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Literature summary for 3.4.11.18 extracted from

  • Trenholme, K.R.; Brown, C.L.; Skinner-Adams, T.S.; Stack, C.; Lowther, J.; To, J.; Robinson, M.W.; Donnelly, S.M.; Dalton, J.P.; Gardiner, D.L.
    Aminopeptidases of malaria parasites: new targets for chemotherapy (2010), Infect. Disord. Drug Targets, 10, 217-225.
    View publication on PubMed
Search for more literature for 3.4.11.18

Application

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(Commentary)

Cloned (Comment) Organism
isozymes MetAP1a, MetAP1b, MetAP1c, and MetAP2 are encoded on chromosomes 5, 10, 8, and 14 Plasmodium falciparum

Inhibitors

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

Localization Comment Organism GeneOntology No. Textmining
cytosol
-
 Plasmodium falciparum 5829
-

Metals/Ions

Metals/Ions Comment Organism Structure
additional information MetAPs are metalloproteases Plasmodium falciparum

Natural Substrates/ Products (Substrates)

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

Organism UniProt Comment Textmining
Plasmodium falciparum
-
 four isozymes MetAP1a, MetAP1b, MetAP1c, and MetAP2
-

Source Tissue

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 and Products (Substrate)

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

Subunits Comment Organism
More type 2 MetAPs contain a 60 amino acid insertion near the catalytic domain, while MetAP1s do not Plasmodium falciparum

Synonyms

Synonyms Comment Organism
MetAP1a
-
 Plasmodium falciparum
MetAP1b
-
 Plasmodium falciparum
MetAP1c
-
 Plasmodium falciparum
MetAP2
-
 Plasmodium falciparum
methionine aminopeptidase
-
 Plasmodium falciparum

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
-
 Plasmodium falciparum

pH Range

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 IC50 Value Maximum Comment Organism Inhibitor Structure
0.0007
-
 isozyme MetAP1b Plasmodium falciparum XC-11

General Information

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