Shulan International Medical College, Zhejiang Shuren University, Hangzhou, People's Republic of China.
Zhejiang Chinese Medical University, Hangzhou, People's Republic of China.
Drug Des Devel Ther. 2022 Apr 8;16:1067-1082. doi: 10.2147/DDDT.S359009. eCollection 2022.
Coronavirus disease 2019 (COVID-19) caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) currently poses a threat to human health. 3C-like proteinase (3CLpro) plays an important role in the viral life cycle. Hence, it is considered an attractive antiviral target protein. Whole-genome sequencing showed that the sequence homology between SARS-CoV-2 3CLpro and SARS-CoV 3CLpro is 96.08%, with high similarity in the substrate-binding region. Thus, assessing peptidomimetic inhibitors of SARS-CoV 3CLpro could accelerate the development of peptidomimetic inhibitors for SARS-CoV-2 3CLpro. Accordingly, we herein discuss progress on SARS-CoV-2 3CLpro peptidomimetic inhibitors. Inflammation plays a major role in the pathophysiological process of COVID-19. Small-molecule compounds targeting 3CLpro with both antiviral and anti-inflammatory effects are also briefly discussed in this paper.
由严重急性呼吸系统综合征冠状病毒 2（SARS-CoV-2）引起的 2019 年冠状病毒病（COVID-19）目前对人类健康构成威胁。3C 样蛋白酶（3CLpro）在病毒生命周期中发挥重要作用。因此，它被认为是一种有吸引力的抗病毒靶蛋白。全基因组测序显示，SARS-CoV-2 3CLpro 与 SARS-CoV 3CLpro 的序列同源性为 96.08%，底物结合区域具有高度相似性。因此，评估 SARS-CoV 3CLpro 的拟肽抑制剂可以加速 SARS-CoV-2 3CLpro 拟肽抑制剂的开发。因此，我们在此讨论 SARS-CoV-2 3CLpro 拟肽抑制剂的研究进展。炎症在 COVID-19 的病理生理过程中起主要作用。本文还简要讨论了具有抗病毒和抗炎作用的靶向 3CLpro 的小分子化合物。
