Evaluation of Xa inhibitors as potential inhibitors of the SARS-CoV-2 Mpro protease | Zendy

Katarzyna Papaj | Zendy; Patrycja Spychalska | Zendy; Patryk Kapica | Zendy; André Fischer | Zendy; Jakub Nowak | Zendy; Maria Bzówka | Zendy; Manuel Sellner | Zendy; Markus A. Lill | Zendy; Martin Smieško | Zendy; Artur Góra | Zendy

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Evaluation of Xa inhibitors as potential inhibitors of the SARS-CoV-2 Mpro protease

Author(s) -

Katarzyna Papaj,

Patrycja Spychalska,

Patryk Kapica,

André Fischer,

Jakub Nowak,

Maria Bzówka,

Manuel Sellner,

Markus A. Lill,

Martin Smieško,

Artur Góra

Publication year - 2022

Publication title -

plos one

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.99

H-Index - 332

ISSN - 1932-6203

DOI - 10.1371/journal.pone.0262482

Subject(s) - microscale thermophoresis , apixaban , protease , in silico , rivaroxaban , covid-19 , chemistry , proteases , pharmacology , computational biology , enzyme , biochemistry , biology , medicine , disease , infectious disease (medical specialty) , pathology , warfarin , cardiology , gene , atrial fibrillation

Based on previous large-scale in silico screening several factor Xa inhibitors were proposed to potentially inhibit SARS-CoV-2 M pro . 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 M pro 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 M pro inhibition is rather negligible.

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