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Gina L C Yosten, Grant R Kolar, Lauren J Redlinger and Willis K Samson

that the CpepR is a GPCR, perhaps one of the 136 orphan GPCRs cataloged by IUPHAR ( Sharman et al . 2013 ). We have developed a Deductive Ligand-Receptor Matching Strategy that we recently used to identify the cognate receptor of the peptide hormone

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Christoffer Clemmensen, Sanela Smajilovic, Andreas N Madsen, Anders B Klein, Birgitte Holst and Hans Bräuner-Osborne

GPCRs, which include eight metabotropic glutamate receptors, the calcium-sensing receptor, two γ-aminobutyric acid type B receptors, three T1R taste receptors and a subset of orphan GPCRs ( Wellendorph et al . 2009 a ). The most potent endogenous

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M S Mondal, H Yamaguchi, Y Date, K Toshinai, T Kawagoe, T Tsuruta, H Kageyama, Y Kawamura, S Shioda, Y Shimomura, M Mori and M Nakazato

. Discussion Using cell-based reporter systems, searches for endogenous ligand for orphan GPCRs have led to the discovery of multiple novel peptides ( Kalra et al. 1999 , Schwartz et al. 2000 , Spiegelman & Flier 2001 , Ahima & Osei 2001 ). NPW

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Waljit S Dhillo, Kevin G Murphy and Steve Bloom

process. The conserved sequence of G-protein coupled receptors (GPCRs) has permitted the discovery and cloning of thousands of these receptors. Reverse pharmacology uses libraries of cells expressing these orphan GPCRs to screen putative ligands for

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Takaharu Maruyama, Kenichi Tanaka, Jun Suzuki, Hiroyuki Miyoshi, Naomoto Harada, Takao Nakamura, Yasuhisa Miyamoto, Akio Kanatani and Yoshitaka Tamai

orphan GPCR, which did not show high homology to known GPCRs, and identified the endogenous ligand, bile acid ( Maruyama et al. 2002 , Kawamata et al. 2003 ). We have also revealed that the G protein-coupled bile acid receptor 1 ( Gpbar1/M-Bar/TGR5

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Anne-Marie O'Carroll, Stephen J Lolait, Louise E Harris and George R Pope

be constitutively active ( Jones et al . 2007 , Tanaka et al . 2007 ). The cognate ligands for some of these orphan GPCRs have been identified, often based on the cellular and tissue distributions of the orphan GPCRs and occasionally using ‘reverse

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Georgina G J Hazell, Song T Yao, James A Roper, Eric R Prossnitz, Anne-Marie O'Carroll and Stephen J Lolait

follicle. Scale bars, 1 mm in (A and C–F); 25 μm in (B). Discussion GPR30 was originally cloned by us as an orphan GPCR over 10 years ago ( Owman et al . 1996 ) and subsequently identified as an ER in a number of laboratories ( Filardo et al . 2000

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László Szidonya, Miklós Cserző and László Hunyady

by changing the conformation of the cytoplasmic regions of the receptor that interacts with the G-proteins ( Nag et al . 2007 ). The mechanism may be similar to the one found in the case of GPR50, an orphan GPCR, which has been shown to