Evaluation of Xa inhibitors as potential inhibitors of the SARS-CoV-2 Mpro protease.
oleh: Katarzyna Papaj, Patrycja Spychalska, Patryk Kapica, André Fischer, Jakub Nowak, Maria Bzówka, Manuel Sellner, Markus A Lill, Martin Smieško, Artur Góra
| Format: | Article |
|---|---|
| Diterbitkan: | Public Library of Science (PLoS) 2022-01-01 |
Deskripsi
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.