G Protein-Coupled Receptor Deorphanizations

被引：141

作者：

Civelli, Olivier ^{[1
,2
,3
]}

Reinscheid, Rainer K. ^{[1
,2
]}

Zhang, Yan ^{[1
]}

Wang, Zhiwei ^{[1
]}

Fredriksson, Robert ^{[4
]}

Schioth, Helgi B. ^{[4
]}

机构：

[1] Univ Calif Irvine, Dept Pharmacol, Irvine, CA 92617 USA

[2] Univ Calif Irvine, Dept Pharmaceut Sci, Irvine, CA 92617 USA

[3] Univ Calif Irvine, Dept Dev & Cell Biol, Irvine, CA 92617 USA

[4] Uppsala Univ, Dept Neurosci, SE-75124 Uppsala, Sweden

来源：

ANNUAL REVIEW OF PHARMACOLOGY AND TOXICOLOGY, VOL 53, 2013 | 2013年 / 53卷

关键词：

orphan receptors; neuropeptides; reverse pharmacology; phylogeny; lipid mediators; BETA-ADRENERGIC-RECEPTOR; OPIOID RECEPTOR; ENDOGENOUS LIGAND; OREXIN RECEPTORS; ORPHAN RECEPTOR; PHYLOGENETIC ANALYSIS; NATURAL LIGANDS; GENE-EXPRESSION; NEUROPEPTIDE-S; HEAD ACTIVATOR;

D O I：

10.1146/annurev-pharmtox-010611-134548

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

G protein-coupled receptors (GPCRs) are major regulators of intercellular interactions. They initiate these actions by being activated by a wide variety of natural ligands. Historically, ligands were discovered first, but the advent of molecular biology reversed this trend. Most GPCRs are identified on the basis of their DNA sequences and thus are initially unmatched to known natural ligands. They are termed orphan GPCRs. Discovering their ligands-i.e., "deorphanizing" the GPCRs-gave birth to the field of reverse pharmacology. This review discusses the present status of GPCR deorphanization, presents a few examples of successes and surprises, and highlights difficulties encountered in these efforts.

引用

页码：127 / 146

页数：20

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