典型文献
Harnessing the cyclization strategy for new drug discovery
文献摘要：
The design of new ligands with high affinity and specificity against the targets of interest has been a central focus in drug discovery.As one of the most commonly used methods in drug discovery,the cyclization represents a feasible strategy to identify new lead compounds by increasing structural novelty,scaffold diversity and complexity.Such strategy could also be potentially used for the follow-on drug dis-covery without patent infringement.In recent years,the cyclization strategy has witnessed great success in the discovery of new lead compounds against different targets for treating various diseases.Herein,we first briefly summarize the use of the cyclization strategy in the discovery of new small-molecule lead compounds,including the proteolysis targeting chimeras(PROTAC)molecules.Particularly,we focus on four main strategies including fused ring cyclization,chain cyclization,spirocyclization and macrocy-clization and highlight the use of the cyclization strategy in lead generation.Finally,the challenges including the synthetic intractability,relatively poor pharmacokinetics(PK)profiles and the absence of the structural information for rational structure-based cyclization are also briefly discussed.We hope this review,not exhaustive,could provide a timely overview on the cyclization strategy for the discovery of new lead compounds.
文献关键词：
中图分类号：
作者姓名：
Kai Tang;Shu Wang;Wenshuo Gao;Yihui Song;Bin Yu
作者机构：
School of Pharmaceutical Sciences,Zhengzhou University,Zhengzhou 450001,China
文献出处：
引用格式：
[1]Kai Tang;Shu Wang;Wenshuo Gao;Yihui Song;Bin Yu-.Harnessing the cyclization strategy for new drug discovery)[J].药学学报（英文版）,2022(12):4309-4326
A类：
spirocyclization,macrocy,clization,intractability
B类：
Harnessing,strategy,new,drug,discovery,design,ligands,affinity,specificity,against,targets,interest,has,been,central,focus,one,most,commonly,methods,represents,feasible,identify,lead,compounds,by,increasing,structural,novelty,scaffold,diversity,complexity,Such,could,also,potentially,follow,without,patent,infringement,In,recent,years,witnessed,great,success,different,treating,various,diseases,Herein,we,first,briefly,summarize,small,including,proteolysis,targeting,chimeras,PROTAC,molecules,Particularly,four,main,strategies,fused,chain,highlight,generation,Finally,challenges,synthetic,relatively,poor,pharmacokinetics,PK,profiles,absence,information,rational,structure,are,discussed,We,hope,this,review,not,exhaustive,provide,timely,overview
AB值：
0.512021
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