陈文敏 刘新泳. LEDGF/p75:  抗HIV-1感染的新靶点及其抑制剂研究J. 药学学报, 2009,44(9): 953-960.
引用本文: 陈文敏 刘新泳. LEDGF/p75:  抗HIV-1感染的新靶点及其抑制剂研究J. 药学学报, 2009,44(9): 953-960.
shu
CHEN Wen-Min, LIU Xin-Yong. LEDGF/p75: a novel target for anti-HIV therapy and advances in the study of its related inhibitorsJ. 药学学报, 2009,44(9): 953-960.
Citation: CHEN Wen-Min, LIU Xin-Yong. LEDGF/p75: a novel target for anti-HIV therapy and advances in the study of its related inhibitorsJ. 药学学报, 2009,44(9): 953-960.
shu

LEDGF/p75:  抗HIV-1感染的新靶点及其抑制剂研究

LEDGF/p75: a novel target for anti-HIV therapy and advances in the study of its related inhibitors

    摘要
  • 摘要:

    晶状体上皮源性生长因子 (lens epithelium-derived growth factor, LEDGF) 又名p75蛋白是人类免疫缺陷病毒1型 (human immunodeficiency virus type 1, HIV-1) 整合过程中不可缺少的细胞辅助因子。LEDGF/p75将整合酶链合到特定的DNA序列上, 促进链转移反应和整合的完成。LEDGF/p75对整合酶具有稳定作用, 在LEDGF/p75缺陷的感染细胞中, 整合酶很快被降解, HIV-1的复制和感染被阻断, 大量研究证明干扰LEDGF/p75的作用是抑制HIV复制感染的有效途径。而LEDGF/p75与整合酶结合的三维晶体结构已被解析, 并通过高通量筛选获得了该细胞辅助因子的抑制剂。本文综述了LEDGF/p75的结构功能、与整合酶作用的机制以及基于该细胞辅助因子的抑制剂研究。

     

    Abstract:

    LEDGF/p75 is a newly found cell cofactor, which plays an essential role in the integration     of HIV-1 cDNA into host chromosomes.  LEDGF/p75 tethers HIV integrase to chromatin, protects it from  degradation, and strongly influences the genome-wide pattern of HIV integration.  Depleting the protein from cells or over-expressing the integrase-binding domain of LEDGF/p75 blocks viral replication.  The essential role of LEDGF/p75 in HIV-1 replication makes it a new target for anti-HIV-1 drug development.  This article reviews the function of LEDGF/p75, LEDGF/p75-integrase interaction and LEDGF/p75 inhibitors.

     

    • HTML全文
    • 参考文献(0)
    • 相关文章
    • 施引文献
  • 资源附件(0)

/

返回文章
返回