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Chemical Diversity in the G Protein-Coupled Receptor Superfamily
2018-05
发表期刊TRENDS IN PHARMACOLOGICAL SCIENCES (IF:13.9[JCR-2023],14.3[5-Year])
ISSN0165-6147
卷号39期号:5页码:494-512
发表状态已发表
DOI10.1016/j.tips.2018.02.004
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.
收录类别SCI ; SCIE
语种英语
资助项目Netherlands eScience Center (NLeSC)/NWO Enabling Technologies project: 3D-e-Chem[027.014.201]
WOS研究方向Pharmacology & Pharmacy
WOS类目Pharmacology & Pharmacy
WOS记录号WOS:000430562900006
出版者ELSEVIER SCIENCE LONDON
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
原始文献类型Review
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文献类型期刊论文
条目标识符https://kms.shanghaitech.edu.cn/handle/2MSLDSTB/20827
专题iHuman研究所
iHuman研究所_特聘教授组_Raymond Stevens组
生命科学与技术学院_特聘教授组_王明伟组
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, Natl Ctr Drug Screening, 189 Guo Shou Jing Rd, Shanghai 201203, Peoples R China
3.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, 189 Guo Shou Jing Rd, Shanghai 201203, Peoples R China
4.ShanghaiTech Univ, iHuman Inst, 393 Hua Xia Zhong Rd, Shanghai 201210, Peoples R China
5.ShanghaiTech Univ, Sch Life Sci Technol, 393 Hua Xia Zhong Rd, Shanghai 201210, Peoples R China
6.Univ Southern Calif, Bridge Inst, Dept Biol & Chem, Los Angeles, CA 90089 USA
7.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China
8.Fudan Univ, Sch Pharm, 826 Zhangheng Rd, Shanghai 201203, Peoples R China
通讯作者单位iHuman研究所;  生命科学与技术学院
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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