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有机化学
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有机化学 ›› 2010, Vol. 30 ›› Issue (04): 477-485.    下一篇

综述与进展

HIV整合酶抑制剂的研究进展

郭涤亮1,2，刘冠男1，周宇1，李建1，徐进宜2，蒋华良1，陈凯先1，柳红*,1,2   

  1. (1中国科学院上海药物研究所 新药研究国家重点实验室药物设计和发现中心 上海 201203)
    (2中国药科大学药学院 南京210009)
  • 收稿日期:2009-04-16 修回日期:2009-08-06 发布日期:2010-04-28
  • 通讯作者: 柳红 E-mail:hliu@mail.shcnc.ac.cn
  • 基金资助:

    国家级.863计划

Research Progress in HIV Integrase Inhibitors

Guo Diliang1,2 Liu Guannan1 Zhou Yu1, Li Jian1 Xu Jinyi2 Jiang Hualiang1 Chen Kaixian1 Liu Hong*,1,2   

  1. (1 Drug Discovery and Design Centre, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203)
    (2 School of Pharmacy, China Pharmaceutical University, Nanjing 210009)
  • Received:2009-04-16 Revised:2009-08-06 Published:2010-04-28
  • Contact: Hong Liu E-mail:hliu@mail.shcnc.ac.cn

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HIV整合酶是病毒DNA复制所必需的3个基本酶之一, 是新批准上市的抗艾滋病药物Raltegravir (MK-0518, Isentress)的分子靶标. HIV整合酶抑制剂已经成为新一类治疗获得性免疫缺陷综合症的药物. 对HIV整合酶抑制剂的研究进展进行了综述, 为研究新型人类免疫缺陷病毒整合酶抑制剂提供参考.

关键词: 人类免疫缺陷病毒, 整合酶抑制剂, 二酮酸类, Raltegravir

HIV integrase is one of the three essential enzymes for viral DNA replication and the molecular target of the newly approved anti-AIDS drug raltegravir (MK-0518, Isentress). HIV integrase inhibitors have emerged as a new class of drugs for the treatment of AIDS. In this article, the recent progress of HIV integrase inhibitors is reviewed to provide some useful information for the further research and development of HIV integrase inhibitors.

Key words: HIV, integrase inhibitor, diketoacid, Raltegravir