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2022-03-07
摘要翻译:
新冠肺炎的流行病威胁有超过3700万例病例,其中约5%进入以细胞因子风暴和过度炎症为特征的关键阶段,该州更经常导致进入重症监护室,死亡率很快。Jak-1、Jak-2、Jak-3和Tyk2的Janus激酶似乎是药物抑制细胞因子风暴的良好靶点。本文从不同的角度研究了不同镇痛药物对这些靶点的抑制作用,以评价它们的临床应用能力。我们的对接结果表明,萘普生、美沙酮和阿米替林考虑到其较高的结合能、较低的能量方差和较高的疏水性,对Janus激酶的抑制作用似乎比已批准的抑制剂巴里西替尼和鲁索利替尼更强。因此,我们建议我们广泛的候选药物清单,包括消炎痛、依托度酸、丁丙诺啡、罗非昔布、度洛西汀、伐地考昔、萘普生、美沙酮和阿米替林,以用于临床评估它们在新冠肺炎治疗中的有效性,特别是考虑到迄今为止尚未批准治疗该病的方法。
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英文标题:
《Old Drugs for JAK-STAT Pathway Inhibition in COVID-19》
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作者:
Mohammad Reza Dayer
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最新提交年份:
2020
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分类信息:

一级分类:Quantitative Biology        数量生物学
二级分类:Other Quantitative Biology        其他定量生物学
分类描述:Work in quantitative biology that does not fit into the other q-bio classifications
不适合其他q-bio分类的定量生物学工作
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英文摘要:
  The pandemic threat of COVID-19 with more than 37 million cases in which about 5 percent entering critical stage characterized by cytokine storm and hyperinflammatory condition, the state more often leads to admission to intensive care unit with rapid mortality. Janus kinase enzymes of Jak-1, Jak-2, Jak-3, and Tyk2 seem to be good targets for inhibition by medications to control cytokine storm in this context. In the present work, the inhibitory properties of different analgesic drugs on these targets are studied to assess their ability for clinical application from different points of view. Our docking results indicated that naproxen, methadone, and amitriptyline considering their higher binding energy, lower energy variance, and higher hydrophobicity, seem to express more inhibitory effects on Janus kinase enzymes than thats for approved inhibitors i.e. baricitinib and ruxolitinib. Accordingly, we suggest our wide list of candidate drugs including indomethacin, etodolac, buprenorphine, rofecoxib, duloxetine, valdecoxib, naproxen, methadone, and amitriptilin for clinical assessments for their usefulness in COVID-19 treatment, especially taking into account that up to now, there is no approved cure for this disease.
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PDF链接:
https://arxiv.org/pdf/2010.12332
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