抗艾滋病药物设计新策略：多靶点及多价态结合配体  

Novel strategies in rational design of anti-HIV agents:multitarget and multivalency ligands

作　　者：展鹏[1] 李潇[1] 康东伟[1] 刘新泳[1] 

机构地区：[1]山东大学药学院药物化学研究所、化学生物学教育部重点实验室,山东济南250012

出　　处：《中国药物化学杂志》2013年第5期406-416,共11页Chinese Journal of Medicinal Chemistry

基　　金：重大国际合作项目(30910103908);国家自然科学基金项目(81102320,81273354)

摘　　要：HIV是艾滋病(AIDS)的主要病原体,由于目前临床药物严重的耐药性问题以及长期应用的毒副作用,研发高效抗耐药的抗艾滋病药物及全新疗法是当前药物化学领域的研究热点。近年来,多靶点和多价态结合药物越来越受到研究者的关注,并且成为合理设计抗艾滋病药物的新途径。本文结合具体实例综述了合理设计多靶点及多价态抗艾滋病药物的新进展,并对目前存在的问题和研究趋势进行了总结和展望,为发现新一代抗HIV药物提供重要信息。Human immunodeficiency virus type 1 （ HIV-1 ） is the etiological agent of acquired irnmunodeficiency syndrome（AIDS）. Emergence of drug-resistant HIV-1 mutants and side effects impede the long-term usage of drugs,requiring a significant need for new strategies of drug discovery and alternative therapeutic agents or protocols. More recently, among the most promising strategies, design of multitarget-directed ligands （MTDLs） and multivalency ligands have gained increasing acceptance. The exploration of MTDLs and multivalency ligands strategy should be valuable in anti-HIV drug discovery. In this review, current knowledge, challenges and outlook for the rational design of the multitarget and multivalency anti-HIV agents are described and a number of illustrative examples are given to highlight the representative rational design paradigms, and to help medicinal chemists discover the next generation of anti-HIV agents.

关 键 词：HIV 艾滋病 多靶点药物 多价态结合药物 药物设计 

分 类 号：R914[医药卫生—药物化学]