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Literature summary extracted from

  • Bell, A.S.; Mills, J.E.; Williams, G.P.; Brannigan, J.A.; Wilkinson, A.J.; Parkinson, T.; Leatherbarrow, R.J.; Tate, E.W.; Holder, A.A.; Smith, D.F.
    Selective inhibitors of protozoan protein N-myristoyltransferases as starting points for tropical disease medicinal chemistry programs (2012), PLoS Negl. Trop. Dis., 6, e1625.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.3.1.97 sequence comparisons Homo sapiens
2.3.1.97 sequence comparisons Leishmania donovani
2.3.1.97 sequence comparisons Plasmodium falciparum
2.3.1.97 sequence comparisons Trypanosoma brucei

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.1.97 (2S)-N-(2-cyclohexylethyl)-2-[[N-([3-[4-(2-methyl-1H-imidazol-1-yl)butyl]phenyl]acetyl)-L-seryl]amino]heptanamide
-
 Leishmania donovani
2.3.1.97 (2S)-N-(2-cyclohexylethyl)-2-[[N-([3-[4-(2-methyl-1H-imidazol-1-yl)butyl]phenyl]acetyl)-L-seryl]amino]heptanamide
-
 Plasmodium falciparum
2.3.1.97 (2S)-N-(2-cyclohexylethyl)-2-[[N-([3-[4-(2-methyl-1H-imidazol-1-yl)butyl]phenyl]acetyl)-L-seryl]amino]heptanamide
-
 Trypanosoma brucei
2.3.1.97 (3R)-3-amino-4-(4-chlorophenyl)-1-[(3R,4S)-3-(hydroxymethyl)-4-(4-methoxyphenyl)pyrrolidin-1-yl]butan-1-one
-
 Homo sapiens
2.3.1.97 (3R)-3-amino-4-(4-chlorophenyl)-1-[(3R,4S)-3-(hydroxymethyl)-4-(4-methoxyphenyl)pyrrolidin-1-yl]butan-1-one
-
 Leishmania donovani
2.3.1.97 (3R)-3-amino-4-(4-chlorophenyl)-1-[(3R,4S)-3-(hydroxymethyl)-4-(4-methoxyphenyl)pyrrolidin-1-yl]butan-1-one
-
 Plasmodium falciparum
2.3.1.97 (3R)-3-amino-4-(4-chlorophenyl)-1-[(3R,4S)-3-(hydroxymethyl)-4-(4-methoxyphenyl)pyrrolidin-1-yl]butan-1-one
-
 Trypanosoma brucei
2.3.1.97 (3R)-3-amino-4-(4-chlorophenyl)-1-[(3S,4R)-3-(4-chlorophenyl)-4-(hydroxymethyl)pyrrolidin-1-yl]butan-1-one
-
 Homo sapiens
2.3.1.97 (3R)-3-amino-4-(4-chlorophenyl)-1-[(3S,4R)-3-(4-chlorophenyl)-4-(hydroxymethyl)pyrrolidin-1-yl]butan-1-one
-
 Leishmania donovani
2.3.1.97 (3R)-3-amino-4-(4-chlorophenyl)-1-[(3S,4R)-3-(4-chlorophenyl)-4-(hydroxymethyl)pyrrolidin-1-yl]butan-1-one
-
 Plasmodium falciparum
2.3.1.97 (3R)-3-amino-4-(4-chlorophenyl)-1-[(3S,4R)-3-(4-chlorophenyl)-4-(hydroxymethyl)pyrrolidin-1-yl]butan-1-one
-
 Trypanosoma brucei
2.3.1.97 1-(5-chloro-2-[[2-(dimethylamino)ethyl]amino]pyrimidin-4-yl)-N-(2,4-difluorobenzyl)azetidine-3-carboxamide
-
 Homo sapiens
2.3.1.97 1-(5-chloro-2-[[2-(dimethylamino)ethyl]amino]pyrimidin-4-yl)-N-(2,4-difluorobenzyl)azetidine-3-carboxamide
-
 Leishmania donovani
2.3.1.97 1-(5-chloro-2-[[2-(dimethylamino)ethyl]amino]pyrimidin-4-yl)-N-(2,4-difluorobenzyl)azetidine-3-carboxamide
-
 Plasmodium falciparum
2.3.1.97 1-(5-chloro-2-[[2-(dimethylamino)ethyl]amino]pyrimidin-4-yl)-N-(2,4-difluorobenzyl)azetidine-3-carboxamide
-
 Trypanosoma brucei
2.3.1.97 1-(5-chloro-2-[[2-(dimethylamino)ethyl]amino]pyrimidin-4-yl)-N-[(5-methylpyrazin-2-yl)methyl]azetidine-3-carboxamide
-
 Homo sapiens
2.3.1.97 1-(5-chloro-2-[[2-(dimethylamino)ethyl]amino]pyrimidin-4-yl)-N-[(5-methylpyrazin-2-yl)methyl]azetidine-3-carboxamide
-
 Leishmania donovani
2.3.1.97 1-(5-chloro-2-[[2-(dimethylamino)ethyl]amino]pyrimidin-4-yl)-N-[(5-methylpyrazin-2-yl)methyl]azetidine-3-carboxamide
-
 Plasmodium falciparum
2.3.1.97 1-(5-chloro-2-[[2-(dimethylamino)ethyl]amino]pyrimidin-4-yl)-N-[(5-methylpyrazin-2-yl)methyl]azetidine-3-carboxamide
-
 Trypanosoma brucei
2.3.1.97 2,6-dichloro-4-[2-(piperazin-1-yl)pyridin-4-yl]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzenesulfonamide
-
 Leishmania donovani
2.3.1.97 2,6-dichloro-4-[2-(piperazin-1-yl)pyridin-4-yl]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzenesulfonamide
-
 Trypanosoma brucei
2.3.1.97 2-(4-fluorophenyl)-N-[3-(piperidin-4-yl)-1H-indol-5-yl]acetamide
-
 Homo sapiens
2.3.1.97 2-(4-fluorophenyl)-N-[3-(piperidin-4-yl)-1H-indol-5-yl]acetamide
-
 Leishmania donovani
2.3.1.97 2-(4-fluorophenyl)-N-[3-(piperidin-4-yl)-1H-indol-5-yl]acetamide
-
 Plasmodium falciparum
2.3.1.97 2-(4-fluorophenyl)-N-[3-(piperidin-4-yl)-1H-indol-5-yl]acetamide
-
 Trypanosoma brucei
2.3.1.97 2-([[trans-4-(aminomethyl)cyclohexyl]carbonyl]amino)-N,N-dimethyl-1,3-benzothiazole-6-carboxamide
-
 Leishmania donovani
2.3.1.97 2-([[trans-4-(aminomethyl)cyclohexyl]carbonyl]amino)-N,N-dimethyl-1,3-benzothiazole-6-carboxamide
-
 Plasmodium falciparum
2.3.1.97 2-([[trans-4-(aminomethyl)cyclohexyl]carbonyl]amino)-N,N-dimethyl-1,3-benzothiazole-6-carboxamide
-
 Trypanosoma brucei
2.3.1.97 3-(methyl[6-methyl-2-[methyl(1-methylpiperidin-4-yl)amino]thieno[3,2-d]pyrimidin-4-yl]amino)propanenitrile
-
 Homo sapiens
2.3.1.97 3-(methyl[6-methyl-2-[methyl(1-methylpiperidin-4-yl)amino]thieno[3,2-d]pyrimidin-4-yl]amino)propanenitrile
-
 Leishmania donovani
2.3.1.97 3-(methyl[6-methyl-2-[methyl(1-methylpiperidin-4-yl)amino]thieno[3,2-d]pyrimidin-4-yl]amino)propanenitrile
-
 Plasmodium falciparum
2.3.1.97 3-(methyl[6-methyl-2-[methyl(1-methylpiperidin-4-yl)amino]thieno[3,2-d]pyrimidin-4-yl]amino)propanenitrile
-
 Trypanosoma brucei
2.3.1.97 5-chloro-2-[[4-(3,5-difluorophenyl)piperidin-1-yl]methyl]-1-methyl-1H-benzimidazole
-
 Homo sapiens
2.3.1.97 5-chloro-2-[[4-(3,5-difluorophenyl)piperidin-1-yl]methyl]-1-methyl-1H-benzimidazole
-
 Leishmania donovani
2.3.1.97 5-chloro-2-[[4-(3,5-difluorophenyl)piperidin-1-yl]methyl]-1-methyl-1H-benzimidazole
-
 Plasmodium falciparum
2.3.1.97 5-chloro-2-[[4-(3,5-difluorophenyl)piperidin-1-yl]methyl]-1-methyl-1H-benzimidazole
-
 Trypanosoma brucei
2.3.1.97 additional information development of specific anti-protozoan inhibitors against NMT, specificity over the human isozymes, component screening, structure-activity relationships, overview; development of specific anti-protozoan inhibitors against NMT, specificity over the human isozymes, component screening, structure-activity relationships, overview Homo sapiens
2.3.1.97 additional information development of specific anti-protozoan inhibitors against NMT, specificity over the human isozymes, component screening, structure-activity relationships, overview Leishmania donovani
2.3.1.97 additional information development of specific anti-protozoan inhibitors against NMT, specificity over the human isozymes, component screening, structure-activity relationships, overview Plasmodium falciparum
2.3.1.97 additional information development of specific anti-protozoan inhibitors against NMT, specificity over the human isozymes, component screening, structure-activity relationships, overview Trypanosoma brucei
2.3.1.97 N,N-dimethyl-1-[5-(2-methylphenyl)-1H-indazol-3-yl]methanamine
-
 Homo sapiens
2.3.1.97 N,N-dimethyl-1-[5-(2-methylphenyl)-1H-indazol-3-yl]methanamine
-
 Leishmania donovani
2.3.1.97 N,N-dimethyl-1-[5-(2-methylphenyl)-1H-indazol-3-yl]methanamine
-
 Plasmodium falciparum
2.3.1.97 N,N-dimethyl-1-[5-(2-methylphenyl)-1H-indazol-3-yl]methanamine
-
 Trypanosoma brucei
2.3.1.97 N-[(3R)-1-(N-methylglycyl)pyrrolidin-3-yl]-2-(trifluoromethyl)benzamide
-
 Homo sapiens
2.3.1.97 N-[(3R)-1-(N-methylglycyl)pyrrolidin-3-yl]-2-(trifluoromethyl)benzamide
-
 Leishmania donovani
2.3.1.97 N-[(3R)-1-(N-methylglycyl)pyrrolidin-3-yl]-2-(trifluoromethyl)benzamide
-
 Plasmodium falciparum
2.3.1.97 N-[(3R)-1-(N-methylglycyl)pyrrolidin-3-yl]-2-(trifluoromethyl)benzamide
-
 Trypanosoma brucei
2.3.1.97 N-[[3'-(6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-5(4H)-ylmethyl)biphenyl-3-yl]methyl]-2-(pyridin-3-yl)ethanamine
-
 Homo sapiens
2.3.1.97 N-[[3'-(6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-5(4H)-ylmethyl)biphenyl-3-yl]methyl]-2-(pyridin-3-yl)ethanamine
-
 Leishmania donovani
2.3.1.97 N-[[3'-(6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-5(4H)-ylmethyl)biphenyl-3-yl]methyl]-2-(pyridin-3-yl)ethanamine
-
 Plasmodium falciparum
2.3.1.97 N-[[3'-(6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-5(4H)-ylmethyl)biphenyl-3-yl]methyl]-2-(pyridin-3-yl)ethanamine
-
 Trypanosoma brucei
2.3.1.97 [4-[3-(benzylamino)propoxy]-3-methyl-1-benzofuran-2-yl](1-methyl-1H-imidazol-2-yl)methanone
-
 Leishmania donovani
2.3.1.97 [4-[3-(benzylamino)propoxy]-3-methyl-1-benzofuran-2-yl](1-methyl-1H-imidazol-2-yl)methanone
-
 Plasmodium falciparum
2.3.1.97 [4-[3-(benzylamino)propoxy]-3-methyl-1-benzofuran-2-yl](1-methyl-1H-imidazol-2-yl)methanone
-
 Trypanosoma brucei

Organism

EC Number Organism UniProt Comment Textmining
2.3.1.97 Homo sapiens O60551 NMT isoform HsNMT2; NMT isoform HsNMT2
-
2.3.1.97 Homo sapiens P30419 NMT isoform HsNMT1; NMT isoform HsNMT1
-
2.3.1.97 Leishmania donovani D0AB09
-
-
2.3.1.97 Plasmodium falciparum Q8ILW6
-
-
2.3.1.97 Trypanosoma brucei D0A003
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.3.1.97 additional information N-myristoylation of the synthetic peptide CAP5.5, derived from the N-terminus of the Trypanosoma brucei CAP5.5 protein, with myristoyl-CoA Homo sapiens ?
-
 ?
2.3.1.97 additional information N-myristoylation of the synthetic peptide CAP5.5, derived from the N-terminus of the Trypanosoma brucei CAP5.5 protein, with myristoyl-CoA Leishmania donovani ?
-
 ?
2.3.1.97 additional information N-myristoylation of the synthetic peptide CAP5.5, derived from the N-terminus of the Trypanosoma brucei CAP5.5 protein, with myristoyl-CoA Trypanosoma brucei ?
-
 ?
2.3.1.97 myristoyl-CoA + peptide CAP5.5 N-myristoylation of the synthetic peptide CAP5.5, derived from the N-terminus of the Trypanosoma brucei CAP5.5 protein Plasmodium falciparum CoA + N-myristoyl-peptide CAP5.5
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.3.1.97 HsNMT1
-
 Homo sapiens
2.3.1.97 HsNMT2
-
 Homo sapiens
2.3.1.97 N-myristoyltransferase
-
 Homo sapiens
2.3.1.97 N-myristoyltransferase
-
 Leishmania donovani
2.3.1.97 N-myristoyltransferase
-
 Plasmodium falciparum
2.3.1.97 N-myristoyltransferase
-
 Trypanosoma brucei
2.3.1.97 NMT
-
 Homo sapiens
2.3.1.97 NMT
-
 Leishmania donovani
2.3.1.97 NMT
-
 Plasmodium falciparum
2.3.1.97 NMT
-
 Trypanosoma brucei

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.3.1.97 7.4
-
 assay at Homo sapiens
2.3.1.97 7.4
-
 assay at Leishmania donovani
2.3.1.97 7.4
-
 assay at Plasmodium falciparum
2.3.1.97 7.4
-
 assay at Trypanosoma brucei

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.3.1.97 additional information
-
 IC50 values of different inhibitors, overview Homo sapiens additional information
2.3.1.97 additional information
-
 IC50 values of different inhibitors, overview Leishmania donovani additional information
2.3.1.97 additional information
-
 IC50 values of different inhibitors, overview Plasmodium falciparum additional information
2.3.1.97 additional information
-
 IC50 values of different inhibitors, overview Trypanosoma brucei additional information