整合酶：抗病毒方案中的关键酶概述。

The Integrase: An Overview of a Key Player Enzyme in the Antiviral Scenario.

机构信息

Neuroscienze, Psicologia, Area del Farmaco e Salute del Bambino (NEUROFARBA) Department, Sezione di Scienze Farmaceutiche e Nutraceutiche, University of Florence, Via Ugo Schiff 6, Sesto Fiorentino, 50019 Florence, Italy.

出版信息

Int J Mol Sci. 2023 Jul 29;24(15):12187. doi: 10.3390/ijms241512187.

DOI:10.3390/ijms241512187

PMID:37569561

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10419282/

Abstract

Integration of a desossiribonucleic acid (DNA) copy of the viral ribonucleic acid (RNA) into host genomes is a fundamental step in the replication cycle of all retroviruses. The highly conserved virus-encoded Integrase enzyme (IN; EC 2.7.7.49) catalyzes such a process by means of two consecutive reactions named 3'-processing (3-P) and strand transfer (ST). The Authors report and discuss the major discoveries and advances which mainly contributed to the development of Human Immunodeficiency Virus (HIV) -IN targeted inhibitors for therapeutic applications. All the knowledge accumulated over the years continues to serve as a valuable resource for the design and development of effective antiretroviral drugs.

摘要

整合病毒核糖核酸（RNA）的去氧核糖核酸（DNA）拷贝到宿主基因组中是所有逆转录病毒复制周期的一个基本步骤。高度保守的病毒编码整合酶（IN；EC 2.7.7.49）通过两种连续的反应（分别命名为 3’-加工（3-P）和链转移（ST））催化这一过程。作者报告并讨论了主要的发现和进展，这些发现和进展主要促成了针对治疗应用的人类免疫缺陷病毒（HIV）-IN 靶向抑制剂的开发。多年来积累的所有知识继续为设计和开发有效的抗逆转录病毒药物提供宝贵的资源。