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Crystal Structures of Inhibitor Complexes of Human T-Cell Leukemia Virus (HTLV-1) Protease

  1. Author:
    Satoh, T.
    Li, M.
    Nguyen, J. T.
    Kiso, Y.
    Gustchina, A.
    Wlodawer, A.

  2. Author Address

    [Satoh, Tadashi; Li, Mi; Gustchina, Alla; Wlodawer, Alexander] NCI, Prot Struct Sect, Macromol Crystallog Lab, Ft Detrick, MD 21702 USA. [Li, Mi] SAIC Frederick, Basic Res Program, Frederick, MD USA. [Nguyen, Jeffrey-Tri; Kiso, Yoshiaki] Kyoto Pharmaceut Univ, Ctr Frontier Res Med Sci, Dept Med Chem, Yamashina Ku, Kyoto 6078412, Japan.;Wlodawer, A, NCI, Prot Struct Sect, Macromol Crystallog Lab, Ft Detrick, MD 21702 USA.;wlodawer@nih.gov
    1. Year: 2010
    2. Date: Aug
  2. Journal: Journal of Molecular Biology
    1. 401
    2. 4
    3. Pages: 626-641
  4. Type of Article: Article
  5. ISSN: 0022-2836
  1. Abstract:

    Human T-cell leukemia virus type 1 (HTLV-1) is a retrovirus associated with several serious diseases, such as adult T-cell leukemia and tropical spastic paraparesis/myelopathy. For a number of years, the protease (PR) encoded by HTLV-1 has been a target for designing antiviral drugs, but that effort was hampered by limited available structural information. We report a high-resolution crystal structure of HTLV-1 PR complexed with a statine-containing inhibitor, a significant improvement over the previously available moderate-resolution structure. We also report crystal structures of the complexes of HTLV-1 PR with five different inhibitors that are more compact and more potent. A detailed study of structure activity relationships was performed to interpret in detail the influence of the polar and hydrophobic interactions between the inhibitors and the protease. Published by Elsevier Ltd.

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External Sources

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  2. DOI: 10.1016/j.jmb.2010.06.052
  3. View record in Web of Science®
  4. WOS: 000281262400007

Library Notes

  1. Fiscal Year: FY2009-2010
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