人类免疫缺陷病毒1型（HIV-1）药物研发：用分支肽靶向折叠的RNA结构
HIV-1 drug discovery: targeting folded RNA structures with branched peptides.
作者信息
Wynn Jessica E, Santos Webster L
机构信息
Department of Chemistry and Virginia Tech Center for Drug Discovery, Virginia Tech, Blacksburg, Virginia 24061, USA.
出版信息
Org Biomol Chem. 2015 Jun 7;13(21):5848-58. doi: 10.1039/c5ob00589b.
Abstract
Human immunodeficiency virus type 1 (HIV-1) is an RNA virus that is prone to high rates of mutation. While the disease is managed with current antiretroviral therapies, drugs with a new mode of action are needed. A strategy towards this goal is aimed at targeting the native three-dimensional fold of conserved RNA structures. This perspective highlights medium-sized peptides and peptidomimetics used to target two conserved RNA structures of HIV-1. In particular, branched peptides have the capacity to bind in a multivalent fashion, utilizing a large surface area to achieve the necessary affinity and selectivity toward the target RNA.
摘要
1型人类免疫缺陷病毒（HIV-1）是一种易于发生高突变率的RNA病毒。虽然目前通过抗逆转录病毒疗法来控制该疾病，但仍需要具有新作用模式的药物。实现这一目标的一种策略是针对保守RNA结构的天然三维折叠。本文综述了用于靶向HIV-1的两种保守RNA结构的中等大小肽和肽模拟物。特别是，分支肽能够以多价方式结合，利用大的表面积来实现对靶RNA的必要亲和力和选择性。
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