中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
Chemical Diversity in the G Protein-Coupled Receptor Superfamily

文献类型:期刊论文

作者Vass, Marton1; Kooistra, Albert J.1; Yang, Dehua2,8; Stevens, Raymond C.3,4,5; Wang, Ming-Wei2,4,6,7,8; de Graaf, Chris1
刊名TRENDS IN PHARMACOLOGICAL SCIENCES
出版日期2018-05
卷号39期号:5页码:494-512
ISSN号0165-6147
DOI10.1016/j.tips.2018.02.004
文献子类Review
英文摘要G protein-coupled receptors (GPCRs) are the largest family of cell signaling transmembrane proteins that can be modulated by a plethora of chemical compounds. Systematic cheminformatics analysis of structurally and pharma-cologically characterized GPCR ligands shows that cocrystallized GPCR ligands cover a significant part of chemical ligand space, despite their limited number. Many GPCR ligands and substructures interact with multiple receptors, providing a basis for polypharmacological ligand design. Experimentally determined GPCR structures represent a variety of binding sites and receptorligand interactions that can be translated to chemically similar ligands for which structural data are lacking. This integration of structural, pharmacological, and chemical information on GPCR-ligand interactions enables the extension of the structural GPCR-ligand interactome and the structure-based design of novel modulators of GPCR function.
WOS关键词MUSCARINIC ACETYLCHOLINE-RECEPTOR ; ADENOSINE A(2A) RECEPTOR ; DELTA-OPIOID RECEPTOR ; GPCR DRUG DISCOVERY ; SERIAL FEMTOSECOND CRYSTALLOGRAPHY ; HUMAN P2Y(12) RECEPTOR ; CRYSTAL-STRUCTURE ; STRUCTURAL BASIS ; ALLOSTERIC MODULATORS ; BETA(1)-ADRENERGIC RECEPTOR
资助项目National Natural Science Foundation of China[81573479] ; Chinese Academy of Sciences[XDA12020347] ; Chinese Academy of Sciences[XDA12040308] ; 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] ; Novo Nordisk-Chinese Academy of Sciences Research Fund[00000000] ; Shanghai Science and Technology Development Fund[15DZ2291600] ; Shanghai local government[00000000] ; GPCR Consortium[00000000] ; Netherlands eScience Center (NLeSC)/NWO Enabling Technologies project: 3D-e-Chem[027.014.201]
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000430562900006
出版者ELSEVIER SCIENCE LONDON
源URL[http://119.78.100.183/handle/2S10ELR8/279782]  
专题国家新药筛选中心
通讯作者Stevens, Raymond C.; Wang, Ming-Wei; de Graaf, Chris
作者单位1.Vrije Univ Amsterdam, Div Med Chem, Fac Sci, AIMMS, Boelelaan 1108, NL-1081 HZ Amsterdam, Netherlands;
2.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, 189 Guo Shou Jing Rd, Shanghai 201203, Peoples R China;
3.ShanghaiTech Univ, iHuman Inst, 393 Hua Xia Zhong Rd, Shanghai 201210, Peoples R China;
4.ShanghaiTech Univ, Sch Life Sci Technol, 393 Hua Xia Zhong Rd, Shanghai 201210, Peoples R China;
5.Univ Southern Calif, Bridge Inst, Dept Biol & Chem, Los Angeles, CA 90089 USA;
6.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China;
7.Fudan Univ, Sch Pharm, 826 Zhangheng Rd, Shanghai 201203, Peoples R China
8.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, 189 Guo Shou Jing Rd, Shanghai 201203, Peoples R China;
推荐引用方式
GB/T 7714
Vass, Marton,Kooistra, Albert J.,Yang, Dehua,et al. Chemical Diversity in the G Protein-Coupled Receptor Superfamily[J]. TRENDS IN PHARMACOLOGICAL SCIENCES,2018,39(5):494-512.
APA Vass, Marton,Kooistra, Albert J.,Yang, Dehua,Stevens, Raymond C.,Wang, Ming-Wei,&de Graaf, Chris.(2018).Chemical Diversity in the G Protein-Coupled Receptor Superfamily.TRENDS IN PHARMACOLOGICAL SCIENCES,39(5),494-512.
MLA Vass, Marton,et al."Chemical Diversity in the G Protein-Coupled Receptor Superfamily".TRENDS IN PHARMACOLOGICAL SCIENCES 39.5(2018):494-512.

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来源:上海药物研究所

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