通过大规模复合物再利用发现SARS-CoV-2抗病毒药物
Laura Riva1, Shuofeng Yuan2,3,4, Xin Yin1
1Immunity and Pathogenesis Program, Infectious and Inflammatory Disease Center, Sanford Burnham Prebys Medical Discovery Institute, La Jolla, CA, USA.
Nature
|July 25, 2020
概括
药物重用提供了更快的COVID-19治疗途径. 研究人员选了12,000种药物,确定了100种抑制SARS-CoV-2复制的药物,其中13种药物在与患者相关的剂量中具有治疗潜力.
科学领域:
- 病毒学
- 药物发现
- 传染性疾病
背景情况:
- 由SARS-CoV-2引起的COVID-19大流行需要快速治疗.
- 传统的药物开发时间表对于正在进行的流行病来说太长了.
- 重新利用现有药物提供了一种加速治疗可用性的策略.
研究的目的:
- 确定可以抑制SARS-CoV-2复制的现有药物.
- 通过药物重用,寻找COVID-19治疗的候选疗法.
主要方法:
- 对大约12,000个临床阶段或FDA批准的小分子进行查.
- 针对抑制SARS-CoV-2病毒复制的药物候选人的分析.
- 在相关细胞和组织模型中评估有效度和抗病毒功效.
主要成果:
- 确定了100种抑制SARS-CoV-2复制的分子.
- 发现了21种与剂量反应相关的药物.
- 发现了13种有效度适合患者治疗的药物,包括阿皮利莫德和囊蛋白酶抑制剂.
结论:
- 药物重用是加速COVID-19治疗发展的可行策略.
- 包括阿皮利莫德在内的几种已识别的药物显示出治疗COVID-19的前景.
- 这些重定向药物的已知安全性概况有助于快速临床评估.
相关概念视频
Drug Discovery: Overview
10.7K
Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...
10.7K
Structure-Activity Relationships and Drug Design
1.5K
Drug design is a dynamic field that involves discovering and developing new medications based on specific biological targets. This process heavily relies on structure-activity relationships (SAR) and quantitative structure-activity relationships (QSAR) to guide the design and optimization of efficient drugs.
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence...
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence...
1.5K


