HIV-1 NNRTIs耐药性产生的结构基础及分子机制
Structural Basis and Molecular Mechanisms of Resistance to Non-nucleoside inhibitors of HIV-1 Reverse Transcriptase
目的 综述HIV-1 NNRTIs耐药性产生的结构基础及分子机制。方法 以近几年有代表性的论文为依据，进行分析、整理和归纳。结果与结论 HIV-1 NNRTIs耐药性产生的结构基础是由于结合位点的氨基酸突变；在分子水平上，HIV-1突变株主要通过使RT/NNRTI之间关键性疏水性作用、立体位阻、电性分布及氢键作用发生改变，导致耐药性的产生。对NNRTIs耐药性产生的结构基础及分子机制的认识有助于设计新一代的抗耐药性抑制剂。
OBJECTIVE In this review, the structural basis and molecular mechanisms of resistance to non-nucleoside inhibitors of HIV-1 reverse transcriptase, are described. METHODS Retrieve and analysis of related literacture published in recent years. CONCLUSION There are three primary mechanisms by which a mutation can confer resistance to NNRTIs: loss or changes of Van Der Waals interactions; steric hindrance with the inhibitor; and change of electrostatic charge or hydrogen bonding properties. Understanding mechanisms of NNRTIs resistance is necessary for successful designs in the next generation of anti-HIV-1 drugs.
展鹏、刘新泳
基础医学分子生物学药学
获得性免疫缺陷综合征艾滋病毒非核苷类逆转录酶抑制剂耐药性分子机制
IDSHIVNNRTIsdrug resistancemolecular mechanisms
展鹏,刘新泳.HIV-1 NNRTIs耐药性产生的结构基础及分子机制[EB/OL].(2009-06-23)[2025-08-02].http://www.paper.edu.cn/releasepaper/content/200906-637.点此复制
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