Cloned (Comment) | Organism |
---|---|
expression of MetAP2 using the baculovirus transfection system | Encephalitozoon cuniculi |
Crystallization (Comment) | Organism |
---|---|
purified recombinant MetAP2 with and without the bound inhibitors fumagillin and TNP-470, sitting drop vapor diffusion at 20°C, mixing of 2 mg/ml protein, in 10 mM HEPES, 150 mM NaCl, 10% glycerol, 5 mM DTT, pH 7.5, with 30% w/v PEG 4000, 0.2 M ammonium sulfate, for inhibitor bound enzyme crystals co-cyrstallization with 0.5 mM inhibitor in 27% PEG 4000, 0.2 M ammonium sulfate, ten days, X-ray diffraction structure determination and analysis at 2.18-2.89 A resolution, molecular replacement | Encephalitozoon cuniculi |
Protein Variants | Comment | Organism |
---|---|---|
H382Y | the single site mutation in the S1 subsite of human MetAP2b results in inhibitor resistance | Homo sapiens |
Y444C | the single site mutation in the S1 subsite of human MetAP2b results in inhibitor resistance | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
fumagillin | binding structure, overview | Encephalitozoon cuniculi | |
fumagillin | binding structure, overview. Fumagillin and its analogues show inhibitory activity in vitro and in animal models of microsporidiosis and human infections due to Enterocytozoon bieneusi | Enterocytozoon bieneusi | |
fumagillin | binding structure, specificity determinants lie in the S1 hydrophobic methionine binding subsite, overview | Homo sapiens | |
TNP-470 | binding structure, overview | Encephalitozoon cuniculi | |
TNP-470 | binding structure, overview | Enterocytozoon bieneusi | |
TNP-470 | binding structure, specificity determinants lie in the S1 hydrophobic methionine binding subsite, overview | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
1.95 | - |
Met-Ala-Ser | pH 8.5, 37°C, recombinant MetAP2 | Encephalitozoon cuniculi | |
2.08 | - |
Met-Ala-Ser | pH 8.5, 37°C | Homo sapiens |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Co2+ | activates | Homo sapiens | |
Co2+ | activates | Encephalitozoon cuniculi | |
Fe2+ | activates slightly | Encephalitozoon cuniculi | |
Mn2+ | activates | Encephalitozoon cuniculi |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Encephalitozoon cuniculi | - |
- |
- |
Enterocytozoon bieneusi | B7XJ30 | - |
- |
Enterocytozoon bieneusi H348 | B7XJ30 | - |
- |
Homo sapiens | - |
- |
- |
Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
---|---|---|---|
2.9 | - |
in presence of Fe2+, purified recombinant MetAP2 | Encephalitozoon cuniculi |
7.9 | - |
in presence of Mn2+, purified recombinant MetAP2 | Encephalitozoon cuniculi |
8.3 | - |
- |
Homo sapiens |
11.7 | - |
in presence of Co2+, purified recombinant MetAP2 | Encephalitozoon cuniculi |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
Met-Ala-Ser + H2O | - |
Homo sapiens | Met + Ala-Ser | - |
? | |
Met-Ala-Ser + H2O | - |
Encephalitozoon cuniculi | Met + Ala-Ser | - |
? | |
additional information | active site structure and substrate binding, overview | Encephalitozoon cuniculi | ? | - |
? | |
additional information | active site structure and substrate binding, overview | Enterocytozoon bieneusi | ? | - |
? | |
additional information | active site strutcure and substrate binding, overview | Homo sapiens | ? | - |
? | |
additional information | active site structure and substrate binding, overview | Enterocytozoon bieneusi H348 | ? | - |
? |
Subunits | Comment | Organism |
---|---|---|
More | EbMetAP2 structure analysis by homology modelling using the structure of EcMetAP2 from Enterocytozoon cuniculi | Enterocytozoon bieneusi |
More | sequence comparisons, e.g. with the human enzyme structure, PDB ID 1YW9, overview | Encephalitozoon cuniculi |
More | sequence comparisons, overview | Homo sapiens |
Synonyms | Comment | Organism |
---|---|---|
MetAP2 | - |
Homo sapiens |
MetAP2 | - |
Encephalitozoon cuniculi |
MetAP2 | - |
Enterocytozoon bieneusi |
methionine aminopeptidase type 2 | - |
Homo sapiens |
methionine aminopeptidase type 2 | - |
Encephalitozoon cuniculi |
methionine aminopeptidase type 2 | - |
Enterocytozoon bieneusi |
More | EcMetAP2 as a member of the MetAP2c family | Encephalitozoon cuniculi |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Homo sapiens |
37 | - |
assay at | Encephalitozoon cuniculi |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.5 | - |
- |
Homo sapiens |
8.5 | - |
- |
Encephalitozoon cuniculi |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
10.6 | - |
pH 8.5, 37°C, recombinant MetAP2 | Encephalitozoon cuniculi | TNP-470 | |
11.1 | - |
pH 8.5, 37°C, recombinant MetAP2 | Encephalitozoon cuniculi | fumagillin |