2020 年至 2022 年 SARS-CoV-2 主蛋白酶抑制剂的研究进展。

The research progress of SARS-CoV-2 main protease inhibitors from 2020 to 2022.

机构信息

Wuya College of Innovation, Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang, 110016, China.

Institute of Structural Pharmacology & TCM Chemical Biology, College of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou, 350122, China.

出版信息

Eur J Med Chem. 2023 Sep 5;257:115491. doi: 10.1016/j.ejmech.2023.115491. Epub 2023 May 22.

DOI:10.1016/j.ejmech.2023.115491

PMID:37244162

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10201905/

Abstract

The novel coronavirus disease 2019 (COVID-19) caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has spread worldwide. The main protease (M) of SARS-CoV-2 plays a central role in viral replication and transcription and represents an attractive drug target for fighting COVID-19. Many SARS-CoV-2 M inhibitors have been reported, including covalent and noncovalent inhibitors. The SARS-CoV-2 M inhibitor PF-07321332 (Nirmatrelvir) designed by Pfizer has been put on the market. This paper briefly introduces the structural characteristics of SARS-CoV-2 M and summarizes the research progress of SARS-CoV-2 M inhibitors from the aspects of drug repurposing and drug design. These information will provide a basis for the drug development of treating the infection of SARS-CoV-2 and even other coronaviruses in the future.

摘要

新型冠状病毒病 2019（COVID-19）由严重急性呼吸综合征冠状病毒 2（SARS-CoV-2）引起，已在全球范围内传播。SARS-CoV-2 的主要蛋白酶（M）在病毒复制和转录中起着核心作用，是抗击 COVID-19 的一个有吸引力的药物靶点。已经报道了许多 SARS-CoV-2 M 抑制剂，包括共价和非共价抑制剂。辉瑞公司设计的 SARS-CoV-2 M 抑制剂 PF-07321332（Nirmatrelvir）已上市。本文简要介绍了 SARS-CoV-2 M 的结构特征，并从药物再利用和药物设计两个方面总结了 SARS-CoV-2 M 抑制剂的研究进展。这些信息将为未来治疗 SARS-CoV-2 甚至其他冠状病毒感染的药物开发提供依据。