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  • Diketoacid Inhibitors of HIV-1 Integrase: From L-708,906 to Raltegravir and Beyond

    Author(s)
    Beare, KD
    Coster, MJ
    Rutledge, PJ
    Griffith University Author(s)
    Coster, Mark J.
    Year published
    2012
    Metadata
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    Abstract
    HIV-1 integrase is one of the three viral enzymes essential to HIV replication. Consequently the development of therapeutics targeting this enzyme has been a major focus of antiretroviral research over the past two decades. Several classes of integrase inhibitors have been identified; of these the diketoacids (DKAs) show greatest promise: raltegravir (Merck & Co) has been approved by the US Food and Drug Administration (FDA) for HIV-1 therapy, while elvitegravir (Gilead Sciences/ Japan Tobacco) has reached phase III clinical trials. This review considers the development of DKA-based inhibitors from early screening studies ...
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    HIV-1 integrase is one of the three viral enzymes essential to HIV replication. Consequently the development of therapeutics targeting this enzyme has been a major focus of antiretroviral research over the past two decades. Several classes of integrase inhibitors have been identified; of these the diketoacids (DKAs) show greatest promise: raltegravir (Merck & Co) has been approved by the US Food and Drug Administration (FDA) for HIV-1 therapy, while elvitegravir (Gilead Sciences/ Japan Tobacco) has reached phase III clinical trials. This review considers the development of DKA-based inhibitors from early screening studies through to the release of raltegravir. SAR data collated from numerous studies are compared and analysed, shedding light on the geometric and electronic requirements for effective binding to HIV-1 integrase. This information will in turn aid the rational design of future generations of integrase inhibitors.
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    Journal Title
    Current Medicinal Chemistry
    Volume
    19
    Issue
    8
    DOI
    https://doi.org/10.2174/092986712799320565
    Subject
    Medicinal and biomolecular chemistry
    Biologically active molecules
    Biochemistry and cell biology
    Pharmacology and pharmaceutical sciences
    Publication URI
    http://hdl.handle.net/10072/48221
    Collection
    • Journal articles

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