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Literature summary for 3.4.11.18 extracted from

  • Li, J.Y.; Chen, L.L.; Cui, Y.M.; Luo, Q.L.; Li, J.; Nan, F.J.; Ye, Q.Z.
    Specificity for inhibitors of metal-substituted methionine aminopeptidase (2003), Biochem. Biophys. Res. Commun., 307, 172-179.
    View publication on PubMed
Search for more literature for 3.4.11.18

Inhibitors

Inhibitors Comment Organism Structure
(3R)-amino-(2S)-hydroxypentanoic acid IC50: 0.0123 mM for the Co2+-substituted enzyme, 0.0115 mM for the Mn2+-substituted enzyme, 0.0093 mM for the Zn2+-substituted enzyme, 0.0223 for the Ni2+-substituted enzyme Escherichia coli
(5,5-Dimethyl-4,5-dihydro-thiazol-2-yl)-(3-methyl-pyridin-2-yl)-amine IC50 for Co-EcMetAP1: 0.00021 mM Escherichia coli
2-[2-(2-amino-4-methylsulfanyl-butyrylsulfanyl)-3-phenyl-propionylamino]-3-hydroxy-propionic acid IC50 for Co-EcMetAP1: 0.0296 mM, IC50 for Mn-EcMetAPa: 0.0441 mM, IC50 for Zn-EcMetAP1: 0.0365 mM Escherichia coli
2-[2-(2-Amino-4-methylsulfanyl-butyrylsulfanyl)-5-methyl-hexanoylamino]-3-hydroxy-propionic acid IC50 for Co-EcMetAP1: 0.0286 mM, IC50 for Mn-EcMetAPa: 0.0443 mM, IC50 for Zn-EcMetAP1: 0.0498 mM, IC50 for Ni-EcMetAP1: 0.0357 mM Escherichia coli
2-[2-(3-Amino-2-hydroxy-heptanoylamino)-propionylamino]-4-methyl-pentanoic acid methyl ester IC50 for Co-EcMetAP1: 0.0229 mM, IC50 for Mn-EcMetAPa: 0.0252 mM, IC50 for Zn-EcMetAP1: 0.0167 mM, IC50 for Ni-EcMetAP1: 0.0125 mM Escherichia coli
2-[4-(2-Cyano-2-ethoxycarbonyl-1-methyl-vinyl)-phenyl]-1,3-dioxo-2,3-dihydro-1H-isoindole-5-carboxylic acid IC50 for Co-EcMetAP1: 0.037 mM Escherichia coli
3-But-3-enoylamino-pyridine-2-carboxylic acid thiazol-2-ylamide IC50 for Co-EcMetAP1: 0.0001 mM, IC50 for Mn-EcMetAPa: 0.0233 mM, IC50 for Zn-EcMetAP1: 0.0224 mM, IC50 for Ni-EcMetAP1: 0.00076 mM Escherichia coli
Pyridine-2-carboxylic acid thiazol-2-ylamide IC50 for Co-EcMetAP1: 0.0013 mM Escherichia coli

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.86
-
 Met-S-Gly-Phe pH 7.0, Co2+-substituted enzyme Escherichia coli
1.24
-
 Met-7-amido-4-methylcoumarin pH 7.0, Ni2+-substituted enzyme Escherichia coli
2.01
-
 Met-S-Gly-Phe pH 7.0, Zn2+-substituted enzyme Escherichia coli
3.89
-
 Met-S-Gly-Phe pH 7.0, Mn2+-substituted enzyme Escherichia coli
4.32
-
 Met-7-amido-4-methylcoumarin pH 7.0, Co2+-substituted enzyme Escherichia coli
6.27
-
 Met-7-amido-4-methylcoumarin pH 7.0, Mn2+-substituted enzyme Escherichia coli

Metals/Ions

Metals/Ions Comment Organism Structure
Mn2+ activates apoenzyme Escherichia coli
Ni2+ activates apoenzyme with Met-7-amido-4-methylcoumarin as substrate, very poor activity in presence of Met-S-Gly-Phe as substrate Escherichia coli
Zn2+ activates apoenzyme Escherichia coli

Organism

Organism UniProt Comment Textmining
Escherichia coli
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Met-7-amido-4-methylcoumarin + H2O
-
 Escherichia coli Met + 7-amino-4-methylcoumarin
-
 ?
Met-S-Gly-Phe + H2O
-
 Escherichia coli Met + Gly-Phe
-
 ?

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.00164
-
 Met-7-amido-4-methylcoumarin pH 7.0, Ni2+-substituted enzyme Escherichia coli
0.0059
-
 Met-7-amido-4-methylcoumarin pH 7.0, Mn2+-substituted enzyme Escherichia coli
0.0114
-
 Met-7-amido-4-methylcoumarin pH 7.0, Co2+-substituted enzyme Escherichia coli
11.1
-
 Met-S-Gly-Phe pH 7.0, Zn2+-substituted enzyme Escherichia coli
20.2
-
 Met-S-Gly-Phe pH 7.0, Co2+-substituted enzyme Escherichia coli
42.5
-
 Met-S-Gly-Phe pH 7.0, Mn2+-substituted enzyme Escherichia coli

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0001
-
 IC50 for Co-EcMetAP1: 0.0001 mM Escherichia coli 3-But-3-enoylamino-pyridine-2-carboxylic acid thiazol-2-ylamide
0.00021
-
 IC50 for Co-EcMetAP1: 0.00021 mM Escherichia coli (5,5-Dimethyl-4,5-dihydro-thiazol-2-yl)-(3-methyl-pyridin-2-yl)-amine
0.00076
-
 IC50 for Ni-EcMetAP1: 0.00076 mM Escherichia coli 3-But-3-enoylamino-pyridine-2-carboxylic acid thiazol-2-ylamide
0.0013
-
 IC50 for Co-EcMetAP1: 0.0013 mM Escherichia coli Pyridine-2-carboxylic acid thiazol-2-ylamide
0.0123
-
 IC50: 0.0123 mM for the Co2+-substituted enzyme, 0.0115 mM for the Mn2+-substituted enzyme, 0.0093 mM for the Zn2+-substituted enzyme, 0.0223 for the Ni2+-substituted enzyme Escherichia coli (3R)-amino-(2S)-hydroxypentanoic acid
0.0125
-
 IC50 for Ni-EcMetAP1: 0.0125 mM Escherichia coli 2-[2-(3-Amino-2-hydroxy-heptanoylamino)-propionylamino]-4-methyl-pentanoic acid methyl ester
0.0167
-
 IC50 for Zn-EcMetAP1: 0.0167 mM Escherichia coli 2-[2-(3-Amino-2-hydroxy-heptanoylamino)-propionylamino]-4-methyl-pentanoic acid methyl ester
0.0224
-
 IC50 for Zn-EcMetAP1: 0.0224 mM Escherichia coli 3-But-3-enoylamino-pyridine-2-carboxylic acid thiazol-2-ylamide
0.0229
-
 IC50 for Co-EcMetAP1: 0.0229 mM Escherichia coli 2-[2-(3-Amino-2-hydroxy-heptanoylamino)-propionylamino]-4-methyl-pentanoic acid methyl ester
0.0233
-
 IC50 for Mn-EcMetAPa: 0.0233 mM Escherichia coli 3-But-3-enoylamino-pyridine-2-carboxylic acid thiazol-2-ylamide
0.0252
-
 IC50 for Mn-EcMetAPa: 0.0252 mM Escherichia coli 2-[2-(3-Amino-2-hydroxy-heptanoylamino)-propionylamino]-4-methyl-pentanoic acid methyl ester
0.0286
-
 IC50 for Co-EcMetAP1: 0.0286 mM Escherichia coli 2-[2-(2-Amino-4-methylsulfanyl-butyrylsulfanyl)-5-methyl-hexanoylamino]-3-hydroxy-propionic acid
0.0296
-
 IC50 for Co-EcMetAP1: 0.0296 mM Escherichia coli 2-[2-(2-amino-4-methylsulfanyl-butyrylsulfanyl)-3-phenyl-propionylamino]-3-hydroxy-propionic acid
0.0357
-
 IC50 for Ni-EcMetAP1: 0.0357 mM Escherichia coli 2-[2-(2-Amino-4-methylsulfanyl-butyrylsulfanyl)-5-methyl-hexanoylamino]-3-hydroxy-propionic acid
0.0365
-
 IC50 for Zn-EcMetAP1: 0.0365 mM Escherichia coli 2-[2-(2-amino-4-methylsulfanyl-butyrylsulfanyl)-3-phenyl-propionylamino]-3-hydroxy-propionic acid
0.037
-
 IC50 for Co-EcMetAP1: 0.037 mM Escherichia coli 2-[4-(2-Cyano-2-ethoxycarbonyl-1-methyl-vinyl)-phenyl]-1,3-dioxo-2,3-dihydro-1H-isoindole-5-carboxylic acid
0.0441
-
 IC50 for Mn-EcMetAPa: 0.0441 mM Escherichia coli 2-[2-(2-amino-4-methylsulfanyl-butyrylsulfanyl)-3-phenyl-propionylamino]-3-hydroxy-propionic acid
0.0443
-
 IC50 for Mn-EcMetAPa: 0.0443 mM Escherichia coli 2-[2-(2-Amino-4-methylsulfanyl-butyrylsulfanyl)-5-methyl-hexanoylamino]-3-hydroxy-propionic acid
0.0498
-
 IC50 for Zn-EcMetAP1: 0.0498 mM Escherichia coli 2-[2-(2-Amino-4-methylsulfanyl-butyrylsulfanyl)-5-methyl-hexanoylamino]-3-hydroxy-propionic acid