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Review Article

从认识到反应机制:HIV-1蛋白酶与其天然靶点相互作用的综述

卷 27, 期 15, 2020

页: [2514 - 2549] 页: 36

弟呕挨: 10.2174/0929867325666181113122900

价格: $65

摘要

目前对人类免疫缺陷病毒蛋白酶(HIV-1 PR)作为治疗艾滋病的药物靶点的研究需要更新，以促进进一步开发具有更好抑制活性的有前途的抑制剂。在过去的20年里，每年都有多达100篇关于HIV-1 PR的抑制和催化机制的学术报告发表。但没有关于HIV-1 PR作用导致感染性病毒粒子释放的基本文献综述。本文就HIV-1 PR涉及其天然靶点的识别模式和反应机制提供了最新进展(计算和实验)。这篇评论收录了80多篇来自著名期刊的文章。该酶及其突变类似物对天然Gag和Gag- pol裂解连接的识别首次被提出。随后，对文献中HIV-1 PR对其天然多肽序列的酶促作用机制进行了全面的剖析。此外，我们强调了正在进行的研究课题，利用硅方法可以在分子水平上对HIV-1蛋白酶的自然底物的催化机制提供更深入的见解。了解HIV-1 PR的识别和催化机制，导致感染病毒粒子的释放，并有意影响免疫系统，将有助于设计基于机制的抑制剂，提高生物活性。

关键词: HIV-1 PR，自然底物，识别模式，反应机制，过渡状态模型，免疫系统。

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