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High-throughput identification of G protein-coupled receptor modulators through affinity mass spectrometry screening

文献类型：期刊论文

作者Qin, Shanshan2; Meng, Mengmeng3; Yang, Dehua4; Bai, Wenwen3; Lu, Yan2,5; Peng, Yao2; Song, Gaojie2; Wu, Yiran2; Zhou, Qingtong2; Zhao, Suwen2,5
刊名CHEMICAL SCIENCE
出版日期2018-03-28
卷号9期号:12页码:3192-3199
ISSN号2041-6520
DOI10.1039/c7sc04698g
文献子类Article
英文摘要G protein-coupled receptors (GPCRs) represent the largest class of cell surface proteins and thus constitute an important family of therapeutic targets. Therefore, significant effort has been put towards the identification of novel ligands that can modulate the activity of a GPCR target with high efficacy and selectivity. However, due to limitations inherent to the most common techniques for GPCR ligand discovery, there is a pressing need for more efficient and effective ligand screening methods especially for the identification of potential allosteric modulators. Here we present a high-throughput, label-free and unbiased screening approach for the identification of small molecule ligands towards GPCR targets based on affinity mass spectrometry. This new approach features the usage of target-expressing cell membranes rather than purified proteins for ligand screening and allows the detection of both orthosteric and allosteric ligands targeting specific GPCRs. Screening a small compound library with this approach led to the rapid discovery of an antagonist for the 5-HT receptor and four positive allosteric modulators for GLP-1 receptor that were not previously reported.
WOS关键词GLUCAGON-LIKE PEPTIDE-1 ; DRUG DISCOVERY ; LIGANDS ; BINDING ; GPCR ; INHIBITORS ; STABILITY ; DESIGN ; KINASE ; ASSAYS
资助项目"Hundred Talents Program" of the Chinese Academy of Sciences[00000000] ; ShanghaiTech University[00000000] ; National Natural Science Foundation of China[81373463] ; National Natural Science Foundation of China[81573479] ; National Health and Family Planning Commission[2012ZX09304-011] ; National Health and Family Planning Commission[2013ZX09401003-005] ; National Health and Family Planning Commission[2013ZX09507001] ; National Health and Family Planning Commission[2013ZX09507-002] ; Shanghai Science and Technology Development Fund[15DZ2291600] ; Natural Science Foundation of Shanghai[16ZR1448500] ; National Key Research and Development Program of China[2016YCF0905902]
WOS研究方向Chemistry
语种英语
WOS记录号WOS:000428987200013
出版者ROYAL SOC CHEMISTRY
源URL[http://119.78.100.183/handle/2S10ELR8/279838]  
专题国家新药筛选中心
通讯作者Wang, Ming-Wei; Shui, Wenqing
作者单位1.GPCR Consortium, San Marcos, CA 92078 USA;
2.ShanghaiTech Univ, iHuman Inst, Shanghai 201210, Peoples R China;
3.Nankai Univ, Coll Pharm, Tianjin 300071, Peoples R China;
4.Chinese Acad Sci, Natl Ctr Drug Screening, CAS Key Lab Receptor Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China;
5.ShanghaiTech Univ, Sch Life Sci & Technol, Shanghai 201202, Peoples R China;
6.Univ N Carolina, Chapel Hill Sch Med, Dept Pharmacol, Chapel Hill, NC 27599 USA;
7.Fudan Univ, Sch Pharm, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Qin, Shanshan,Meng, Mengmeng,Yang, Dehua,et al. High-throughput identification of G protein-coupled receptor modulators through affinity mass spectrometry screening[J]. CHEMICAL SCIENCE,2018,9(12):3192-3199.
APA Qin, Shanshan.,Meng, Mengmeng.,Yang, Dehua.,Bai, Wenwen.,Lu, Yan.,...&Shui, Wenqing.(2018).High-throughput identification of G protein-coupled receptor modulators through affinity mass spectrometry screening.CHEMICAL SCIENCE,9(12),3192-3199.
MLA Qin, Shanshan,et al."High-throughput identification of G protein-coupled receptor modulators through affinity mass spectrometry screening".CHEMICAL SCIENCE 9.12(2018):3192-3199.

入库方式： OAI收割

来源：上海药物研究所

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