第41页
小分子
七肽重复区
人类免疫缺陷病毒(HIV)
脂质双层融合
化学
恩夫韦肽
螺旋束
细胞生物学
计算生物学
生物
生物化学
蛋白质结构
肽序列
膜
病毒学
遗传学
表位
抗原
基因
作者
Guangyuan Zhou,Shidong Chu
标识
DOI:10.2174/1381612811319100006
摘要
Gp41 is regarded as an attractive target for development of HIV-1 entry inhibitors since it mediates the fusion process of HIV- 1 entry into the target cell through the six-helix bundle (6-HB) formation between its N-heptad repeat (NHR) and C-heptad repeat (CHR). Any chemical entity that disrupts the six-helix bundle formation may inhibit the fusion process, thereby blocking HIV-1 entry into the target cells. A brief review of discovering small molecule inhibitors targeting gp41 is presented here, including the development of assay methods, current known small molecule inhibitors and their binding mode studies. Lessons learned and challenges remained in view of blocking protein-protein interaction between NHR and CHR are also discussed. Keywords: gp41, HIV-1, assay, small molecule inhibitor, protein-protein interaction
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