Mass spectrometry reveals potential of β-lactams as SARS-CoV-2 Mpro inhibitors. Issue 12 (19th January 2021)

• Record Type: Journal Article
• Authors: Malla, Tika R.; Tumber, Anthony; John, Tobias; Brewitz, Lennart; Strain-Damerell, Claire; Owen, C David; Lukacik, Petra; Chan, H. T. Henry; Maheswaran, Pratheesh; Salah, Eidarus; Duarte, Fernanda; Yang, Haitao; Rao, Zihe; Walsh, Martin A.; Schofield, Christopher J.
• Is Part Of: Chemical communications. Volume 57:Issue 12(2021)
• Page Start: 1430
• Page End: 1433
• Publication Date: 2021-01-19
• Subjects: Chemistry -- Periodicals; 540
• DOI: 10.1039/d0cc06870e
• Languages: English
• ISSNs: 1359-7345

Abstract

Abstract : A high-throughput mass spectrometry based M pro assay identifies penicillin esters as new SARS-CoV-2 M pro inhibitors. Abstract : The main viral protease (M pro ) of SARS-CoV-2 is a nucleophilic cysteine hydrolase and a current target for anti-viral chemotherapy. We describe a high-throughput solid phase extraction coupled to mass spectrometry M pro assay. The results reveal some β-lactams, including penicillin esters, are active site reacting M pro inhibitors, thus highlighting the potential of acylating agents for M pro inhibition.