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

    Author(s)
    Skinner-Adams, Tina S
    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
    Griffith University Author(s)
    Brown, Chris L.
    Gardiner, Donald
    Skinner-Adams, Tina
    Trenholme, Katharine
    Year published
    2012
    Metadata
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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.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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    Journal Title
    Antimicrobial Agents and Chemotherapy
    Volume
    56
    Issue
    6
    DOI
    https://doi.org/10.1128/AAC.06245-11
    Subject
    Medical Parasitology
    Microbiology
    Medical Microbiology
    Pharmacology and Pharmaceutical Sciences
    Publication URI
    http://hdl.handle.net/10072/51686
    Collection
    • Journal articles

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