The Aminopeptidase Inhibitor CHR-2863 Is an Orally Bioavailable Inhibitor of Murine Malaria | Zendy

Tina S. SkinnerAdams | Zendy; Christopher L. Peatey | Zendy; Karen Anderson | Zendy; Katharine R. Trenholme | Zendy; David Krige | Zendy; Christopher L. Brown | Zendy; Colin M. Stack | Zendy; Desire M. M. Nsangou | Zendy; Rency T. Mathews | Zendy; Karine Thivierge | Zendy; John P. Dalton | Zendy; Donald L. Gardiner | Zendy

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The Aminopeptidase Inhibitor CHR-2863 Is an Orally Bioavailable Inhibitor of Murine Malaria

Author(s) -

Tina S. SkinnerAdams,

Christopher L. Peatey,

Karen Anderson,

Katharine R. Trenholme,

David Krige,

Christopher L. Brown,

Colin M. Stack,

Desire M. M. Nsangou,

Rency T. Mathews,

Karine Thivierge,

John P. Dalton,

Donald L. Gardiner

Publication year - 2012

Publication title -

antimicrobial agents and chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.07

H-Index - 259

eISSN - 1070-6283

pISSN - 0066-4804

DOI - 10.1128/aac.06245-11

Subject(s) - aminopeptidase , malaria , pharmacology , biology , bioavailability , chemistry , leucine , amino acid , biochemistry , microbiology and biotechnology , immunology

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.

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