摘要
严重急性呼吸综合征冠状病毒2(severe acute respiratory syndrome coronavirus 2,SARS-CoV-2)引起的新型冠状病毒感染(corona virus disease 2019,COVID-19)对全球公共卫生和经济造成了前所未有的影响。SARSCoV-2通过其表面的刺突蛋白与宿主细胞膜上的血管紧张素转换酶2相结合是入侵宿主细胞的关键步骤,以刺突蛋白为靶标的小分子药物成为抗SARS-CoV-2研究的热点。活性筛选是小分子药物研发的关键步骤。鉴于此,本文综述了SARS-CoV-2刺突蛋白小分子抑制剂的活性筛选方法,以期为靶向刺突蛋白的抗病毒药物研发提供参考。
The pandemic of severe acute respiratory syndrome coronavirus 2(SARS-CoV-2)has caused a serious impact on global public health and the economy.SARS-CoV-2 infiltrates host cells via its surface spike protein,which binds to angiotensin-converting enzyme 2 on the host cell membrane.As a result,small molecules targeting spike protein have emerged as a hotspot in anti-SARS-CoV-2 drug research.Activity screening is an important step in seeking small molecule drugs.Therefore,this article aims to review the biological activity evaluation methods of small molecule inhibitors targeting SARS-CoV-2 spike protein,with the goal of laying the foundation for the discovery of new anti-SARS-CoV-2 drugs.
作者
胡立德
刘传峰
李萍
董冠宇
刘新泳
展鹏
HU Li-de;LIU Chuan-feng;LI Ping;DONG Guan-yu;LIU Xin-yong;ZHAN Peng(Department of Medicinal Chemistry,Key Laboratory of Chemical Biology(Ministry of Education),School of Pharmaceutical Sciences,Shandong University,Jinan 250012,China)
出处
《药学学报》
CAS
CSCD
北大核心
2024年第2期298-312,共15页
Acta Pharmaceutica Sinica
基金
山东省杰出青年基金(ZR2020JQ31)
中国博士后科学基金(2022M711938)。