (O14756)
brenda
Strugala, A.J.; Jagodzinski, P.P.
Conversion of estrone to 17 beta-estradiol in Jurkat acute T cell leukemia Hut-78 T- and Raji B lymphoma cell lines in vitro
Biomed. Pharmacother.
67
299-303
2013
Homo sapiens (P14061)
brenda
Perspicace, E.; Giorgio, A.; Carotti, A.; Marchais-Oberwinkler, S.; Hartmann, R.W.
Novel N-methylsulfonamide and retro-N-methylsulfonamide derivatives as 17beta-hydroxysteroid dehydrogenase type 2 (17beta-HSD2) inhibitors with good ADME-related physicochemical parameters
Eur. J. Med. Chem.
69
201-215
2013
Homo sapiens (P14061), Homo sapiens (P37059)
brenda
Maltais, R.; Trottier, A.; Delhomme, A.; Barbeau, X.; Laguee, P.; Poirier, D.
Identification of fused 16beta,17beta-oxazinone-estradiol derivatives as a new family of non-estrogenic 17beta-hydroxysteroid dehydrogenase type 1 inhibitors
Eur. J. Med. Chem.
93
470-480
2015
Homo sapiens (P14061)
brenda
Nashev, L.; Atanasov, A.; Baker, M.; Odermatt, A.
Cysteine-10 on 17beta-hydroxysteroid dehydrogenase 1 has stabilizing interactions in the cofactor binding region and renders sensitivity to sulfhydryl modifying chemicals
Int. J. Cell Biol.
2013
769536
2013
Homo sapiens (P14061)
brenda
Weber, S.; Salabei, J.K.; Moeller, G.; Kremmer, E.; Bhatnagar, A.; Adamski, J.; Barski, O.A.
Aldo-keto Reductase 1B15 (AKR1B15): a mitochondrial human aldo-keto reductase with activity toward steroids and 3-keto-acyl-CoA conjugates
J. Biol. Chem.
290
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Homo sapiens (C9JRZ8)
brenda
Herman, B.E.; Szabo, J.; Bacsa, I.; Woelfling, J.; Schneider, G.; Balint, M.; Hetenyi, C.; Mernyak, E.; Szecsi, M.
Comparative investigation of the in vitro inhibitory potencies of 13-epimeric estrones and D-secoestrones towards 17beta-hydroxysteroid dehydrogenase type 1
J. Enzyme Inhib. Med. Chem.
36 (Suppl.3)
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2016
Homo sapiens (P14061)
brenda
Maltais, R.; Ayan, D.; Trottier, A.; Barbeau, X.; Laguee, P.; Bouchard, J.E.; Poirier, D.
Discovery of a non-estrogenic irreversible inhibitor of 17beta-hydroxysteroid dehydrogenase type 1 from 3-substituted-16beta-(m-carbamoylbenzyl)-estradiol derivatives
J. Med. Chem.
57
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2014
Homo sapiens
brenda
Vuorinen, A.; Engeli, R.; Meyer, A.; Bachmann, F.; Griesser, U.J.; Schuster, D.; Odermatt, A.
Ligand-based pharmacophore modeling and virtual screening for the discovery of novel 17beta-hydroxysteroid dehydrogenase 2 inhibitors
J. Med. Chem.
57
5995-6007
2014
Homo sapiens (P37059)
brenda
Bertoletti, N.; Braun, F.; Lepage, M.; Moeller, G.; Adamski, J.; Heine, A.; Klebe, G.; Marchais-Oberwinkler, S.
New insights into human 17beta-hydroxysteroid dehydrogenase type 14: first crystal structures in complex with a steroidal ligand and with a potent nonsteroidal inhibitor
J. Med. Chem.
59
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2016
Homo sapiens (Q9BPX1)
brenda
Verma, M.; Miki, Y.; Abe, K.; Suzuki, T.; Niikawa, H.; Suzuki, S.; Kondo, T.; Sasano, H.
Intratumoral localization and activity of 17beta-hydroxysteroid dehydrogenase type 1 in non-small cell lung cancer: A potent prognostic factor
J. Transl. Med.
11
167-177
2013
Homo sapiens (P14061)
brenda
Gargano, E.M.; Allegretta, G.; Perspicace, E.; Carotti, A.; Van Koppen, C.; Frotscher, M.; Marchais-Oberwinkler, S.; Hartmann, R.W.
17beta-Hydroxysteroid dehydrogenase type 2 inhibition: discovery of selective and metabolically stable compounds inhibiting both the human enzyme and its murine ortholog
PLoS ONE
10
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2015
Homo sapiens (P37059), Mus musculus (P51658)
brenda
Salah, M.; Abdelsamie, A.S.; Frotscher, M.
First dual inhibitors of steroid sulfatase (STS) and 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) designed multiple ligands as novel potential therapeutics for estrogen-dependent diseases
J. Med. Chem.
60
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2017
Homo sapiens (P14061)
brenda
Trottier, A.; Maltais, R.; Ayan, D.; Barbeau, X.; Roy, J.; Perreault, M.; Poulin, R.; Laguee, P.; Poirier, D.
Insight into the mode of action and selectivity of PBRM, a covalent steroidal inhibitor of 17beta-hydroxysteroid dehydrogenase type 1
Biochem. Pharmacol.
144
149-161
2017
Homo sapiens (P14061)
brenda
Ferrante, T.; Adinolfi, S.; DArrigo, G.; Poirier, D.; Daga, M.; Lolli, M.L.; Balliano, G.; Spyrakis, F.; Oliaro-Bosso, S.
Multiple catalytic activities of human 17beta-hydroxysteroid dehydrogenase type 7 respond differently to inhibitors
Biochimie
170
106-117
2020
Homo sapiens (P56937)
brenda
Boutin, S.; Roy, J.; Maltais, R.; Alata, W.; Calon, F.; Poirier, D.
Identification of steroidal derivatives inhibiting the transformations of allopregnanolone and estradiol by 17beta-hydroxysteroid dehydrogenase type 10
Bioorg. Med. Chem. Lett.
28
3554-3559
2018
Homo sapiens (Q99714)
brenda
Boutin, S.; Maltais, R.; Roy, J.; Poirier, D.
Synthesis of 17beta-hydroxysteroid dehydrogenase type 10 steroidal inhibitors selectivity, metabolic stability and enhanced potency
Eur. J. Med. Chem.
209
112909
2021
Homo sapiens
brenda
Li, T.; Stephen, P.; Zhu, D.W.; Shi, R.; Lin, S.X.
Crystal structures of human 17beta-hydroxysteroid dehydrogenase type 1 complexed with estrone and NADP+ reveal the mechanism of substrate inhibition
FEBS J.
286
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2019
Homo sapiens (P14061)
brenda
Theriault, J.F.; Lin, S.X.
The dual sex hormone specificity for human reductive 17beta-hydroxysteroid dehydrogenase type 7 Synergistic function in estrogen and androgen control
J. Steroid Biochem. Mol. Biol.
186
61-65
2019
Homo sapiens (P56937)
brenda
Aka, J.; Calvo, E.; Lin, S.
Estradiol-independent modulation of breast cancer transcript profile by 17beta-hydroxysteroid dehydrogenase type 1
Mol. Cell. Endocrinol.
439
175-186
2017
Homo sapiens (P14061)
brenda
Salah, M.; Abdelsamie, A.S.; Frotscher, M.
Inhibitors of 17?-hydroxysteroid dehydrogenase type 1, 2 and 14 Structures, biological activities and future challenges
Mol. Cell. Endocrinol.
489
66-81
2019
Homo sapiens (P14061), Homo sapiens (P37059)
brenda
Penning, T.M.
AKR1C3 (type 5 17beta-hydroxysteroid dehydrogenase/prostaglandin F synthase) Roles in malignancy and endocrine disorders
Mol. Cell. Endocrinol.
489
82-91
2019
Homo sapiens (P42330)
brenda
Hilborn, E.; Stal, O.; Jansson, A.
Estrogen and androgen-converting enzymes 17beta-hydroxysteroid dehydrogenase and their involvement in cancer with a special focus on 17beta-hydroxysteroid dehydrogenase type 1, 2, and breast cancer
Oncotarget
8
30552-30562
2017
Homo sapiens (P14061), Homo sapiens (P37059)
brenda
Hilborn, E.; Stal, O.; Alexeyenko, A.; Jansson, A.
The regulation of hydroxysteroid 17beta-dehydrogenase type 1 and 2 gene expression in breast cancer cell lines by estradiol, dihydrotestosterone, microRNAs, and genes related to breast cancer
Oncotarget
8
62183-62194
2017
Homo sapiens (P37059)
brenda
Liu, J.; He, P.; Lin, L.; Zhao, Y.; Deng, W.; Ding, H.; Li, Q.; Wang, Z.
Characterization of a highly specific monoclonal antibody against human aldo-keto reductase AKR1C3
Steroids
143
73-79
2019
Homo sapiens (P42330), Homo sapiens
brenda
Sali, V.K.; Mani, S.; Meenaloshani, G.; Velmurugan Ilavarasi, A.; Vasanthi, H.R.
Type 5 17-hydroxysteroid dehydrogenase/prostaglandin F synthase (AKR1C3) inhibition and potential anti-proliferative activity of cholest-4-ene-3,6-dione in MCF-7 breast cancer cells
Steroids
159
108638
2020
Homo sapiens (P42330)
brenda