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Literature summary for 2.3.1.97 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
Search for more literature for 2.3.1.97

Cloned(Commentary)

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

Inhibitors

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

Organism

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

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
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 ?
-
 ?
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 ?
-
 ?
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 ?
-
 ?
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

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

pH Optimum

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

IC50 Value

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