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Literature summary for 3.4.11.18 extracted from

  • Chai, S.C.; Ye, Q.Z.
    A cell-based assay that targets methionine aminopeptidase in a physiologically relevant environment (2010), Bioorg. Med. Chem. Lett., 20, 2129-2132.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
overexpression in Escherichia coli strain BL21(DE3) Escherichia coli

Inhibitors

Inhibitors Comment Organism Structure
2-hydroxy-4-(2-methyl-1,3-thiazol-4-yl)benzamide
-
Escherichia coli
3-(2-methyl-1,3-thiazol-4-yl)phenol
-
Escherichia coli
4-(1,3-thiazol-2-yl)benzene-1,2-diol
-
Escherichia coli
4-(2,5-dichlorothiophen-3-yl)benzene-1,2-diol
-
Escherichia coli
4-(2,5-dimethylthiophen-3-yl)benzene-1,2-diol
-
Escherichia coli
4-(2-amino-1,3-thiazol-4-yl)benzene-1,2-diol
-
Escherichia coli
4-(2-methyl-1,3-thiazol-4-yl)-2-nitroaniline
-
Escherichia coli
4-(2-methyl-1,3-thiazol-4-yl)benzene-1,2-diamine
-
Escherichia coli
4-(2-methyl-1,3-thiazol-4-yl)benzene-1,2-diol
-
Escherichia coli
4-(2-methyl-1,3-thiazol-4-yl)benzene-1,3-diol
-
Escherichia coli
4-(3,4-dimethoxyphenyl)-2-methyl-1,3-thiazole
-
Escherichia coli
4-(3-butylthiophen-2-yl)benzene-1,2-diol
-
Escherichia coli
4-(3-ethylthiophen-2-yl)benzene-1,2-diol
-
Escherichia coli
4-(3-methylthiophen-2-yl)benzene-1,2-diol
-
Escherichia coli
4-(3-propylthiophen-2-yl)benzene-1,2-diol
-
Escherichia coli
4-(4-bromo-2,5-dimethylthiophen-3-yl)benzene-1,2-diol
-
Escherichia coli
4-(5-chlorothiophen-2-yl)benzene-1,2-diol
-
Escherichia coli
4-(5-methylthiophen-2-yl)benzene-1,2-diol
-
Escherichia coli
4-(thiophen-2-yl)benzene-1,2-diol
-
Escherichia coli
4-(thiophen-3-yl)benzene-1,2-diol
-
Escherichia coli
4-[3-(2-bromoethyl)thiophen-2-yl]benzene-1,2-diol
-
Escherichia coli
5-(2,5-dichlorophenyl)furan-2-carboxylic acid
-
Escherichia coli
5-(2-chlorophenyl)furan-2-carboxylic acid
-
Escherichia coli
5-(3,4-dihydroxyphenyl)-2-methyl-N-(propan-2-yl)-1,3-thiazole-4-carboxamide
-
Escherichia coli
5-(3,4-dihydroxyphenyl)thiophene-2-carbonitrile
-
Escherichia coli
N-(pyridin-2-ylmethyl)-N'-(1,3-thiazol-2-yl)ethanediamide
-
Escherichia coli
N-cyclopentyl-N'-(1,3-thiazol-2-yl)ethanediamide
-
Escherichia coli
N-cyclopropyl-2-(3,4-dihydroxyphenyl)thiophene-3-carboxamide
-
Escherichia coli
N-cyclopropyl-5-(3,4-dihydroxyphenyl)-2-methyl-1,3-thiazole-4-carboxamide
-
Escherichia coli
N-cyclopropyl-5-(3,4-dihydroxyphenyl)thiophene-2-carboxamide
-
Escherichia coli
N-[4-(2-methyl-1,3-thiazol-4-yl)-2-nitrophenyl]acetamide
-
Escherichia coli

Metals/Ions

Metals/Ions Comment Organism Structure
Co2+ activates Escherichia coli
Fe2+ activates Escherichia coli
Mn2+ activates Escherichia coli
additional information MetAp requires divalent metal ions for catalytic activity Escherichia coli
Ni2+ activates Escherichia coli

Organism

Organism UniProt Comment Textmining
Escherichia coli
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
L-methionyl 4-methylcoumarin-7-amide + H2O fluorogenic substrate Escherichia coli L-methionine + 7-amino-4-methylcoumarin
-
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Synonyms

Synonyms Comment Organism
MetAP
-
Escherichia coli
methionine aminopeptidase
-
Escherichia coli

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
additional information
-
inhibitor screening, assay method development, and assay validation, overview Escherichia coli additional information

General Information

General Information Comment Organism
physiological function MetAP plays a critical role in protein maturation by catalyzing the removal of the N-terminal initiator methionine from nascent proteins Escherichia coli