Application | Comment | Organism |
---|---|---|
drug development | the isoyzmes are targets for the development of antimalarial drugs, and ienzyme inhibitors may be useful as anticancer compounds | Plasmodium falciparum |
Cloned (Comment) | Organism |
---|---|
isozymes MetAP1a, MetAP1b, MetAP1c, and MetAP2 are encoded on chromosomes 5, 10, 8, and 14 | Plasmodium falciparum |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
fumagillin | targets MetAP2, no binding to MetAP1 isozymes | Plasmodium falciparum | |
fumarranol | binds to MetAP2 noncovalently and reversibly | Plasmodium falciparum | |
additional information | identification of pyridinyl-pyrimidine inhibitors with selectivity to isozyme MetAP1b before MetAP1a and MetAP1c | Plasmodium falciparum | |
TNP-470 | a fumagillin derivative, targets MetAP2, no binding to MetAP1 isozymes | Plasmodium falciparum | |
XC-11 | a pyridinyl-pyrimidine inhibitor selective for MetAP1b | Plasmodium falciparum |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
cytosol | - |
Plasmodium falciparum | 5829 | - |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
additional information | MetAPs are metalloproteases | Plasmodium falciparum |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | Plasmodium falciparum | the isozymes act on peptides in the cytosol, that are N-terminal fragments from digestion of hemoglobin in the digestive vacuole. The hemoglobin-derived peptides show leucine and alanine as most abundant amino acids | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Plasmodium falciparum | - |
four isozymes MetAP1a, MetAP1b, MetAP1c, and MetAP2 | - |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
additional information | Plasmodium falciparum life cycle overview | Plasmodium falciparum | - |
trophozoite | expression of isozymes MetAP1a, MetAP1b, and MetAP2, and of isozyme MetAP1c in the late trophozoite | Plasmodium falciparum | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | the isozymes act on peptides in the cytosol, that are N-terminal fragments from digestion of hemoglobin in the digestive vacuole. The hemoglobin-derived peptides show leucine and alanine as most abundant amino acids | Plasmodium falciparum | ? | - |
? | |
additional information | the enzyme shows preference for synthetic peptides containing leucine and alanine | Plasmodium falciparum | ? | - |
? |
Subunits | Comment | Organism |
---|---|---|
More | type 2 MetAPs contain a 60 amino acid insertion near the catalytic domain, while MetAP1s do not | Plasmodium falciparum |
Synonyms | Comment | Organism |
---|---|---|
MetAP1a | - |
Plasmodium falciparum |
MetAP1b | - |
Plasmodium falciparum |
MetAP1c | - |
Plasmodium falciparum |
MetAP2 | - |
Plasmodium falciparum |
methionine aminopeptidase | - |
Plasmodium falciparum |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.4 | - |
- |
Plasmodium falciparum |
pH Minimum | pH Maximum | Comment | Organism |
---|---|---|---|
6 | 7.4 | inactive below pH 6.0, optimal activity at pH 7.4 | Plasmodium falciparum |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0007 | - |
isozyme MetAP1b | Plasmodium falciparum | XC-11 |
General Information | Comment | Organism |
---|---|---|
malfunction | blockade of the isozymes can is lethal to cell proliferation | Plasmodium falciparum |
physiological function | MetAP functions in the catalytic removal of N-terminal initiator methionine residues from proteins during sythesis, which is essential for the correct folding and trafficking of proteins | Plasmodium falciparum |