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Crystal structures of inhibitor complexes of human T-cell leukemia virus (HTLV-1) protease.


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.

SUBMITTER: Satoh T 

PROVIDER: S-EPMC2918672 | biostudies-literature | 2010 Aug

REPOSITORIES: biostudies-literature

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Crystal structures of inhibitor complexes of human T-cell leukemia virus (HTLV-1) protease.

Satoh Tadashi T   Li Mi M   Nguyen Jeffrey-Tri JT   Kiso Yoshiaki Y   Gustchina Alla A   Wlodawer Alexander A  

Journal of molecular biology 20100630 4


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  ...[more]

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