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NCp7: targeting a multitask protein for next-generation anti-HIV drug development part 2. Noncovalent inhibitors and nucleic acid binders.
Drug Discovery Today ( IF 7.4 ) Pub Date : 2018-01-08 , DOI: 10.1016/j.drudis.2018.01.022
Nunzio Iraci 1 , Oriana Tabarrini 2 , Claudio Santi 2 , Luca Sancineto 3
Affiliation  

Nucleocapsid protein 7 (NCp7) represents a viable target not yet reached by the currently available antiretrovirals. It is a small and highly basic protein, which is essential for multiple stages of the viral replicative cycle, with its structure preserved in all viral strains, including clinical isolates. NCp7 can be inhibited covalently, noncovalently and by shielding the nucleic acid (NA) substrates of its chaperone activity. Although covalent NCp7 inhibitors have already been detailed in the first part of this review series, the focus here is based on noncovalent and NA-binder inhibitors and on the analysis of the NCp7 3D structure to deliver fruitful insights for future drug design strategies.

中文翻译:

NCp7:针对下一代抗HIV药物开发第2部分的多任务蛋白。非共价抑制剂和核酸结合剂。

核衣壳蛋白7(NCp7)代表了目前可用的抗逆转录病毒药物尚未达到的可行目标。它是一种小型且高度碱性的蛋白质,对于病毒复制周期的多个阶段都是必不可少的,其结构保留在所有病毒株中,包括临床分离株。可以共价,非共价抑制NCp7,也可以通过屏蔽核酸(NA)底物的分子伴侣活性来抑制NCp7。尽管共价NCp7抑制剂已在本综述系列的第一部分中进行了详细介绍,但此处的重点是基于非共价和NA结合剂抑制剂以及对NCp7 3D结构的分析,以为未来的药物设计策略提供有益的见解。
更新日期:2018-01-08
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