| Literature DB >> 20600105 |
Tadashi Satoh1, Mi Li, Jeffrey-Tri Nguyen, Yoshiaki Kiso, Alla Gustchina, Alexander Wlodawer.
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.Entities:
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Year: 2010 PMID： 20600105 PMCID： PMC2918672 DOI： 10.1016/j.jmb.2010.06.052
Source DB: PubMed Journal: J Mol Biol ISSN： 0022-2836 Impact factor: 5.469