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Literature summary for 3.4.11.18 extracted from

  • Mitra, S.; Sheppard, G.; Wang, J.; Bennett, B.; Holz, R.C.
    Analyzing the binding of Co(II)-specific inhibitors to the methionyl aminopeptidases from Escherichia coli and Pyrococcus furiosus (2009), J. Biol. Inorg. Chem., 14, 573-585.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.11.18

Cloned(Commentary)

Cloned (Comment) Organism
-
 Escherichia coli
-
 Pyrococcus furiosus

Inhibitors

Inhibitors Comment Organism Structure
((2RS,3R)-3-amino-2-hydroxy-5-ethylthio)pentanoyl-((S)-(-)-(1-naphthyl)ethyl)amide A-311263, the inhibitor has little or no preference for the type of divalent metal ion that occupies the active site of MetAP Escherichia coli
((2RS,3R)-3-amino-2-hydroxy-5-ethylthio)pentanoyl-((S)-(-)-(1-naphthyl)ethyl)amide A-311263, the inhibitor has little or no preference for the type of divalent metal ion that occupies the active site of MetAP Pyrococcus furiosus
3-((2-naphthylmethyl)sulfanyl)-4H-1,2,4-triazole A-310840, the inhibitor binds to the Co2+-loaded enzyme well but is approximately 23fold less potent for Mn2+-loaded MetAP Escherichia coli
3-((2-naphthylmethyl)sulfanyl)-4H-1,2,4-triazole A-310840 Pyrococcus furiosus

Metals/Ions

Metals/Ions Comment Organism Structure
Co2+ activity requires divalent cations like Co2+ Escherichia coli
Co2+ activity requires divalent cations like Co2+ Pyrococcus furiosus
Mn2+ activity requires divalent cations like Mn2+ Escherichia coli
Mn2+ activity requires divalent cations like Mn2+ Pyrococcus furiosus

Organism

Organism UniProt Comment Textmining
Escherichia coli
-
-
-
Pyrococcus furiosus
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Escherichia coli
-
 Pyrococcus furiosus

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
L-Met-Gly-L-Met-L-Met + H2O
-
 Escherichia coli L-Met + Gly-L-Met-L-Met
-
 ?
L-Met-Gly-L-Met-L-Met + H2O
-
 Pyrococcus furiosus L-Met + Gly-L-Met-L-Met
-
 ?

Synonyms

Synonyms Comment Organism
MetAP-I
-
 Escherichia coli
MetAP-II
-
 Pyrococcus furiosus
methionine aminopeptidase type I
-
 Escherichia coli
methionine aminopeptidase type II
-
 Pyrococcus furiosus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.002
-
 ((2RS,3R)-3-amino-2-hydroxy-5-ethylthio)pentanoyl-((S)-(-)-(1-naphthyl)ethyl)amide Co2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30°C Pyrococcus furiosus
0.003
-
 3-((2-naphthylmethyl)sulfanyl)-4H-1,2,4-triazole Co2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30°C Pyrococcus furiosus
0.003
-
 ((2RS,3R)-3-amino-2-hydroxy-5-ethylthio)pentanoyl-((S)-(-)-(1-naphthyl)ethyl)amide Co2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30°C Escherichia coli
0.008
-
 3-((2-naphthylmethyl)sulfanyl)-4H-1,2,4-triazole Co2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30°C Escherichia coli
0.02
-
 ((2RS,3R)-3-amino-2-hydroxy-5-ethylthio)pentanoyl-((S)-(-)-(1-naphthyl)ethyl)amide Mn2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30°C Escherichia coli
0.02
-
 ((2RS,3R)-3-amino-2-hydroxy-5-ethylthio)pentanoyl-((S)-(-)-(1-naphthyl)ethyl)amide Mn2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30°C Pyrococcus furiosus
0.44
-
 3-((2-naphthylmethyl)sulfanyl)-4H-1,2,4-triazole Mn2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30°C Pyrococcus furiosus
0.75
-
 3-((2-naphthylmethyl)sulfanyl)-4H-1,2,4-triazole Mn2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30°C Escherichia coli

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.015
-
 Co2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30°C Pyrococcus furiosus 3-((2-naphthylmethyl)sulfanyl)-4H-1,2,4-triazole
0.02
-
 Co2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30°C Pyrococcus furiosus ((2RS,3R)-3-amino-2-hydroxy-5-ethylthio)pentanoyl-((S)-(-)-(1-naphthyl)ethyl)amide
0.027
-
 Mn2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30°C Pyrococcus furiosus ((2RS,3R)-3-amino-2-hydroxy-5-ethylthio)pentanoyl-((S)-(-)-(1-naphthyl)ethyl)amide
0.032
-
 Co2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30°C Escherichia coli ((2RS,3R)-3-amino-2-hydroxy-5-ethylthio)pentanoyl-((S)-(-)-(1-naphthyl)ethyl)amide
0.034
-
 Mn2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30°C Escherichia coli ((2RS,3R)-3-amino-2-hydroxy-5-ethylthio)pentanoyl-((S)-(-)-(1-naphthyl)ethyl)amide
0.044
-
 Co2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30°C Escherichia coli 3-((2-naphthylmethyl)sulfanyl)-4H-1,2,4-triazole
1
-
 Mn2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30°C Escherichia coli 3-((2-naphthylmethyl)sulfanyl)-4H-1,2,4-triazole
1
-
 Mn2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30°C Pyrococcus furiosus 3-((2-naphthylmethyl)sulfanyl)-4H-1,2,4-triazole