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Design, Construction, and Screening of Diversified Pyrimidine-Focused DNA-Encoded Libraries

文献类型：期刊论文

作者Seydimemet, Mengnisa1,2; Yang, Yixuan2; Lv, Yuhan3; Liu, Jiaxiang4; Yan, Ziqin2; Zhao, Yujun2,5; Wang, Xuan2; Lu, Xiaojie1,2,5
刊名ACS MEDICINAL CHEMISTRY LETTERS
出版日期2023-07-27
卷号14期号:8页码:1073-1078
关键词DNA-encoded library technology Pyrimidine-focusedDNA-encodedlibrary BRD4 Affinity screening Inhibitor
ISSN号1948-5875
DOI10.1021/acsmedchemlett.3c00205
通讯作者Zhao, Yujun(yjzhao@simm.ac.cn) ; Wang, Xuan(wangxuan2@simm.ac.cn) ; Lu, Xiaojie(xjlu@simm.ac.cn)
英文摘要Pyrimidineis a ubiquitous component in natural products and approveddrugs, providing an ideal modular scaffold for generating librarieswith drug-like properties. DNA-encoded library technology introducesa novel library modality where each small molecule is covalently linkedto a unique oligo tag. This technology offers the advantages of rapidlygenerating and interrogating large-scale libraries containing billionsof members, substantially reducing the entry barrier to their usein both academia and the pharmaceutical industry. In this Letter,we describe the synthesis of three DNA-encoded libraries based ondifferent functionalized pyrimidine cores featuring diversified chemoselectivityand regioselectivity. Preliminary screening of these DNA-encoded librariesagainst BRD4 identified compounds with nanomolar inhibition activities.
WOS关键词SOLID-PHASE SYNTHESIS ; TECHNOLOGY ; DISCOVERY ; SELECTION ; POTENT
资助项目NSFC[91953203] ; NSFC[92253305] ; Lingang Laboratory[LG-QS-202206-09] ; National Key Research and Development Program of China[2022YFC2804400] ; National Natural Science Foundation of China[82073682] ; National Natural Science Foundation of China[82273759]
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:001037606900001
出版者AMER CHEMICAL SOC
源URL[http://119.78.100.183/handle/2S10ELR8/306815]  
专题新药研究国家重点实验室
通讯作者Zhao, Yujun; Wang, Xuan; Lu, Xiaojie
作者单位1.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210023, Peoples R China
2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China
3.Weifang Med Univ, Sch Pharm, Weifang 261053, Shandong, Peoples R China
4.Alphama Biotechnol Suzhou Co Ltd, Suzhou 215123, Jiangsu, Peoples R China
5.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
推荐引用方式
GB/T 7714		 Seydimemet, Mengnisa,Yang, Yixuan,Lv, Yuhan,et al. Design, Construction, and Screening of Diversified Pyrimidine-Focused DNA-Encoded Libraries[J]. ACS MEDICINAL CHEMISTRY LETTERS,2023,14(8):1073-1078.
APA Seydimemet, Mengnisa.,Yang, Yixuan.,Lv, Yuhan.,Liu, Jiaxiang.,Yan, Ziqin.,...&Lu, Xiaojie.(2023).Design, Construction, and Screening of Diversified Pyrimidine-Focused DNA-Encoded Libraries.ACS MEDICINAL CHEMISTRY LETTERS,14(8),1073-1078.
MLA Seydimemet, Mengnisa,et al."Design, Construction, and Screening of Diversified Pyrimidine-Focused DNA-Encoded Libraries".ACS MEDICINAL CHEMISTRY LETTERS 14.8(2023):1073-1078.

入库方式： OAI收割

来源：上海药物研究所

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