准高峰:重新利用米氏素和二甲胺来阻止SARS-CoV-2感染
Soledad Stagnoli1, Gabriele Macari2, Pietro Corsi2
1Structure and Cell Biology of Viruses Lab, Center for Cooperative Research in Biosciences (CIC bioGUNE), Basque Research and Technology Alliance (BRTA), 48160 Derio, Spain.
ACS omega
|November 29, 2023
概括
研究人员发现,FDA批准的药物密拉米和二甲胺可以通过阻塞尖端蛋白质来阻止SARS-CoV-2感染.
科学领域:
- 病毒学 病毒学
- 药物发现 药物发现 药物发现
- 结构生物学 结构生物学
背景情况:
- 目前的SARS-CoV-2疫苗面临着新兴变种带来的挑战.
- 需要补充疗法来对抗SARS-CoV-2 (严重急性呼吸系统综合征冠状病毒2).
研究的目的:
- 通过向尖端蛋白质的受体结合域 (RBD) 来识别抑制SARS-CoV-2进入的小化合物.
- 调查重新使用现有的FDA批准药物作为SARS-CoV-2治疗的潜力.
主要方法:
- 针对SARS-CoV-2尖端蛋白RBD.的小型化合物的化选.
- 基于细胞的测试,以评估已识别的化合物的抗病毒活性.
- 通过STD-NMR (和转移差核磁共振) 谱学来确认药物向相互作用.
主要成果:
- 两种FDA批准的药物,密拉米和二甲胺,被确定为潜在的抑制剂.
- 这些化合物在微分子度的基于细胞的测试中有效地阻止了SARS-CoV-2感染.
- STD-NMR实验提供了证据,证明二水素和尖蛋白之间的直接相互作用.
结论:
- 甲基素和二甲基胺显示有望作为抗病毒疗法对抗SARS-CoV-2的重新定位.
- 用小分子准RBD提供了一个潜在的策略来防止病毒进入.
- 需要对这些化合物进行进一步的临床研究以治疗SARS-CoV-2.
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