Evaluation of Xa inhibitors as potential inhibitors of the SARS-CoV-2 Mpro protease.
basic_science · Level V
Where this comes from
- Record sourced from PubMed, PMID 35015795.
- Also identified by DOI 10.1371/journal.pone.0262482 and PMC identifier 8752003.
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Abstract
Based on previous large-scale in silico screening several factor Xa inhibitors were proposed to potentially inhibit SARS-CoV-2 Mpro. In addition to their known anticoagulants activity this potential inhibition could have an additional therapeutic effect on patients with COVID-19 disease. In this study we examined the binding of the Apixaban, Betrixaban and Rivaroxaban to the SARS-CoV-2 Mpro with the use of the MicroScale Thermophoresis technique. Our results indicate that the experimentally measured binding affinity is weak and the therapeutic effect due to the SARS-CoV-2 Mpro inhibition is rather negligible.
Medical subject headings
- Coronavirus M Proteins
- Factor Xa Inhibitors
- SARS-CoV-2