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

By Tina S. Skinner-Adams, Christopher L. Peatey, Karen Anderson, Katharine R. Trenholme, David Krige, Christopher L. Brown, Colin Stack, Desire M. M. Nsangou, Rency T. Mathews, Karine Thivierge, John P. Dalton and Donald L. Gardinerd

Abstract

Malaria remains a significant risk in many areas of the world, with resistance to the current antimalarial pharmacopeia an everincreasing 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

Topics: Antimalarial-drug development, Blood-stage malaria, Plasmodium-falciparum, Sulfadoxine-pyrimethamine, Leucine aminopeptidase, Leucyl aminopeptidase, Accurate docking, Plasmepsin-II, Bestatin, 2725 Infectious Diseases, 2736 Pharmacology (medical), 3004 Pharmacology
Publisher: American Society for Microbiology
Year: 2012
DOI identifier: 10.1128/AAC.06245-11
OAI identifier: oai:espace.library.uq.edu.au:UQ:276804

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