Skip NavigationSkip to Content
Return Return to Search Results

HIV-1 Integrase and Virus and Cell DNAs: Complex Formation and Perturbation by Inhibitors of Integration

  1. Author:
    Hobaika, Z.
    Zargarian, L.
    Maroun, R. G.
    Mauffret, O.
    Burke, T. R.
    Ferm, jian

  2. Author Address

    [Hobaika, Z.; Zargarian, L.; Mauffret, O.; Fermandjian, S.] Ecole Normale Super, Lab Biotechnol & Pharmacol Genet Appl, UMR 8113, CNRS, F-94235 Cachan, France. [Maroun, R. G.] Univ St Joseph, Fac Sci, Dept Sci Vie & Terre, CST Mar Roukos, Beirut, Lebanon. [Burke, T. R., Jr.] NCI, Med Chem Lab, Ctr Canc Res, NIH, Frederick, MD 21702 USA.;Fermandjian, S, Ecole Normale Super, Lab Biotechnol & Pharmacol Genet Appl, UMR 8113, CNRS, 61 Ave President Wilson, F-94235 Cachan, France.;serge.fermandjian@lbpa.ens-cachan.fr
    1. Year: 2010
    2. Date: Jun
  2. Journal: Neurochemical Research
    1. 35
    2. 6
    3. Pages: 888-893
  4. Type of Article: Proceedings Paper
  5. ISSN: 0364-3190
  1. Abstract:

    HIV-1 integrase (IN) catalyzes integration of viral DNA into cell DNA through 3'-processing of viral DNA and strand transfer reactions. To learn on binding of IN to DNAs and IN inhibition we applied spectroscopy (circular dichroism, fluorescence) in a simplified model consisting in a peptide analogue (K156) of alpha 4 helix involved in recognition of viral and cell DNA; an oligonucleotide corresponding to the U5' LTR DNA end; and an inhibitor (TB11) of the diketo acid (DKA) family. Results extrapolated to IN show that: the enzyme binds viral DNA with high affinity and specificity, but cell DNA with low affinity and specificity; the affinity of TB11 for IN is high enough to impair the binding of IN to cell DNA, but not to viral DNA. This explains why TB11 is an inhibitor of strand transfer but not of 3'-processing. These results can help in the search of new IN inhibitors.

    See More

  1. Keywords:

External Sources

  1. View Full Text
  2. DOI: 10.1007/s11064-009-0098-2
  3. View record in Web of Science®
  4. WOS: 000278028100007

Library Notes

  1. Fiscal Year: FY2009-2010
NCI at Frederick

You are leaving a government website.

This external link provides additional information that is consistent with the intended purpose of this site. The government cannot attest to the accuracy of a non-federal site.

Linking to a non-federal site does not constitute an endorsement by this institution or any of its employees of the sponsors or the information and products presented on the site. You will be subject to the destination site's privacy policy when you follow the link.

ContinueCancel