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HIV-1 NNRTIs耐药性产生的结构基础及分子机制

发表时间:2010-06-15  浏览量:1460  下载量:729
全部作者: 展鹏,刘新泳
作者单位: 山东大学药学院药物化学研究所
摘 要: 目的:综述HIV-1非核苷类逆转录酶抑制剂(non-nucleoside reverse transcriptase inhibitors,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。结论:HIV-1 NNRTIs耐药性产生的结构基础是结合位点的氨基酸突变;在分子水平上,HIV-1突变株主要通过使逆转录酶(reverse transcriptase, RT)/NNRTIs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抗耐药性抑制剂。
关 键 词: 药物化学;获得性免疫缺陷综合征;综述;人类免疫缺陷病毒;非核苷类逆转录酶抑制剂;耐药性;分子机制
Title: Structural basis and molecular mechanisms of resistance to non-nucleoside inhibitors of HIV-1 reverse transcriptase
Author: ZHAN Peng, LIU Xinyong
Organization: Institute of Medicinal Chemistry, School of Pharmacy, Shandong University
Abstract: Objective: In this paper, the structural basis and molecular mechanisms of resistance to HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) are described. Methods: Retrieve and analysis of related literature published in recent years. Conclusion: Structural basis of resistance to NNRTIs is the mutants around the NNRTIs binding site. 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.
Key words: medicinal chemistry; acquired immune deficiency syndrome; review; human immunodeficiency virus; non-nucleoside reverse transcriptase inhibitors; drug resistance; molecular mechanisms
发表期数: 2010年6月第11期
引用格式: 展鹏,刘新泳. HIV-1 NNRTIs耐药性产生的结构基础及分子机制[J]. 中国科技论文在线精品论文,2010,3(11):1086-1093.
 
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