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The aminopeptidase inhibitor CHR-2863 is an orally bioavailable inhibitor of murine malaria.

ABSTRACT: Malaria remains a significant risk in many areas of the world, with resistance to the current antimalarial pharmacopeia an ever-increasing problem. The M1 alanine aminopeptidase (PfM1AAP) and M17 leucine aminopeptidase (PfM17LAP) are believed to play a role in the terminal stages of digestion of host hemoglobin and thereby generate a pool of free amino acids that are essential for parasite growth and development. Here, we show that an orally bioavailable aminopeptidase inhibitor, CHR-2863, is efficacious against murine malaria.

SUBMITTER: Skinner-Adams TS

PROVIDER: S-EPMC3370795 | biostudies-literature | 2012 Jun

REPOSITORIES: biostudies-literature

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The aminopeptidase inhibitor CHR-2863 is an orally bioavailable inhibitor of murine malaria.

Skinner-Adams Tina S TS Peatey Christopher L CL Anderson Karen K Trenholme Katharine R KR Krige David D Brown Christopher L CL Stack Colin C Nsangou Desire M M DM Mathews Rency T RT Thivierge Karine K Dalton John P JP Gardiner Donald L DL

Antimicrobial agents and chemotherapy 20120326 6

Malaria remains a significant risk in many areas of the world, with resistance to the current antimalarial pharmacopeia an ever-increasing problem. The M1 alanine aminopeptidase (PfM1AAP) and M17 leucine aminopeptidase (PfM17LAP) are believed to play a role in the terminal stages of digestion of host hemoglobin and thereby generate a pool of free amino acids that are essential for parasite growth and development. Here, we show that an orally bioavailable aminopeptidase inhibitor, CHR-2863, is ef ...[more]

PMID: 22450967

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