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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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Raúl M Luque and Rhonda D Kineman

orphan receptor GPCR107 ( Yosten et al. 2012 , Elrick et al. 2016 ). Importantly, we found that GPCR107 is highly expressed in the baboon pituitary (mRNA levels greater than those for all sst-subtypes) and pituitary GPCR107 expression (but not sst1

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László Szidonya, Miklós Cserző and László Hunyady

. 2003 ). A continually updated list of GPCRs is available at http://www.iupharbb.org/receptorList/results.php ( Foord et al . 2005 ). The natural ligand is presently unknown for many of these receptors hence they are the so-called ‘orphan’ receptors

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Ping Ye, Barbara Mariniello, Franco Mantero, Hirotaka Shibata and William E Rainey

. There are compelling evidence to support elevated expression of certain G-protein-coupled receptors (GPCRs) as a cause of some cases of adrenocorticotrophin (ACTH)-independent Cushing’s syndrome ( Bugalho et al. 2000 , Dall’Asta et al. 2004

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A J W Hsueh, P Bouchard and I Ben-Shlomo

identification of novel ligand and receptor genes similar to those of human glycoprotein hormones and their receptors. As shown in Fig. 1 , five orphan G-protein-coupled receptors have been identified in the human genome based on their sequence homology to human

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

membrane-spanning domains and constitute one of the largest and most diverse gene families in the mammalian genome ( Ostrom & Insel 2004 ). Some novel GPCRs do not have obvious endogenous ligands and are termed orphan receptors, a number of which appear to

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B T Layden, V Durai, M V Newman, A M Marinelarena, C W Ahn, G Feng, S Lin, X Zhang, D B Kaufman, N Jafari, G L Sørensen and W L Lowe Jr

throughput screening for orphan and liganded GPCRs . Combinatorial Chemistry & High Throughput Screening 11 195 – 215 doi:10.2174/138620708783877762 . Zhang H Zhang J Pope CF Crawford LA Vasavada RC Jagasia SM Gannon M 2010 Gestational

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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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T Balla

of the 1980s (Fig. 1 and 2 ). The basic elements of this canonical signal-transduction cascade include the activation of the phospholipase C (PLC) β and γ isoforms by G protein-coupled receptors (GPCRs) and receptor tyrosine kinases (RTKs

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Marcello Maggiolini and Didier Picard

-protein coupled receptors spanning the membrane seven times (7TM-GPCRs). Within this family that comprises hundreds of members, it belongs to the class A rhodopsin-like ones and in there, it constitutes the chemokine receptor-like 2 subfamily. With 28% sequence