新型HIV-1非核苷类逆转录酶抑制剂的结合模式特征与抗耐药抑制剂设计研究进展  

Recent advance on characteristics of HIV-1 non-nucleoside reverse transcriptase inhibitors binding modes and design strategies to overcome drug-resistance

作　　者：展鹏[1] 刘新泳[1] 

机构地区：[1]山东大学药学院药物化学研究所,山东济南250012

出　　处：《中国药物化学杂志》2009年第3期228-236,共9页Chinese Journal of Medicinal Chemistry

基　　金：国家自然科学基金项目(30371686;30772629;30873133);科技部国际合作重点项目(2003DF000033);教育部博士点基金项目(070422083)

摘　　要：新一代抗耐药的HIV-1非核苷类逆转录酶抑制剂(NNRTIs)具有较高的柔韧性,能与氨基酸主链形成氢键作用,它能特异性靶向结合位点的保守性区域,且结合模式独特,属于缓慢-紧密型抑制剂。该文综述了新一代HIV-1NNRTIs的结合模式特征,为新型抗耐药抑制剂的设计提供有价值的参考。The availability of structural information revealing classic or distinctive binding modes for NNRTIs will assist in novel inhibitor design. Conformational flexibility, extensive main chain hydrogen bonding, specific targeting highly conserved residues, slow-, tight-binding and distinctive binding modes are main characteristics of next generation NNRTIs that is effective against a wide range of existing drug-resistant HIV-1 viral variants. In this article,the characteristics of novel HIV-1 NNRTIs binding modes are reviewed in order to pave way for novel drug design.

关 键 词：HIV-1 逆转录酶 非核苷类逆转录酶抑制剂 耐药性 药物设计 

分 类 号：R914[医药卫生—药物化学]