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通过DNA编码图书馆查,快速发现针对SARS-CoV-2高峰HR1的重用药物

Qingao Xue¹, Ze Liang², Yi Zhang²

¹Shanghai Institute for Advanced Immunochemical Studies, ShanghaiTech University, Shanghai 200120, China.; State Key Laboratory of Microbial Technology, School of Food Science and Pharmaceutical Engineering, Nanjing Normal University, Nanjing 210023, China.

Bioorganic chemistry

|February 15, 2026

概括

研究人员确定了小分子,包括Rabeprazole,可以抑制SARS-CoV-2尖端蛋白介导的膜融合. 这些化合物显示出作为针对冠状病毒融合的广谱抗病毒剂的潜力.

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:

SARS-CoV-2尖端蛋白的膜融合机制是抗病毒疗法的关键目标.
七度重复1 (HR1) 域的三元槽对于在病毒进入过程中形成六螺旋捆绑至关重要.

研究的目的:

为了识别与SARS-CoV-2 HR1域结合并抑制膜融合的小分子.
评估已识别的HR1向化合物的抗病毒潜力.

主要方法:

用DNA编码的图书馆选,以确定HR1结合的小分子.
生物物理测试 (例如,结合确认) 和用于相互作用分析的计算模拟.
细胞细胞融合试验和针对SARS-CoV-2变种和HCoV-OC43.3的抗病毒试验.

主要成果:

几种化合物,包括拉贝普拉相关化合物E (Rab RCE),奥梅普拉,阿尔维莫潘和奥尔梅沙坦,被确定为HR1结合剂.
奥尔梅沙坦和Rab RCE证明了细胞融合的强烈抑制.
拉贝普拉和Rab RCE对SARS-CoV-2变种和HCoV-OC43表现出部分抗病毒活性,减轻了病毒诱导的亡.
发现拉贝普拉能在HR1.1上竞争性地阻断HR2结合槽.

结论:

HR1向分子,以Rabeprazole为例,代表了开发广谱冠状病毒融合抑制剂的有希望的线索.
抑制HR1-HR2相互作用是对抗冠状病毒感染的可行策略.

关键词:

在 COVID-19 疫情中,DNA编码的图书馆 (DEL)HR1 域名 HR1 域名这就是SARS-CoV-2病毒.小分子分子小分子分子尖蛋白质是一种尖蛋白质.病毒进入抑制剂病毒进入抑制剂

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