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Inhibition of HIV Maturation via Selective Unfolding and Cross-Linking of Gag Polyprotein by a Mercaptobenzamide Acetylator

  1. Author:
    Jenkins, Lisa M. Miller
    Paine, Elliott L.
    Deshmukh, Lalit
    Nikolayevskiy, Herman
    Lyons, Gaelyn C.
    Scerba, Michael T.
    Rosenker, Kara George
    Luecke, Hans F.
    Louis, John M.
    Chertova,Elena
    Gorelick,Robert
    Ott,David
    Clore, G. Marius
    Appella, Daniel H.

  2. Author Address

    NCI, Lab Cell Biol, NIH, Bethesda, MD 20892 USA.NIDDK, Lab Chem Phys, Bethesda, MD 20892 USA.NIDDK, Lab Bioorgan Chem, Bethesda, MD 20892 USA.NIDDK, Adv Mass Spectrometry Core, Bethesda, MD 20892 USA.Leidos Biomed Res Inc, Frederick Natl Lab Canc Res, AIDS & Canc Virus Program, Frederick, MD 21701 USA.Univ Calif San Diego, Dept Chem & Biochem, La Jolla, CA 92093 USA.
    1. Year: 2019
    2. Date: MAY 22
  2. Journal: JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
  3. AMER CHEMICAL SOC,
    1. 141
    2. 20
    3. Pages: 8327-8338
  5. Type of Article: Article
  6. ISSN: 0002-7863
  1. Abstract:

    For HIV to become infectious, any new virion produced from an infected cell must undergo a maturation process that involves the assembly of viral polyproteins Gag and Gag-Pol at the membrane surface. The self-assembly of these viral proteins drives formation of a new viral particle as well as the activation of HIV protease, which is needed to cleave the polyproteins so that the final core sturcture of the virus will properly form. Molecules that interfere with HIV maturation will prevent any new virions from infecting additional cells. In this manuscript, we characterize the unique mechanism by which a mercaptobenzamide thioester small molecule (SAMT-247) interferes with HIV maturation via a series of selective acetylations at highly conserved cysteine and lysine residues in Gag and Gag-Pol polyproteins. The results provide the first insights into how acetylation can be utilized to perturb the process of HIV maturation and reveal a new strategy to limit the infectivity of HIV.

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External Sources

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  2. DOI: 10.1021/jacs.9b02743
  3. View record in Web of Science®
  4. WOS: 000469292300041

Library Notes

  1. Fiscal Year: FY2018-2019
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