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Authentic HIV-1 integrase inhibitors

  1. Author:
    Liao, C. Z.
    March, C.
    Burke, T. R.
    Pommier, Y.
    Nicklaus, M. C.

  2. Author Address

    [Liao, Chenzhong; Burke, Terrence R., Jr.; Nicklaus, Marc C.] NCI, Biol Chem Lab, Ctr Canc Res, NIH,DHHS, Frederick, MD 21702 USA. [Marchand, Christophe; Pommier, Yves] NCI, Mol Pharmacol Lab, Ctr Canc Res, NIH,DHHS, Bethesda, MD 20892 USA.;Nicklaus, MC, NCI, Biol Chem Lab, Ctr Canc Res, NIH,DHHS, Frederick, MD 21702 USA.;mn1@helix.nih.gov
    1. Year: 2010
    2. Date: Jul
  2. Journal: Future Medicinal Chemistry
    1. 2
    2. 7
    3. Pages: 1107-1122
  4. Type of Article: Review
  5. ISSN: 1756-8919
  1. Abstract:

    HIV-1 integrase (IN) is indispensable for HIV-1 replication and has become a validated target for developing anti-AIDS agents. In two decades of development of IN inhibition-based anti-HIV therapeutics, a significant number of compounds were identified as IN inhibitors, but only some of them showed antiviral activity. This article reviews a number of patented HIV-1 IN inhibitors, especially those that possess high selectivity for the strand transfer reaction. These compounds generally have a polar coplanar moiety, which is assumed to chelate two magnesium ions in the binding site. Resistance to those compounds, when given to patients, can develop as a result of IN mutations. We refer to those compounds as authentic IN inhibitors. Continued drug development has so far delivered one authentic IN inhibitor to the market (raltegravir in 2007). Current and future attention will be focused on the development of novel authentic IN inhibitors with the goal of overcoming viral resistance.

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External Sources

  1. View Full Text
  2. DOI: 10.4155/fmc.10.199
  3. View record in Web of Science®
  4. WOS: 000280430900014

Library Notes

  1. Fiscal Year: FY2009-2010
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