tetano
Editor, Senior Moderator
Bioorg Chem
. 2024 Apr 16:147:107380.
doi: 10.1016/j.bioorg.2024.107380. Online ahead of print. Non-peptidic inhibitors targeting SARS-CoV-2 main protease: A review
Ya-Qi Xiao[SUP] 1 [/SUP], Jiao Long[SUP] 1 [/SUP], Shuang-Shuang Zhang[SUP] 2 [/SUP], Yuan-Yuan Zhu[SUP] 3 [/SUP], Shuang-Xi Gu[SUP] 4 [/SUP]
Affiliations
The COVID-19 pandemic continues to pose a threat to global health, and sounds the alarm for research & development of effective anti-coronavirus drugs, which are crucial for the patients and urgently needed for the current epidemic and future crisis. The main protease (M[SUP]pro[/SUP]) stands as an essential enzyme in the maturation process of SARS-CoV-2, playing an irreplaceable role in regulating viral RNA replication and transcription. It has emerged as an ideal target for developing antiviral agents against SARS-CoV-2 due to its high conservation and the absence of homologous proteases in the human body. Among the SARS-CoV-2 M[SUP]pro[/SUP] inhibitors, non-peptidic compounds hold promising prospects owing to their excellent antiviral activity and improved metabolic stability. In this review, we offer an overview of research progress concerning non-peptidic SARS-CoV-2 M[SUP]pro[/SUP] inhibitors since 2020. The efforts delved into molecular structures, structure-activity relationships (SARs), biological activity, and binding modes of these inhibitors with M[SUP]pro[/SUP]. This review aims to provide valuable clues and insights for the development of anti-SARS-CoV-2 agents as well as broad-spectrum coronavirus M[SUP]pro[/SUP] inhibitors.
Keywords: Broad spectrum; COVID-19; Covalent inhibitors; Drug design; Main protease; Non-covalent inhibitors; Non-peptidic inhibitors; SARS-CoV-2.
. 2024 Apr 16:147:107380.
doi: 10.1016/j.bioorg.2024.107380. Online ahead of print. Non-peptidic inhibitors targeting SARS-CoV-2 main protease: A review
Ya-Qi Xiao[SUP] 1 [/SUP], Jiao Long[SUP] 1 [/SUP], Shuang-Shuang Zhang[SUP] 2 [/SUP], Yuan-Yuan Zhu[SUP] 3 [/SUP], Shuang-Xi Gu[SUP] 4 [/SUP]
Affiliations
- PMID: 38636432
- DOI: 10.1016/j.bioorg.2024.107380
The COVID-19 pandemic continues to pose a threat to global health, and sounds the alarm for research & development of effective anti-coronavirus drugs, which are crucial for the patients and urgently needed for the current epidemic and future crisis. The main protease (M[SUP]pro[/SUP]) stands as an essential enzyme in the maturation process of SARS-CoV-2, playing an irreplaceable role in regulating viral RNA replication and transcription. It has emerged as an ideal target for developing antiviral agents against SARS-CoV-2 due to its high conservation and the absence of homologous proteases in the human body. Among the SARS-CoV-2 M[SUP]pro[/SUP] inhibitors, non-peptidic compounds hold promising prospects owing to their excellent antiviral activity and improved metabolic stability. In this review, we offer an overview of research progress concerning non-peptidic SARS-CoV-2 M[SUP]pro[/SUP] inhibitors since 2020. The efforts delved into molecular structures, structure-activity relationships (SARs), biological activity, and binding modes of these inhibitors with M[SUP]pro[/SUP]. This review aims to provide valuable clues and insights for the development of anti-SARS-CoV-2 agents as well as broad-spectrum coronavirus M[SUP]pro[/SUP] inhibitors.
Keywords: Broad spectrum; COVID-19; Covalent inhibitors; Drug design; Main protease; Non-covalent inhibitors; Non-peptidic inhibitors; SARS-CoV-2.