Literature summary for 3.4.11.20 extracted from

Drinkwater, N.; Bamert, R.S.; Kannan Sivaraman, K.; Paiardini, A.; McGowan, S.
X-ray crystal structures of an orally available aminopeptidase inhibitor, tosedostat, bound to anti-malarial drug targets PfA-M1 and PfA-M17 (2015), Proteins, 83, 789-795.

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Cloned(Commentary)

Cloned (Comment)	Organism
expression in Escherichia coli	Plasmodium falciparum

Crystallization (Commentary)

Crystallization (Comment)	Organism
in complex with inhibitor tosedostat. The inhibitor occupies the enzymes' putative product egress channels in addition to the substrate binding pockets. Inhibitor adopts different binding poses when bound to isoforms M1, and M17	Plasmodium falciparum

Inhibitors

Inhibitors	Comment	Organism	Structure
tosedostat	i.e. (2S)-([(2R)-2-[(1S)-1-hydroxy-2-(hydroxyamino)-2-oxoethyl]-4-methylpentanoyl]amino)(phenyl)ethanoic acid, crystal structure; i.e. (2S)-({(2R)-2-[(1S)-1-hydroxy-2-(hydroxyamino)-2-oxoethyl]-4-methylpentanoyl}amino)(phenyl)ethanoic acid, crystal structure	Plasmodium falciparum

Organism

Organism	UniProt	Comment	Textmining
Plasmodium falciparum	O96935	-	-
Plasmodium falciparum	Q8IL11	-	-
Plasmodium falciparum isolate FcB1/Columbia	O96935	-	-

Synonyms

Synonyms	Comment	Organism
aminopeptidase M17	-	Plasmodium falciparum
M1 aminopeptidase	-	Plasmodium falciparum

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Release 2023.1 (January 2023)