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Literature summary for 3.4.11.18 extracted from

  • Oefner, C.; Douangamath, A.; D'Arcy, A.; Hafeli, S.; Mareque, D.; MacSweeney, A.; Padilla, J.; Pierau, S.; Schulz, H.; Thormann, M.; Wadman, S.; Dale, G.E.
    The 1.15.ANG. crystal structure of the Staphylococcus aureus methionyl-aminopeptidase and complexes with triazole based inhibitors (2003), J. Mol. Biol., 332, 13-21.
    View publication on PubMed
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Crystallization (Commentary)

Crystallization (Comment) Organism
crystal structure of MetAP-1 as an apoenzyme and its complexes with various 1,2,4-triazole-based derivatives at high-resolution. Form 1 crystals are grown in the presence of 0.1 mM NiCl2 with 25% PEG 3350, 100 mM bis-Tris, pH 6.5, 200 mM LiSO4. Form 2 crystals are grown in the absence of metal ions using 25% PEG, 100 mM bis-Tris, pH 5.5, 200 mM ammonium acetate as precipitating agent Staphylococcus aureus

Inhibitors

Inhibitors Comment Organism Structure
MCB2379 IC50: 599 nM in presence of Co2+, 1455 nM in presence of Zn2+ Staphylococcus aureus
MCB2813 IC50: 43.7 nM in presence of Co2+, 300 nM in presence of Zn2+ Staphylococcus aureus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.75
-
 Met-Pro-4-nitroanilide pH 7.5, in presence of Mn2+ Staphylococcus aureus
1.41
-
 Met-Pro-4-nitroanilide pH 7.5, in presence of Co2+ Staphylococcus aureus
3.26
-
 Met-Pro-4-nitroanilide pH 7.5, in presence of Zn2+ Staphylococcus aureus

Metals/Ions

Metals/Ions Comment Organism Structure
Co2+ optimal concentration is 0.008 mM Staphylococcus aureus
Fe2+ optimal concentration is 0.008 mM Staphylococcus aureus
Ni2+ enzyme is active at concentrations below 0.002 mM, inhibition at higher concentrations Staphylococcus aureus
Zn2+ optimal concentration Staphylococcus aureus

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
27000
-
 gel filtration Staphylococcus aureus

Organism

Organism UniProt Comment Textmining
Staphylococcus aureus
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Met-Pro-4-nitroanilide + H2O
-
 Staphylococcus aureus Met + Pro-4-nitroanilide
-
 ?

Synonyms

Synonyms Comment Organism
More eukaryotes contain both the type I and the type II MetAPs, whereas prokaryotes possess only the type I enzyme Staphylococcus aureus

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
1.75
-
 Met-Pro-4-nitroanilide pH 7.5, in presence of Mn2+ Staphylococcus aureus
2.67
-
 Met-Pro-4-nitroanilide pH 7.5, in presence of Zn2+ Staphylococcus aureus
11.9
-
 Met-Pro-4-nitroanilide pH 7.5, in presence of Co2+ Staphylococcus aureus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000437 0.0003 IC50: 43.7 nM in presence of Co2+, 300 nM in presence of Zn2+ Staphylococcus aureus MCB2813
0.000599 0.001455 IC50: 599 nM in presence of Co2+, 1455 nM in presence of Zn2+ Staphylococcus aureus MCB2379