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

Skinner-Adams, Tina S., Peatey, Christopher L., Anderson, Karen, Trenholme, Katharine R., Krige, David, Brown, Christopher L., Stack, Colin, Nsangou, Desire M. M., Mathews, Rency T., Thivierge, Karine, Dalton, John P. and Gardinerd, Donald L. (2012) The aminopeptidase inhibitor CHR-2863 is an orally bioavailable inhibitor of murine malaria. Antimicrobial Agents and Chemotherapy, 56 6: 3244-3249.


Author Skinner-Adams, Tina S.
Peatey, Christopher L.
Anderson, Karen
Trenholme, Katharine R.
Krige, David
Brown, Christopher L.
Stack, Colin
Nsangou, Desire M. M.
Mathews, Rency T.
Thivierge, Karine
Dalton, John P.
Gardinerd, Donald L.
Title The aminopeptidase inhibitor CHR-2863 is an orally bioavailable inhibitor of murine malaria
Journal name Antimicrobial Agents and Chemotherapy  (ERA 2012 Listed)    (ERA 2010 Rank A*)   Check publisher's open access policy
Publication date 2012-06
Sub-type Article
DOI 10.1128/AAC.06245-11
Volume number 56
Issue number 6
ISSN 0066-4804; 1098-6596
Start page 3244
End page 3249
Total pages 6
Place of publication Washington, United States
Publisher American Society for Microbiology
Collection year 2013
Language eng
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.
Keyword Antimalarial-drug development
Blood-stage malaria
Plasmodium-falciparum
Sulfadoxine-pyrimethamine
Leucine aminopeptidase
Leucyl aminopeptidase
Accurate docking
Plasmepsin-II
Bestatin
Q-Index Code C1
Q-Index Status Confirmed Code
Institutional Status UQ
Additional Notes Published ahead of print: 26 March 2012.

Document type: Journal Article
Sub-type: Article
Collections: Official 2013 Collection
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