于生辉 谭艳梅 赵桂森. α, γ-二酮类HIV-1整合酶抑制剂研究进展J. 药学学报, 2010,45(2): 215-223.
引用本文: 于生辉 谭艳梅 赵桂森. α, γ-二酮类HIV-1整合酶抑制剂研究进展J. 药学学报, 2010,45(2): 215-223.
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XU Sheng-Hui, TAN Yan-Mei, DIAO Gui-Sen. Advances in the study of HIV-1 integrase inhibitors of α, γ-diketo compoundsJ. 药学学报, 2010,45(2): 215-223.
Citation: XU Sheng-Hui, TAN Yan-Mei, DIAO Gui-Sen. Advances in the study of HIV-1 integrase inhibitors of α, γ-diketo compoundsJ. 药学学报, 2010,45(2): 215-223.
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α, γ-二酮类HIV-1整合酶抑制剂研究进展

Advances in the study of HIV-1 integrase inhibitors of α, γ-diketo compounds

    摘要
  • 摘要:

    整合酶 (integrase, IN) 是人类免疫缺陷1型病毒 (human immunodeficiency virus-1, HIV-1) 复制过程必需的酶, 而人类细胞中没有该酶的类似物, 理论上抑制IN对人体副作用很小, 因此HIV-1 IN成为治疗艾滋病 (acquired immunodeficiency syndrome, AIDS) 合理的靶点。本文综述了近年来α, γ-二酮类IN抑制剂的发展现状, 为发展定量构效关系 (quantitative structure-activity relationship, QSAR)、进行虚拟筛选、确认药效团假说和指导合成活性更高的IN抑制剂提供参考。

     

    Abstract:

    HIV-1 integrase (IN) is an essential enzyme for retroviral replication.  There is no analogue for this enzyme in human cells so that inhibition of IN will not bring strong effect on human body.  Thus, HIV-1 IN has become a rational target for therapy of AIDS.  This review provides a comprehensive report of α, γ-diketo IN inhibitors discovered in recent years.  Compilation of such data will prove to be beneficial in developing QSAR, pharmacophore hypothesis generation and validation, virtual screening and synthesis of compounds with higher activity.

     

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