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Small-molecule inactivation of HIV-1 NCp7 by repetitive intracellular acyl transfer

  1. Author:
    Jenkins, L. M. M.
    Ott, D. E.
    Hayashi, R.
    Coren, L. V.
    Wang, D. Y.
    Xu, Q.
    Schito, M. L.
    Inman, J. K.
    Appella, D. H.
    Appella, E.

  2. Author Address

    [Jenkins, Lisa M. Miller; Hayashi, Ryo; Schito, Marco L.; Appella, Ettore] NCI, Cell Biol Lab, NIH, Bethesda, MD 20892 USA. [Ott, David E.; Coren, Lori V.] NCI, AIDS & Canc Virus Program, SAIC Frederick Inc, Frederick, MD 21701 USA. [Wang, Deyun; Xu, Qun; Appella, Daniel H.] NIDDKD, Bioorgan Chem Lab, Bethesda, MD 20892 USA. [Inman, John K.] NIAID, Bethesda, MD 20892 USA.;Jenkins, LMM, NCI, Cell Biol Lab, NIH, Bldg 37, Bethesda, MD 20892 USA.;appellae@mail.nih.gov
    1. Year: 2010
    2. Date: Dec
  2. Journal: Nature Chemical Biology
    1. 6
    2. 12
    3. Pages: 887-889
  4. Type of Article: Article
  5. ISSN: 1552-4450
  1. Abstract:

    The zinc fingers of the HIV-1 nucleocapsid protein, NCp7, are prime targets for antiretroviral therapeutics. Here we show that S-acyl-2-mercaptobenzamide thioester (SAMT) chemotypes inhibit HIV by modifying the NCp7 region of Gag in infected cells, thereby blocking Gag processing and reducing infectivity. The thiol produced by SAMT reaction with NCp7 is acetylated by cellular enzymes to regenerate active SAMTs via a recycling mechanism unique among small-molecule inhibitors of HIV.

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External Sources

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  2. DOI: 10.1038/nchembio.456
  3. View record in Web of Science®
  4. WOS: 000284214700017

Library Notes

  1. Fiscal Year: FY2010-2011
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