HIV-1 drug discovery: targeting folded RNA structures with branched peptides.

HIV-1 drug discovery: targeting folded RNA structures with branched peptides.
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DOI:
10.1039/c5ob00589b
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发表时间:
2015-06-07
影响因子:
3.2
通讯作者:
Santos WL
Santos WL
中科院分区:
化学3区
文献类型:
--
作者:
Wynn JE;Santos WL

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人类免疫缺陷病毒1型(HIV-1)是一种容易发生高变异率的RNA病毒。虽然目前的抗逆转录病毒疗法可以控制这种疾病,但需要具有新作用模式的药物。实现这一目标的一种策略是以保守的RNA结构的天然三维折叠为目标。这种观点强调了中等大小的多肽和多肽仿制药用于靶向HIV-1的两个保守的RNA结构。特别是,支化肽具有以多价方式结合的能力,利用较大的表面积来实现对目标RNA的必要亲和力和选择性。
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.