Evaluation of Xa inhibitors as potential inhibitors of the SARS-CoV-2 Mpro protease.
Evaluation of Xa inhibitors as potential inhibitors of the SARS-CoV-2 Mpro protease.
复制标题
DOI：
10.1371/journal.pone.0262482
复制
发表时间：
2022
期刊：
影响因子：
3.7
通讯作者：
Góra A
中科院分区：
文献类型：
--
作者：
Papaj K;Spychalska P;Kapica P;Fischer A;Nowak J;Bzówka M;Sellner M;Lill MA;Smieško M;Góra A
基于先前的大规模硅筛选，提出了几种因子Xa抑制剂可能抑制SARS-CoV-2 Mpro。除了已知的抗凝血活性外，这种潜在的抑制作用可能对COVID-19患者具有额外的治疗作用。在这项研究中，我们使用微尺度热电泳技术检测了阿哌沙班、倍特里沙班和利伐沙班与SARS-CoV-2 Mpro的结合。我们的结果表明，实验测量的结合亲和力较弱，由于抑制SARS-CoV-2 Mpro的治疗效果可以忽略不计。
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.
影响因子：
5.6
作者：
Fischer A;Sellner M;Mitusińska K;Bzówka M;Lill MA;Góra A;Smieško M
通讯作者：
Smieško M