Institute of Pharmacy, Pharmaceutical/Medicinal Chemistry and Tuebingen Center for Academic Drug Discovery, Eberhard Karls University Tübingen, Auf der Morgenstelle 8, 72076 Tübingen, Germany; School of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, PO Box 1627, FI-70211 Kuopio, Finland; Cluster of Excellence iFIT (EXC 2180) 'Image-Guided and Functionally Instructed Tumor Therapies', University of Tübingen, 72076 Tübingen, Germany.
Institute of Pharmacy, Pharmaceutical/Medicinal Chemistry and Tuebingen Center for Academic Drug Discovery, Eberhard Karls University Tübingen, Auf der Morgenstelle 8, 72076 Tübingen, Germany; Cluster of Excellence iFIT (EXC 2180) 'Image-Guided and Functionally Instructed Tumor Therapies', University of Tübingen, 72076 Tübingen, Germany.
Drug Discov Today. 2023 Jun;28(6):103579. doi: 10.1016/j.drudis.2023.103579. Epub 2023 Apr 5.
The severe acute respiratory syndrome-coronavirus 2 (SARS-CoV-2) is the causative factor behind the 2019 global coronavirus pandemic (COVID-19). The main protease, known as M, is encoded by the viral genome and is essential for viral replication. It has also been an effective target for drug development. In this review, we discuss the rationale for inhibitors that specifically target SARS-CoV-2 M. Small molecules and peptidomimetic inhibitors are two types of inhibitor with various modes of action and we focus here on novel inhibitors that were only discovered during the COVID-19 pandemic highlighting their binding modes and structures.
严重急性呼吸综合征冠状病毒 2(SARS-CoV-2)是导致 2019 年全球冠状病毒大流行(COVID-19)的病原体。主要蛋白酶,又称 M,由病毒基因组编码,是病毒复制所必需的。它也是药物开发的有效靶点。在这篇综述中,我们讨论了专门针对 SARS-CoV-2 M 的抑制剂的基本原理。小分子和拟肽抑制剂是两种具有不同作用模式的抑制剂,我们在这里重点介绍仅在 COVID-19 大流行期间发现的新型抑制剂,强调它们的结合模式和结构。