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伊维菌素与纤维蛋白原相互作用的计算预测。

Computational Prediction of the Interaction of Ivermectin with Fibrinogen.

机构信息

Department of Biomedical Engineering, University of Alberta, Edmonton, AB T6G 1Z2, Canada.

Department of Mechanical Engineering, University of Alberta, Edmonton, AB T6G 1H9, Canada.

出版信息

Int J Mol Sci. 2023 Jul 14;24(14):11449. doi: 10.3390/ijms241411449.

Abstract

Hypercoagulability and formation of extensive and difficult-to-lyse microclots are a hallmark of both acute COVID-19 and long COVID. Fibrinogen, when converted to fibrin, is responsible for clot formation, but abnormal structural and mechanical clot properties can lead to pathologic thrombosis. Recent experimental evidence suggests that the spike protein (SP) from severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) may directly bind to the blood coagulation factor fibrinogen and induce structurally abnormal blood clots with heightened proinflammatory activity. Accordingly, in this study, we used molecular docking and molecular dynamics simulations to explore the potential activity of the antiparasitic drug ivermectin (IVM) to prevent the binding of the SARS-CoV-2 SP to fibrinogen and reduce the occurrence of microclots. Our computational results indicate that IVM may bind with high affinity to multiple sites on the fibrinogen peptide, with binding more likely in the central, E region, and in the coiled-coil region, as opposed to the globular D region. Taken together, our in silico results suggest that IVM may interfere with SP-fibrinogen binding and, potentially, decrease the formation of fibrin clots resistant to degradation. Additional in vitro studies are warranted to validate whether IVM binding to fibrinogen is sufficiently stable to prevent interaction with the SP, and potentially reduce its thrombo-inflammatory effect in vivo.

摘要

高凝状态和广泛且难以溶解的微血栓的形成是急性 COVID-19 和长 COVID 的共同特征。纤维蛋白原转化为纤维蛋白后负责血栓形成,但异常的结构和机械血栓特性可导致病理性血栓形成。最近的实验证据表明,严重急性呼吸综合征冠状病毒 2(SARS-CoV-2)的刺突蛋白(SP)可能直接与凝血因子纤维蛋白原结合,并诱导具有增强促炎活性的结构异常的血栓。因此,在这项研究中,我们使用分子对接和分子动力学模拟来探索驱虫药伊维菌素(IVM)预防 SARS-CoV-2 SP 与纤维蛋白原结合并减少微血栓形成的潜在活性。我们的计算结果表明,IVM 可能与纤维蛋白原肽上的多个位点以高亲和力结合,结合更可能发生在中央 E 区和卷曲螺旋区,而不是球状 D 区。综上所述,我们的计算机模拟结果表明,IVM 可能干扰 SP-纤维蛋白原结合,并可能减少对降解有抗性的纤维蛋白凝块的形成。需要进一步的体外研究来验证 IVM 与纤维蛋白原的结合是否足够稳定,以防止与 SP 相互作用,并可能降低其体内的血栓炎症作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e87/10380762/511c69680d3f/ijms-24-11449-g0A1.jpg

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