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Literature summary for 3.4.11.18 extracted from

  • Wang, J.; Sheppard, G.S.; Lou, P.; Kawai, M.; Park, C.; Egan, D.A.; Schneider, A.; Bouska, J.; Lesniewski, R.; Henkin, J.
    Physiologically relevant metal cofactor for methionine aminopeptidase-2 is manganese (2003), Biochemistry, 42, 5035-5042.
    View publication on PubMed
Search for more literature for 3.4.11.18

Application

Application Comment Organism
medicine MetAP2 is a molecular target for antiangiogenesis and anticancer therapy Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
A-310840 IC50: 0.000031 mM for enzyme with Zn2+, 0.000043 mM for enzyme with Ni2+, 0.000069 mM for enzyme with Co2+, 0.000026 for enzyme with Fe2+, 0.0578 mM for enzyme with Mn2+ Homo sapiens
A-311263 IC50: 0.000121 mM for enzyme with Zn2+, 0.000107 mM for enzyme with Ni2+, 0.000149 mM for enzyme with Co2+, 0.00011 mM for enzyme with Fe2+, 0.000055 mM for enzyme with Mn2+ Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Ca2+ 0.0001-0.001 mM, activity is enhanced 5-10fold Homo sapiens
Co2+ stimulates activity of MetAP2 with Met-Ala-Ser or Met-Gly-Ala-Gln-Phe-Ser-Lys-Thr 10-20fold, maximal stimulation at 0.01 mM. In presence of 5 mM glutathione 30-40fold stimulation Homo sapiens
Mn2+ stimulates activity of MetAP2 with Met-Ala-Ser or Met-Gly-Ala-Gln-Phe-Ser-Lys-Thr 10-20fold, maximal stimulation at 0.001 mM. In presence of 5 mM glutathione 30-40fold stimulation Homo sapiens
Zn2+ 0.0001-0.001 mM, activity of MetAP2 is enhanced 5-10fold Homo sapiens
Zn2+ Zn2+ is the best metal cofactor for MetAP1 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
 methionine aminopeptidase type 2
-

Source Tissue

Source Tissue Comment Organism Textmining
endothelial cell neonatal dermal microvascular Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Met-Ala-Ser + H2O
-
 Homo sapiens Met + Ala-Ser
-
 ?
Met-Ala-Ser-Lys-(biotin)-Gly + H2O
-
 Homo sapiens Met + Ala-Ser-Lys-(biotin)-Gly
-
 ?
Met-Gly-Ala-Gln-Phe-Ser-Lys-Thr + H2O
-
 Homo sapiens Met + Gly-Ala-Gln-Phe-Ser-Lys-Thr
-
 ?

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.0517
-
 Met-Ala-Ser pH 7.4, MetAP2 Homo sapiens
0.0683
-
 Met-Gly-Ala-Gln-Phe-Ser-Lys-Thr pH 7.4, MetAP2 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000031
-
 IC50: 0.000031 mM for enzyme with Zn2+, 0.000043 mM for enzyme with Ni2+, 0.000069 mM for enzyme with Co2+, 0.000026 for enzyme with Fe2+, 0.0578 mM for enzyme with Mn2+ Homo sapiens A-310840
0.000121
-
 IC50: 0.000121 mM for enzyme with Zn2+, 0.000107 mM for enzyme with Ni2+, 0.000149 mM for enzyme with Co2+, 0.00011 mM for enzyme with Fe2+, 0.000055 mM for enzyme with Mn2+ Homo sapiens A-311263