Identification of a small molecule HIV-1 inhibitor that targets the capsid hexamer.
Identification of a small molecule HIV-1 inhibitor that targets the capsid hexamer.
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DOI：
10.1016/j.bmcl.2015.12.087
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发表时间：
2016-02-01
影响因子：
2.7
通讯作者：
Cocklin S
中科院分区：
文献类型：
--
作者：
Xu JP;Branson JD;Lawrence R;Cocklin S
HIV-1 CA蛋白是开发新的抗病毒药物的一个有吸引力的治疗靶点。CA的六聚体结构中的原聚体间口袋是关键宿主依赖因子的结合位点，是小分子靶向的一个特别有吸引力的区域。利用已知与该区域相互作用的抑制剂衍生的基于场的药效团，结合生化和生物学评估，我们已经确定了一种抑制HIV-1感染的新化合物，并靶向组装的CA六聚体。
The HIV-1 CA protein is an attractive therapeutic target for the development of new antivirals. An inter-protomer pocket within the hexamer configuration of the CA, which is a binding site for key host dependency factors, is an especially appealing region for small molecule targeting. Using a field-based pharmacophore derived from an inhibitor known to interact with this region, coupled to biochemical and biological assessment, we have identified a new compound that inhibits HIV-1 infection and that targets the assembled CA hexamer.