Journal
CHEMMEDCHEM
Volume 17, Issue 4, Pages -Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.202100582
Keywords
M-pro inhibition; SARS-CoV-2; COVID-19; ebselen; ebsulfur; nucleophilic cysteine protease
Categories
Funding
- Biotechnology and Biological Research Council
- Cancer Research UK
- Wellcome Trust [106244/Z/14/Z]
- King Abdulaziz University, Saudi Arabia
- BBSRC [BB/M011224/1]
- Oxford Covid Development Fund
- BBSRC [BB/V003291/1, BB/M011224/1] Funding Source: UKRI
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The study suggests that there is room for optimization of sulfur analogues for improved inhibition of M-pro mediated by ebselen/ebselen derivatives, particularly in terms of enhanced selectivity.
The reactive organoselenium compound ebselen is being investigated for treatment of coronavirus disease 2019 (COVID-19) and other diseases. We report structure-activity studies on sulfur analogues of ebselen with the Severe Acute Respiratory Syndrome coronavirus 2 (SARS-CoV-2) main protease (M-pro), employing turnover and protein-observed mass spectrometry-based assays. The results reveal scope for optimisation of ebselen/ebselen derivative- mediated inhibition of M-pro, particularly with respect to improved selectivity.
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