期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 206, 期 -, 页码 -出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2020.112711
关键词
Coronaviruses; 3C-like protease (3CL(pro)) inhibitors; Peptidomimetic inhibitors; COVID-19; Proteolytic targeting chimaera (PROTAC)
资金
- National Natural Science Foundation of China [81602967, 81803784]
- China Postdoctoral Science Foundation [2016M592898XB, 2019M663921XB]
- Basic Research Program of Natural Science of Shaanxi Province [2019JQ779, 2020CGXNG-044, 19JC006, 2019JQ-484, 2019JQ-252]
- Basic Research Plan of the Education Department of Shaanxi Province [19JC006]
- College Students' Innovative Entrepreneurial Training Program [201510708172, 201610708019, 2019107080827]
This review fully describes the coronavirus 3CL(pro) peptidomimetic inhibitors and nonpeptidic small molecule inhibitors developed from 2010 to 2020. Specifically, the structural characteristics, binding modes and SARs of these 3CL(pro) inhibitors are expounded in detail by division into two categories: peptidomimetic inhibitors mainly utilize electrophilic warhead groups to covalently bind the 3CLpro Cys145 residue and thereby achieve irreversible inhibition effects, whereas nonpeptidic small molecule inhibitors mainly interact with residues in the S1', S1, S2 and S4 pockets via hydrogen bonds, hydrophobic bonds and van der Waals forces. Based on the emerging PROTAC technology and the existing 3CL(pro) inhibitors, 3CL(pro) PROTAC degraders are hypothesised to be next-generation anti-coronavirus drugs. (C) 2020 Elsevier Masson SAS. All rights reserved.
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