The Aminopeptidase Inhibitor CHR-2863 Is an Orally Bioavailable Inhibitor of Murine Malaria
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Peatey, Christopher L
Anderson, Karen
Trenholme, Katharine R
Krige, David
Brown, Christopher L
Stack, Colin
Nsangou, Desire MM
Mathews, Rency T
Thivierge, Karine
Dalton, John P
Gardinerd, Donald L
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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.
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Antimicrobial Agents and Chemotherapy
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56
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6
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Microbiology
Medical microbiology
Medical parasitology
Pharmacology and pharmaceutical sciences