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Silaproline-bearing nirmatrelvir derivatives are potent inhibitors of the SARS-CoV-2 main protease highlighting the value of silicon-derivatives in structure-activity-relationship studies

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Year: 2025
Type: article
Abstract: and, by implication, other nucleophilic cysteine enzymes.
Source: European Journal of Medicinal Chemistry
DOI: 10.1016/j.ejmech.2025.117603
Authors: Dóra Laczi, Sofia Schönbauer Huamán, Taylah Andrews-Clark, Stephen M. Laidlaw, Eidarus Salah, Leo Dumjahn, Petra Lukacik, Hani Choudhry, Martin A. Walsh, Miles W. Carroll, Christopher J. Schofield, Lennart Brewitz
Institutions: University of Oxford, Diamond Light Source, Research Complex at Harwell, Centre for Human Genetics, King Abdulaziz University
Language: English

Topic: SARS-CoV-2 and COVID-19 Research
Subfield: Infectious Diseases
Field: Medicine
Domain: Health Sciences

Open Access status: hybrid
Estimated APC paid: $4,650

Funders: Wellcome Trust, European Commission, King Abdulaziz University, U.S. Food and Drug Administration, Biotechnology and Biological Sciences Research Council
Awards: RapidFire Enhancement of Mass Spectrometry Capability Across the Biosciences, G3420693015, Defining the physiology and therapeutic potential of oxygenases as signalling enzymes., Evolution of Oxygen Sensing in Animals
OpenAlex ID: W4409252796
FWCI: 6.339
Cites: 125
Cited by: 9
Related to: 10
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