中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
首页 机构 成果 学者
  
  1. CAS IR Grid
  2. 上海药物研究所
  3. 中国科学院上海药物研究所
  4. 新药研究国家重点实验室
Triazine-Based Covalent DNA-Encoded Libraries for Discovery of Covalent Inhibitors of Target Proteins

文献类型：期刊论文

作者Li, Linjie6; Su, Mingbo5,6; Lu, Weiwei6; Song, Hongzhi4; Liu, Jiaxiang6; Wen, Xin3,6; Suo, Yanrui3,6; Qi, Jingjing5,6; Luo, Xiaomin5,6; Zhou, Yu-Bo2,3,5,6
刊名ACS MEDICINAL CHEMISTRY LETTERS
出版日期2022-08-15
页码8
ISSN号1948-5875
关键词DNA encoded library covalent library library design covalent inhibitors
DOI10.1021/acsmedchemlett.2c00127
通讯作者Liao, Xin-Hua(xinhualiao@foxmail.com) ; Li, Jia(jli@simm.ac.cn) ; Lu, Xiaojie(xjlu@simm.ac.cn)
英文摘要Since ibrutinib was approved by the FDA as an effective monotherapy for chronic lymphocytic leukemia (CLL) and multilymphoma, more and more FDA-approved covalent drugs are coming back into the market. On this occasion, the resurgence of interest in covalent drugs calls for more hit discovery techniques. However, the limited numbers of covalent libraries prevent the development of this area. Herein, we report the design of covalent DNA-encoded library (DEL) and its selection method for the discovery of covalent inhibitors for target proteins. These triazine-based covalent DELs yielded potent compounds after covalent selection against target proteins, including Bruton's Tyrosine Kinase (BTK), Janus kinase 3 (JAK3), and peptidyl-prolyl cis/ trans isomerase NIMA-interacting-1 (Pin1).
WOS关键词BRUTONS TYROSINE KINASE ; DRUG DISCOVERY
资助项目Science and Technology Commission of Shanghai Municipality[NSFC-81821005] ; Shanghai Municipal Science and Technology Major Project[18431907100] ; Shanghai Municipal Science and Technology Major Project[19430750100] ; Shanghai Municipal Science and Technology Major Project[NSFC-91953203] ; Shanghai Municipal Science and Technology Major Project[NSFC-21877117] ; Shanghai Municipal Science and Technology Major Project[NSFC-81972563]
WOS研究方向Pharmacology & Pharmacy
语种英语
出版者AMER CHEMICAL SOC
WOS记录号WOS:000841608100001
源URL[http://119.78.100.183/handle/2S10ELR8/302329]  
专题新药研究国家重点实验室
通讯作者Liao, Xin-Hua; Li, Jia; Lu, Xiaojie
作者单位1.Shanghai Univ, Sch Life Sci, Shanghai 200444, Peoples R China
2.Chinese Acad Sci, Zhongshan Inst Drug Discovery, Shanghai Inst Mat Med, R China, Guangdong 528400, Peoples R China
3.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
4.Shanghai Univ, Sch Med, R China, Shanghai 200444, Peoples R China
5.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210023, Peoples R China
6.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Li, Linjie,Su, Mingbo,Lu, Weiwei,et al. Triazine-Based Covalent DNA-Encoded Libraries for Discovery of Covalent Inhibitors of Target Proteins[J]. ACS MEDICINAL CHEMISTRY LETTERS,2022:8.
APA Li, Linjie.,Su, Mingbo.,Lu, Weiwei.,Song, Hongzhi.,Liu, Jiaxiang.,...&Lu, Xiaojie.(2022).Triazine-Based Covalent DNA-Encoded Libraries for Discovery of Covalent Inhibitors of Target Proteins.ACS MEDICINAL CHEMISTRY LETTERS,8.
MLA Li, Linjie,et al."Triazine-Based Covalent DNA-Encoded Libraries for Discovery of Covalent Inhibitors of Target Proteins".ACS MEDICINAL CHEMISTRY LETTERS (2022):8.

入库方式： OAI收割

来源：上海药物研究所

浏览0
下载0
收藏0
其他版本

除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。