tetano
Editor, Senior Moderator
Eur J Med Chem
. 2024 Feb 24:268:116263.
doi: 10.1016/j.ejmech.2024.116263. Online ahead of print. Synthesis and biological evaluation of novel peptidomimetic inhibitors of the coronavirus 3C-like protease
Franck Amblard[SUP] 1 [/SUP], Julia C LeCher[SUP] 2 [/SUP], Ramyani De[SUP] 2 [/SUP], Shaoman Zhou[SUP] 2 [/SUP], Peng Liu[SUP] 2 [/SUP], Shu Ling Goh[SUP] 2 [/SUP], Sijia Tao[SUP] 2 [/SUP], Dharmeshkumar Patel[SUP] 2 [/SUP], Jessica Downs-Bowen[SUP] 2 [/SUP], Keivan Zandi[SUP] 2 [/SUP], Huanchun Zhang[SUP] 2 [/SUP], Gitika Chaudhry[SUP] 2 [/SUP], Tamara McBrayer[SUP] 2 [/SUP], Michael Muczynski[SUP] 3 [/SUP], Abdullah Al-Homoudi[SUP] 3 [/SUP], Joseph Engel[SUP] 3 [/SUP], Shuiyun Lan[SUP] 2 [/SUP], Stefan G Sarafianos[SUP] 2 [/SUP], Ladislau C Kovari[SUP] 3 [/SUP], Raymond F Schinazi[SUP] 4 [/SUP]
Affiliations
Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), and related variants, are responsible for the devastating coronavirus disease 2019 (COVID-19) pandemic. The SARS-CoV-2 main protease (Mpro) plays a central role in the replication of the virus and represents an attractive drug target. Herein, we report the discovery of novel SARS-CoV-2 Mpro covalent inhibitors, including highly effective compound NIP-22c which displays high potency against several key variants and clinically relevant nirmatrelvir Mpro E166V mutants.
Keywords: 3CL(pro); Antivirals; HCoV-OC43; Main protease; Mpro; NIP-22c; Peptides; SARS-CoV-2.
. 2024 Feb 24:268:116263.
doi: 10.1016/j.ejmech.2024.116263. Online ahead of print. Synthesis and biological evaluation of novel peptidomimetic inhibitors of the coronavirus 3C-like protease
Franck Amblard[SUP] 1 [/SUP], Julia C LeCher[SUP] 2 [/SUP], Ramyani De[SUP] 2 [/SUP], Shaoman Zhou[SUP] 2 [/SUP], Peng Liu[SUP] 2 [/SUP], Shu Ling Goh[SUP] 2 [/SUP], Sijia Tao[SUP] 2 [/SUP], Dharmeshkumar Patel[SUP] 2 [/SUP], Jessica Downs-Bowen[SUP] 2 [/SUP], Keivan Zandi[SUP] 2 [/SUP], Huanchun Zhang[SUP] 2 [/SUP], Gitika Chaudhry[SUP] 2 [/SUP], Tamara McBrayer[SUP] 2 [/SUP], Michael Muczynski[SUP] 3 [/SUP], Abdullah Al-Homoudi[SUP] 3 [/SUP], Joseph Engel[SUP] 3 [/SUP], Shuiyun Lan[SUP] 2 [/SUP], Stefan G Sarafianos[SUP] 2 [/SUP], Ladislau C Kovari[SUP] 3 [/SUP], Raymond F Schinazi[SUP] 4 [/SUP]
Affiliations
- PMID: 38432056
- DOI: 10.1016/j.ejmech.2024.116263
Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), and related variants, are responsible for the devastating coronavirus disease 2019 (COVID-19) pandemic. The SARS-CoV-2 main protease (Mpro) plays a central role in the replication of the virus and represents an attractive drug target. Herein, we report the discovery of novel SARS-CoV-2 Mpro covalent inhibitors, including highly effective compound NIP-22c which displays high potency against several key variants and clinically relevant nirmatrelvir Mpro E166V mutants.
Keywords: 3CL(pro); Antivirals; HCoV-OC43; Main protease; Mpro; NIP-22c; Peptides; SARS-CoV-2.