SARS-CoV和SARS-CoV-2主要蛋白酶及其抑制的结构和功能:综合性综述
1Department of Pharmacology and Chemical Biology, Baylor College of Medicine, 1 Baylor Plaza, Houston, TX, 77030, USA; Dan L. Duncan Comprehensive Cancer Center, Baylor College of Medicine, 1 Baylor Plaza, Houston, TX, 77030, USA.
European journal of medicinal chemistry
|September 2, 2023
概括
主蛋白酶 (Mpro) 对SARS-CoV和SARS-CoV-2复制至关重要. 这篇评论详细介绍了Mpro的细节.
科学领域:
- 病毒学 病毒学
- 生物化学 生物化学
- 药物发现 药物发现 药物发现
背景情况:
- 严重急性呼吸系统综合征相关的冠状病毒 (SARS-CoV) 和SARS-CoV-2导致全球重大健康危机.
- 尽管有现有的治疗方法,但新冠病毒的出现和病毒的进化需要新的治疗策略.
- 主蛋白酶 (Mpro) 是冠状病毒复制的关键酶,也是有前途的药物标.
研究的目的:
- 提供SARS-CoV和SARS-CoV-2主要蛋白酶 (Mpro) 的功能,结构和抑制的全面审查.
- 探索Mpro向治疗的结构-活性关系和蛋白质-抑制剂相互作用.
- 总结一下Mpro抑制剂的临床试验状态.
主要方法:
- 关于SARS-CoV和SARS-CoV-2的科学出版物的文献综述 Mpro.
- 分析与Mpro功能和抑制相关的结构数据和生物化学研究.
- 汇编有关Mpro抑制剂的数据,包括结构-活性关系和临床试验结果.
主要成果:
- 详细描述Mpro在SARS-CoV和SARS-CoV-2病毒生命周期中的重要作用.
- 多种Mpro抑制剂的概述,重点介绍关键相互作用和结构-活性关系.
- 目前Mpro抑制剂在临床前和临床开发中的情况概述.
结论:
- Mpro酶是针对SARS-CoV和SARS-CoV-2的抗病毒药物开发的高度保存和验证的目标.
- 了解Mpro的结构和抑制机制对于设计有效的治疗方法至关重要.
- 对Mpro抑制剂的持续研究对于对抗当前和未来的冠状病毒威胁至关重要.
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