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Literature summary 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

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
3.4.11.18 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

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

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.4.11.18 0.75
-
Met-Pro-4-nitroanilide pH 7.5, in presence of Mn2+ Staphylococcus aureus
3.4.11.18 1.41
-
Met-Pro-4-nitroanilide pH 7.5, in presence of Co2+ Staphylococcus aureus
3.4.11.18 3.26
-
Met-Pro-4-nitroanilide pH 7.5, in presence of Zn2+ Staphylococcus aureus

Metals/Ions

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

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
3.4.11.18 27000
-
gel filtration Staphylococcus aureus

Organism

EC Number Organism UniProt Comment Textmining
3.4.11.18 Staphylococcus aureus
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.11.18 Met-Pro-4-nitroanilide + H2O
-
Staphylococcus aureus Met + Pro-4-nitroanilide
-
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Synonyms

EC Number Synonyms Comment Organism
3.4.11.18 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]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
3.4.11.18 1.75
-
Met-Pro-4-nitroanilide pH 7.5, in presence of Mn2+ Staphylococcus aureus
3.4.11.18 2.67
-
Met-Pro-4-nitroanilide pH 7.5, in presence of Zn2+ Staphylococcus aureus
3.4.11.18 11.9
-
Met-Pro-4-nitroanilide pH 7.5, in presence of Co2+ Staphylococcus aureus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.11.18 0.0000437 0.0003 IC50: 43.7 nM in presence of Co2+, 300 nM in presence of Zn2+ Staphylococcus aureus MCB2813
3.4.11.18 0.000599 0.001455 IC50: 599 nM in presence of Co2+, 1455 nM in presence of Zn2+ Staphylococcus aureus MCB2379