以SARS-CoV-2膜融合过程6-HB核心为靶标的多肽类融合抑制剂的研究进展  

RESEARCH PROGRESS ON PEPTIDE-BASED FUSION INHIBITORS TARGETING THE 6-HB CORE OF SARS-CoV-2 MEMBRANE FUSION PROCESS

作　　者：罗慧 嘎鲁 马宇衡 梁国栋 LUO Hui;GA Lu;MA Yuheng;LIANG Guodong(Key Laboratory for Candidate Drug Design and Screening Based on Chemical Biology,College of Pharmacy,Inner Mongolia Medical University,Hohhot 010059,China)

机构地区：[1]内蒙古医科大学药学院,基于化学生物学的候选药物设计与筛选重点实验室,内蒙古呼和浩特010059

出　　处：《内蒙古医科大学学报》2024年第3期316-322,共7页Journal of Inner Mongolia Medical University

基　　金：内蒙古自治区自然科学基金项目(2023LHMS08045);内蒙古医科大学青年项目(YKD2023QN053);内蒙古医科大学学科建设项目(YKD2024XK006);内蒙古自治区本级事业单位引进高层次人才科研支持项目(DC2300001713)。

摘　　要：由新型冠状病毒(SARS-CoV-2)引起的新型冠状病毒肺炎对人类健康产生了深远的影响,不断出现的SARS-CoV-2变异株持续威胁全球公共卫生安全。因此,抗SARS-CoV-2药物的研发需求十分迫切。SARSCoV-2包膜在与宿主细胞膜融合过程中会形成六股螺旋束(6-HB),以6-HB或组成6-HB的HR1/HR2区域为靶标能够成功设计一系列多肽类融合抑制剂。本文综述了SARS-CoV-2的6-HB构效关系及多肽类融合抑制剂的设计思路和改造方法,以期为开发抗SARS-CoV-2药物提供新的研究思路。Corona virus disease 2019(COVID-19)caused by severe acute respiratory syndrome coronavirus 2(SARSCoV-2)has profoundly affected human health.Meanwhile,the continuously arising of SARS-CoV-2 has been posting a continuing threat to public health safety globally.Therefore,it is urgent to develop anti-SARS-CoV-2 agents.SARS-CoV-2 envelope forms a six-helix bundle(6-HB)structure during the membrane fusion process with the host cell.A series of peptidebased fusion inhibitors have been successfully obtained by targeting the 6-HB or the HR1/HR2 regions composing 6-HB.This paper reviewed the structure-activity relationship of the SARS-CoV-26-HB and the design ideas and retrofitting methods of peptide-based fusion inhibitors.We hope that this review will provide new research insights for the development of anti-SARS-CoV-2 agents.

关 键 词：新型冠状病毒 六股螺旋束 多肽 融合抑制剂 

分 类 号：R34[医药卫生—基础医学]