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Structure of the Catalytic Domain of Avian Sarcoma Virus Integrase With a Bound Hiv-1 Integrase-Targeted Inhibitor

  1. Author:
    Lubkowski, J.
    Yang, F.
    Alexandratos, J.
    Wlodawer, A.
    Zhao, H.
    Burke, T. R.
    Neamati, N.
    Pommier, Y.
    Merkel, G.
    Skalka, A. M.
    1. Year: 1998
  2. Journal: Proceedings of the National Academy of Sciences of the United States of America
    1. 95
    2. 9
    3. Pages: 4831-4836
  4. Type of Article: Article
  1. Abstract:

    The x-ray structures of an inhibitor complex of the catalytic core domain of avian sarcoma virus integrase (ASV IN) were solved at 1.9- to 2.0-Angstrom resolution at two pH values, with and without Mn2+ cations. This inhibitor (Y-3), originally identified in a screen for inhibitors of the catalytic activity of HIV type 1 integrase (HIV-1 IN), was found in the present study to be active against ASV IN as well as HIV-1 IN. The Y-3 molecule is located in close proximity to the enzyme active site, interacts with the flexible loop, alters loop conformation, and affects the conformations of active site residues. As crystallized, a Y-3 molecule stacks against its symmetry-related mate. Preincubation of IN with metal cations does not prevent inhibition, and Y-3 binding does not prevent binding of divalent cations to IN. Three compounds chemically related to Y-3 also were investigated, but no binding was observed in the crystals. Our results identify the structural elements of the inhibitor that likely determine its binding properties. [References: 36]

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