非核苷类逆转录酶抑制剂结合诱导的HIV-1逆转录酶构象变化。
Conformational changes in HIV-1 reverse transcriptase induced by nonnucleoside reverse transcriptase inhibitor binding.
作者信息
Sluis-Cremer Nicolas, Temiz N Alpay, Bahar Ivet
机构信息
University of Pittsburgh, Department of Medicine, Division of Infectious Diseases, Pittsburgh, Pennsylvania 15261, USA.
出版信息
Curr HIV Res. 2004 Oct;2(4):323-32. doi: 10.2174/1570162043351093.
Abstract
Nonnucleoside reverse transcriptase inhibitors (NNRTI) are a group of small hydrophobic compounds with diverse structures that specifically inhibit HIV-1 reverse transcriptase (RT). NNRTIs interact with HIV-1 RT by binding to a single site on the p66 subunit of the p66/p51 heterodimeric enzyme, termed the NNRTI-binding pocket (NNRTI-BP). This binding interaction results in both short-range and long-range distortions of RT structure. In this article, we review the structural, computational and experimental evidence of the NNRTI-induced conformational changes in HIV-1 RT and relate them to the mechanism by which these compounds inhibit HIV-1 reverse transcription.
摘要
非核苷类逆转录酶抑制剂（NNRTI）是一组结构多样的小分子疏水性化合物，它们特异性抑制HIV-1逆转录酶（RT）。NNRTI通过与p66/p51异二聚体酶p66亚基上的一个位点结合来与HIV-1 RT相互作用，该位点称为NNRTI结合口袋（NNRTI-BP）。这种结合相互作用导致RT结构的短程和长程扭曲。在本文中，我们综述了NNRTI诱导HIV-1 RT构象变化的结构、计算和实验证据，并将它们与这些化合物抑制HIV-1逆转录的机制联系起来。
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