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HIV-1反式激活抑制剂的研究进展 被引量：2

Recent advances on inhibitors of HIV-1 transactivation
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摘要 转录反式激活因子(Tat)在HIV-1的转录和复制过程中起着十分重要的调节作用。Tat蛋白与反式激活应答区(TAR)RNA及正向转录延伸因子(P-TEFb)形成三元复合物,不仅促使转录完全,并且显著提高转录效率。Tat蛋白对HIV-1转录水平的重要调控作用及其结构的高度保守使它成为研究抗艾滋病药物的新靶点。该文将简要介绍HIV-1 Tat介导的反式激活过程,并对近年报道的以TAR、Tat和P-TEFb为靶点的小分子抑制剂进行综述。 Trans-activator of transcription（Tat） plays a very important role in HIV-1 transcription and replication. Tat forms ternary complex with trans-activator response region（TAR） RNA and positive transcription elongation factor（P-TEFb）, which not only promotes the development of full-length HIV genome, but also significantly improves the efficiency of transcription. Its crucial regulatory role on transcription level and highly conservative structure make Tat an attractive new therapeutic target for anti-HIV drugs. Herein, the HIV-1 Tat-mediated transactivation were briefly introduced, and the small-molecule inhibitors against TAR, Tat and P-TEFb reported recently were reviewed.
作者 张传明 肖志艳 胡春 郭宗儒
机构地区 沈阳药科大学制药工程学院 中国医学科学院北京协和医学院药物研究所
出处 《中国药物化学杂志》 CAS CSCD 2008年第6期461-467,477,共8页 Chinese Journal of Medicinal Chemistry
基金 北京市自然科学基金项目(7082061)
关键词 构效关系 人类免疫缺陷病毒1型 转录反式激活因子 抑制剂 structure-activity relationship HIV- 1 trans-activator of transcription inhibitors
分类号 R978.7 [医药卫生—药品]
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参考文献30

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共引文献5

同被引文献23

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中国药物化学杂志
2008年 第6期

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