典型文献
Molecular glues modulate protein functions by inducing protein aggregation:A promising therapeutic strategy of small molecules for disease treatment
文献摘要:
Molecular glues can specifically induce aggregation between two or more proteins to modu-late biological functions.In recent years,molecular glues have been widely used as protein degraders.In addition,however,molecular glues play a variety of vital roles,such as complex stabilization,interactome modulation and transporter inhibition,enabling challenging therapeutic targets to be druggable and offer-ing an exciting novel approach for drug discovery.Since most molecular glues are identified serendipi-tously,exploration of their systematic discovery and rational design are important.In this review,representative examples of molecular glues with various physiological functions are divided into those mediating homo-dimerization,homo-polymerization and hetero-dimerization according to their aggrega-tion modes,and we attempt to elucidate their mechanisms of action.In particular,we aim to highlight some biochemical techniques typically exploited within these representative studies and classify them in terms of three stages of molecular glue development:starting point,optimization and identification.
文献关键词:
中图分类号:
作者姓名:
Hongyu Wu;Hong Yao;Chen He;Yilin Jia;Zheying Zhu;Shengtao Xu;Dahong Li;Jinyi Xu
作者机构:
State Key Laboratory of Natural Medicines,Department of Medicinal Chemistry,China Pharmaceutical University,Nanjing 210009,China;Division of Molecular Therapeutics&Formulation,School of Pharmacy,the University of Nottingham,University Park Campus,Nottingham NG7 2RD,UK;Key Laboratory of Structure-Based Drug Design&Discovery,Ministry of Education,School of Traditional Chinese Materia Medica,Shenyang Pharmaceutical University,Shenyang 110016,China
文献出处:
引用格式:
[1]Hongyu Wu;Hong Yao;Chen He;Yilin Jia;Zheying Zhu;Shengtao Xu;Dahong Li;Jinyi Xu-.Molecular glues modulate protein functions by inducing protein aggregation:A promising therapeutic strategy of small molecules for disease treatment)[J].药学学报(英文版),2022(09):3548-3566
A类:
glues,degraders,serendipi
B类:
Molecular,modulate,functions,by,inducing,aggregation,promising,therapeutic,strategy,small,molecules,disease,treatment,can,specifically,induce,between,two,more,proteins,biological,In,recent,years,molecular,have,been,widely,used,addition,however,play,variety,vital,roles,such,complex,stabilization,interactome,modulation,transporter,inhibition,enabling,challenging,targets,druggable,offer,exciting,novel,approach,discovery,Since,most,are,identified,tously,exploration,their,systematic,rational,design,important,this,review,representative,examples,various,physiological,divided,into,those,mediating,homo,dimerization,polymerization,hetero,according,modes,attempt,elucidate,mechanisms,action,particular,aim,highlight,some,biochemical,techniques,typically,exploited,within,these,studies,classify,them,terms,three,stages,development,starting,point,optimization,identification
AB值:
0.624318
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