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Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
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Table 1 lists a number of putative GPCRs identified by NC-IUPHAR [29], for which preliminary evidence for an endogenous ligand has been published, or for which there exists a potential link to a disease, or disorder. These GPCRs have recently been reviewed in detail [20]. The GPCRs in Table 1 are all Class A, rhodopsin-like GPCRs. Class A orphan GPCRs not listed in Table 1 are putative GPCRs with as-yet unidentified endogenous ligands.
Table 1: Class A orphan GPCRs with putative endogenous ligands
GPR3 | GPR4 | GPR6 | GPR12 | GPR15 | GPR17 | GPR20 |
GPR22 | GPR26 | GPR31 | GPR34 | GPR35 | GPR37 | GPR39 |
GPR50 | GPR63 | GRP65 | GPR68 | GPR75 | GPR84 | GPR87 |
GPR88 | GPR132 | GPR149 | GPR161 | GPR183 | LGR4 | LGR5 |
LGR6 | MAS1 | MRGPRD | MRGPRX1 | MRGPRX2 | P2RY10 | TAAR2 |
GPR3
C
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BB3 receptor
C
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GPR4
C
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GPR6
C
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GPR42
C
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GPR12
C
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GPR15
C
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GPR17
C
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GPR18
C
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GPR19
C
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GPR20
C
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GPR21
C
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GPR22
C
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GPR25
C
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GPR26
C
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GPR27
C
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GPR31
C
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GPR32
C
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GPR33
C
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GPR34
C
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GPR35
C
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GPR37
C
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GPR37L1
C
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GPR39
C
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GPR45
C
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GPR50
C
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GPR55
C
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GPR61
C
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GPR62
C
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GPR63
C
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GPR65
C
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GPR68
C
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GPR75
C
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GPR78
C
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GPR79
C
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GPR82
C
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GPR83
C
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GPR84
C
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GPR85
C
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GPR87
C
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GPR88
C
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GPR101
C
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GPR119
C
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GPR132
C
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GPR135
C
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GPR139
C
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GPR141
C
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GPR142
C
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GPR146
C
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GPR148
C
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GPR149
C
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GPR150
C
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GPR151
C
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GPR152
C
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GPR153
C
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GPR160
C
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GPR161
C
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GPR162
C
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GPR171
C
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GPR173
C
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GPR174
C
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GPR176
C
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GPR182
C
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GPR183
C
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LGR4
C
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LGR5
C
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LGR6
C
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MAS1
C
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MAS1L
C
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MRGPRD
C
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MRGPRE
C
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MRGPRF
C
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MRGPRG
C
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MRGPRX1
C
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MRGPRX2
C
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MRGPRX3
C
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MRGPRX4
C
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P2RY8
C
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P2RY10
C
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TAAR2
C
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TAAR3
C
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TAAR4P
C
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TAAR5
C
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TAAR6
C
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TAAR8
C
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TAAR9
C
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* Key recommended reading is highlighted with an asterisk
* McNeil BD, Pundir P, Meeker S, Han L, Undem BJ, Kulka M, Dong X. (2015) Identification of a mast-cell-specific receptor crucial for pseudo-allergic drug reactions. Nature, 519 (7542): 237-41. [PMID:25517090]
* Wirthgen E, Hoeflich A, Rebl A, Günther J. (2017) Kynurenic Acid: The Janus-Faced Role of an Immunomodulatory Tryptophan Metabolite and Its Link to Pathological Conditions. Front Immunol, 8: 1957. [PMID:29379504]
Zhang LY, Jia MR, Sun T. (2018) The roles of special proresolving mediators in pain relief. Rev Neurosci, 29 (6): 645-660. [PMID:29420307]
1. Adams JW, Wang J, Davis JR, Liaw C, Gaidarov I, Gatlin J, Dalton ND, Gu Y, Ross J, Behan D, Chien K, Connolly D. (2008) Myocardial expression, signaling, and function of GPR22: a protective role for an orphan G protein-coupled receptor. Am. J. Physiol. Heart Circ. Physiol., 295 (2): H509-21. [PMID:18539757]
2. Bechtold DA, Sidibe A, Saer BR, Li J, Hand LE, Ivanova EA, Darras VM, Dam J, Jockers R, Luckman SM et al.. (2012) A role for the melatonin-related receptor GPR50 in leptin signaling, adaptive thermogenesis, and torpor. Curr. Biol., 22 (1): 70-7. [PMID:22197240]
3. Benned-Jensen T, Rosenkilde MM. (2010) Distinct expression and ligand-binding profiles of two constitutively active GPR17 splice variants. Br. J. Pharmacol., 159 (5): 1092-105. [PMID:20148890]
4. Bi Y, Dzierba CD, Fink C, Garcia Y, Green M, Han J, Kwon S, Kumi G, Liang Z, Liu Y et al.. (2015) The discovery of potent agonists for GPR88, an orphan GPCR, for the potential treatment of CNS disorders. Bioorg. Med. Chem. Lett., 25 (7): 1443-7. [PMID:25754495]
5. Bjursell M, Gerdin AK, Jönsson M, Surve VV, Svensson L, Huang XF, Törnell J, Bohlooly-Y M. (2006) G protein-coupled receptor 12 deficiency results in dyslipidemia and obesity in mice. Biochem. Biophys. Res. Commun., 348 (2): 359-66. [PMID:16887097]
6. Borowsky B, Adham N, Jones KA, Raddatz R, Artymyshyn R, Ogozalek KL, Durkin MM, Lakhlani PP, Bonini JA, Pathirana S et al.. (2001) Trace amines: identification of a family of mammalian G protein-coupled receptors. Proc. Natl. Acad. Sci. U.S.A., 98 (16): 8966-71. [PMID:11459929]
7. Brennan, Thomas et al.. (2007) Transgenic mice containing GPCR5-1 gene disruptions. Patent number: US2007/0074299. Assignee: Deltagen. Priority date: 28/08/1999. Publication date: 29/03/2007.
8. Brézillon S, Detheux M, Parmentier M, Hökfelt T, Hurd YL. (2001) Distribution of an orphan G-protein coupled receptor (JP05) mRNA in the human brain. Brain Res., 921 (1-2): 21-30. [PMID:11720708]
9. Bäck M, Powell WS, Dahlén SE, Drazen JM, Evans JF, Serhan CN, Shimizu T, Yokomizo T, Rovati GE. (2014) Update on leukotriene, lipoxin and oxoeicosanoid receptors: IUPHAR Review 7. Br. J. Pharmacol., 171 (15): 3551-74. [PMID:24588652]
10. Carmon KS, Gong X, Lin Q, Thomas A, Liu Q. (2011) R-spondins function as ligands of the orphan receptors LGR4 and LGR5 to regulate Wnt/beta-catenin signaling. Proc. Natl. Acad. Sci. U.S.A., 108 (28): 11452-7. [PMID:21693646]
11. Catalán V, Gómez-Ambrosi J, Rotellar F, Silva C, Gil MJ, Rodríguez A, Cienfuegos JA, Salvador J, Frühbeck G. (2007) The obestatin receptor (GPR39) is expressed in human adipose tissue and is down-regulated in obesity-associated type 2 diabetes mellitus. Clin. Endocrinol. (Oxf), 66 (4): 598-601. [PMID:17371481]
12. Cavanaugh DJ, Lee H, Lo L, Shields SD, Zylka MJ, Basbaum AI, Anderson DJ. (2009) Distinct subsets of unmyelinated primary sensory fibers mediate behavioral responses to noxious thermal and mechanical stimuli. Proc. Natl. Acad. Sci. U.S.A., 106 (22): 9075-80. [PMID:19451647]
13. Chen H, Ikeda SR. (2004) Modulation of ion channels and synaptic transmission by a human sensory neuron-specific G-protein-coupled receptor, SNSR4/mrgX1, heterologously expressed in cultured rat neurons. J. Neurosci., 24 (21): 5044-53. [PMID:15163697]
14. Chen Q, Kogan JH, Gross AK, Zhou Y, Walton NM, Shin R, Heusner CL, Miyake S, Tajinda K, Tamura K et al.. (2012) SREB2/GPR85, a schizophrenia risk factor, negatively regulates hippocampal adult neurogenesis and neurogenesis-dependent learning and memory. Eur. J. Neurosci., 36 (5): 2597-608. [PMID:22697179]
15. Chiang N, Fredman G, Bäckhed F, Oh SF, Vickery T, Schmidt BA, Serhan CN. (2012) Infection regulates pro-resolving mediators that lower antibiotic requirements. Nature, 484 (7395): 524-8. [PMID:22538616]
16. Chobanian HR, Guo Y, Liu P, Chioda M, Lanza Jr TJ, Chang L, Kelly TM, Kan Y, Palyha O, Guan XM et al.. (2012) Discovery of MK-7725, A Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity. ACS Med Chem Lett, 3 (3): 252-6. [PMID:24900461]
17. Chu ZL, Carroll C, Chen R, Alfonso J, Gutierrez V, He H, Lucman A, Xing C, Sebring K, Zhou J et al.. (2010) N-oleoyldopamine enhances glucose homeostasis through the activation of GPR119. Mol. Endocrinol., 24 (1): 161-70. [PMID:19901198]
18. Ciana P, Fumagalli M, Trincavelli ML, Verderio C, Rosa P, Lecca D, Ferrario S, Parravicini C, Capra V, Gelosa P, Guerrini U, Belcredito S, Cimino M, Sironi L, Tremoli E, Rovati GE, Martini C, Abbracchio MP. (2006) The orphan receptor GPR17 identified as a new dual uracil nucleotides/cysteinyl-leukotrienes receptor. EMBO J., 25 (19): 4615-27. [PMID:16990797]
19. Console-Bram L, Brailoiu E, Brailoiu GC, Sharir H, Abood ME. (2014) Activation of GPR18 by cannabinoid compounds: a tale of biased agonism. Br. J. Pharmacol., 171 (16): 3908-17. [PMID:24762058]
20. Davenport AP, Alexander SP, Sharman JL, Pawson AJ, Benson HE, Monaghan AE, Liew WC, Mpamhanga CP, Bonner TI, Neubig RR et al.. (2013) International Union of Basic and Clinical Pharmacology. LXXXVIII. G protein-coupled receptor list: recommendations for new pairings with cognate ligands. Pharmacol. Rev., 65 (3): 967-86. [PMID:23686350]
21. de Lau W, Barker N, Low TY, Koo BK, Li VS, Teunissen H, Kujala P, Haegebarth A, Peters PJ, van de Wetering M et al.. (2011) Lgr5 homologues associate with Wnt receptors and mediate R-spondin signalling. Nature, 476 (7360): 293-7. [PMID:21727895]
22. Dinter J, Mühlhaus J, Wienchol CL, Yi CX, Nürnberg D, Morin S, Grüters A, Köhrle J, Schöneberg T, Tschöp M et al.. (2015) Inverse agonistic action of 3-iodothyronamine at the human trace amine-associated receptor 5. PLoS ONE, 10 (2): e0117774. [PMID:25706283]
23. Divorty N, Mackenzie AE, Nicklin SA, Milligan G. (2015) G protein-coupled receptor 35: an emerging target in inflammatory and cardiovascular disease. Front Pharmacol, 6: 41. [PMID:25805994]
24. Edinger AL, Mankowski JL, Doranz BJ, Margulies BJ, Lee B, Rucker J, Sharron M, Hoffman TL, Berson JF, Zink MC, Hirsch VM, Clements JE, Doms RW. (1997) CD4-independent, CCR5-dependent infection of brain capillary endothelial cells by a neurovirulent simian immunodeficiency virus strain. Proc. Natl. Acad. Sci. U.S.A., 94 (26): 14742-7. [PMID:9405683]
25. Edson MA, Lin YN, Matzuk MM. (2010) Deletion of the novel oocyte-enriched gene, Gpr149, leads to increased fertility in mice. Endocrinology, 151 (1): 358-68. [PMID:19887567]
26. Eggerickx D, Denef JF, Labbe O, Hayashi Y, Refetoff S, Vassart G, Parmentier M, Libert F. (1995) Molecular cloning of an orphan G-protein-coupled receptor that constitutively activates adenylate cyclase. Biochem. J., 309 ( Pt 3): 837-43. [PMID:7639700]
27. Engel KM, Schröck K, Teupser D, Holdt LM, Tönjes A, Kern M, Dietrich K, Kovacs P, Krügel U, Scheidt HA et al.. (2011) Reduced food intake and body weight in mice deficient for the G protein-coupled receptor GPR82. PLoS ONE, 6 (12): e29400. [PMID:22216272]
28. Evangelou E, Valdes AM, Kerkhof HJ, Styrkarsdottir U, Zhu Y, Meulenbelt I, Lories RJ, Karassa FB, Tylzanowski P, Bos SD et al.. (2011) Meta-analysis of genome-wide association studies confirms a susceptibility locus for knee osteoarthritis on chromosome 7q22. Ann. Rheum. Dis., 70 (2): 349-55. [PMID:21068099]
29. Foord SM, Bonner TI, Neubig RR, Rosser EM, Pin JP, Davenport AP, Spedding M, Harmar AJ. (2005) International Union of Pharmacology. XLVI. G protein-coupled receptor list. Pharmacol. Rev., 57 (2): 279-88. [PMID:15914470]
30. Gembardt F, Grajewski S, Vahl M, Schultheiss HP, Walther T. (2008) Angiotensin metabolites can stimulate receptors of the Mas-related genes family. Mol. Cell. Biochem., 319 (1-2): 115-23. [PMID:18636314]
31. Gironacci MM, Adamo HP, Corradi G, Santos RA, Ortiz P, Carretero OA. (2011) Angiotensin (1-7) induces MAS receptor internalization. Hypertension, 58 (2): 176-81. [PMID:21670420]
32. Gomes I, Aryal DK, Wardman JH, Gupta A, Gagnidze K, Rodriguiz RM, Kumar S, Wetsel WC, Pintar JE, Fricker LD et al.. (2013) GPR171 is a hypothalamic G protein-coupled receptor for BigLEN, a neuropeptide involved in feeding. Proc. Natl. Acad. Sci. U.S.A., 110 (40): 16211-6. [PMID:24043826]
33. Gomes I, Bobeck EN, Margolis EB, Gupta A, Sierra S, Fakira AK, Fujita W, Müller TD, Müller A, Tschöp MH et al.. (2016) Identification of GPR83 as the receptor for the neuroendocrine peptide PEN. Sci Signal, 9 (425): ra43. [PMID:27117253]
34. Guan XM, Chen H, Dobbelaar PH, Dong Y, Fong TM, Gagen K, Gorski J, He S, Howard AD, Jian T et al.. (2010) Regulation of energy homeostasis by bombesin receptor subtype-3: selective receptor agonists for the treatment of obesity. Cell Metab., 11 (2): 101-12. [PMID:20096642]
35. Guo Y, Zhang W, Giroux C, Cai Y, Ekambaram P, Dilly AK, Hsu A, Zhou S, Maddipati KR, Liu J et al.. (2011) Identification of the orphan G protein-coupled receptor GPR31 as a receptor for 12-(S)-hydroxyeicosatetraenoic acid. J. Biol. Chem., 286 (39): 33832-40. [PMID:21712392]
36. Han S, Narayanan S, Kim SH, Calderon I, Zhu X, Kawasaki A, Yue D, Lehmann J, Wong A, Buzard DJ et al.. (2015) Discovery of a novel trans-1,4-dioxycyclohexane GPR119 agonist series. Bioorg. Med. Chem. Lett., 25 (15): 3034-8. [PMID:26048791]
37. Hannedouche S, Zhang J, Yi T, Shen W, Nguyen D, Pereira JP, Guerini D, Baumgarten BU, Roggo S, Wen B et al.. (2011) Oxysterols direct immune cell migration via EBI2. Nature, 475 (7357): 524-7. [PMID:21796212]
38. Hansen W, Westendorf AM, Toepfer T, Mauel S, Geffers R, Gruber AD, Buer J. (2010) Inflammation in vivo is modulated by GPR83 isoform-4 but not GPR83 isoform-1 expression in regulatory T cells. Genes Immun., 11 (4): 357-61. [PMID:20200545]
39. Hase M, Yokomizo T, Shimizu T, Nakamura M. (2008) Characterization of an orphan G protein-coupled receptor, GPR20, that constitutively activates Gi proteins. J. Biol. Chem., 283 (19): 12747-55. [PMID:18347022]
40. Hay DL, Walker CS, Poyner DR. (2011) Adrenomedullin and calcitonin gene-related peptide receptors in endocrine-related cancers: opportunities and challenges. Endocr. Relat. Cancer, 18 (1): C1-14. [PMID:21051558]
41. He S, Dobbelaar PH, Liu J, Jian T, Sebhat IK, Lin LS, Goodman A, Guo C, Guzzo PR, Hadden M et al.. (2010) Discovery of substituted biphenyl imidazoles as potent, bioavailable bombesin receptor subtype-3 agonists. Bioorg. Med. Chem. Lett., 20 (6): 1913-7. [PMID:20167483]
42. Henstridge CM, Balenga NA, Schröder R, Kargl JK, Platzer W, Martini L, Arthur S, Penman J, Whistler JL, Kostenis E, Waldhoer M, Irving AJ. (2010) GPR55 ligands promote receptor coupling to multiple signalling pathways. Br. J. Pharmacol., 160 (3): 604-14. [PMID:20136841]
43. Heynen-Genel S, Dahl R, Shi S, Milan L, Hariharan S, Sergienko E, Hedrick M, Dad S, Stonich D, Su Y et al.. (2010) Screening for Selective Ligands for GPR55 - Antagonists. Probe Reports from the NIH Molecular Libraries Program,. [PMID:22091481]
44. Holst B, Egerod KL, Schild E, Vickers SP, Cheetham S, Gerlach LO, Storjohann L, Stidsen CE, Jones R, Beck-Sickinger AG, Schwartz TW. (2007) GPR39 signaling is stimulated by zinc ions but not by obestatin. Endocrinology, 148: 13-20. [PMID:16959833]
45. Huang XP, Karpiak J, Kroeze WK, Zhu H, Chen X, Moy SS, Saddoris KA, Nikolova VD, Farrell MS, Wang S et al.. (2015) Allosteric ligands for the pharmacologically dark receptors GPR68 and GPR65. Nature, 527 (7579): 477-83. [PMID:26550826]
46. Ignatov A, Hermans-Borgmeyer I, Schaller HC. (2004) Cloning and characterization of a novel G-protein-coupled receptor with homology to galanin receptors. Neuropharmacology, 46 (8): 1114-20. [PMID:15111018]
47. Ignatov A, Lintzel J, Hermans-Borgmeyer I, Kreienkamp HJ, Joost P, Thomsen S, Methner A, Schaller HC. (2003) Role of the G-protein-coupled receptor GPR12 as high-affinity receptor for sphingosylphosphorylcholine and its expression and function in brain development. J. Neurosci., 23 (3): 907-14. [PMID:12574419]
48. Ignatov A, Lintzel J, Kreienkamp HJ, Schaller HC. (2003) Sphingosine-1-phosphate is a high-affinity ligand for the G protein-coupled receptor GPR6 from mouse and induces intracellular Ca2+ release by activating the sphingosine-kinase pathway. Biochem. Biophys. Res. Commun., 311 (2): 329-36. [PMID:14592418]
49. Ignatov A, Robert J, Gregory-Evans C, Schaller HC. (2006) RANTES stimulates Ca2+ mobilization and inositol trisphosphate (IP3) formation in cells transfected with G protein-coupled receptor 75. Br. J. Pharmacol., 149 (5): 490-7. [PMID:17001303]
50. Ikubo M, Inoue A, Nakamura S, Jung S, Sayama M, Otani Y, Uwamizu A, Suzuki K, Kishi T, Shuto A et al.. (2015) Structure-Activity Relationships of Lysophosphatidylserine Analogs as Agonists of G-Protein-Coupled Receptors GPR34, P2Y10, and GPR174. J. Med. Chem., 58 (10): 4204-19. [PMID:25970039]
51. Inoue A, Ishiguro J, Kitamura H, Arima N, Okutani M, Shuto A, Higashiyama S, Ohwada T, Arai H, Makide K et al.. (2012) TGFα shedding assay: an accurate and versatile method for detecting GPCR activation. Nat. Methods, 9 (10): 1021-9. [PMID:22983457]
52. Isberg V, Andersen KB, Bisig C, Dietz GP, Bräuner-Osborne H, Gloriam DE. (2014) Computer-aided discovery of aromatic l-α-amino acids as agonists of the orphan G protein-coupled receptor GPR139. J Chem Inf Model, 54 (6): 1553-7. [PMID:24826842]
53. Jensen T, Elster L, Nielsen SM, Poda SB, Loechel F, Volbracht C, Klewe IV, David L, Watson SP. (2014) The identification of GPR3 inverse agonist AF64394; the first small molecule inhibitor of GPR3 receptor function. Bioorg. Med. Chem. Lett., 24 (22): 5195-8. [PMID:25442311]
54. Jin C, Yin F, Lin M, Li H, Wang Z, Weng J, Liu M, Da Dong X, Qu J, Tu L. (2008) GPR48 regulates epithelial cell proliferation and migration by activating EGFR during eyelid development. Invest. Ophthalmol. Vis. Sci., 49 (10): 4245-53. [PMID:18487371]
55. Jones PG, Nawoschik SP, Sreekumar K, Uveges AJ, Tseng E, Zhang L, Johnson J, He L, Paulsen JE, Bates B, Pausch MH. (2007) Tissue distribution and functional analyses of the constitutively active orphan G protein coupled receptors, GPR26 and GPR78. Biochim. Biophys. Acta, 1770 (6): 890-901. [PMID:17363172]
56. Kabarowski JH, Zhu K, Le LQ, Witte ON, Xu Y. (2001) Lysophosphatidylcholine as a ligand for the immunoregulatory receptor G2A. Science, 293 (5530): 702-5. [PMID:11474113]
57. Kamohara M, Matsuo A, Takasaki J, Kohda M, Matsumoto M, Matsumoto S, Soga T, Hiyama H, Kobori M, Katou M. (2005) Identification of MrgX2 as a human G-protein-coupled receptor for proadrenomedullin N-terminal peptides. Biochem. Biophys. Res. Commun., 330 (4): 1146-52. [PMID:15823563]
58. Kapas S, Catt KJ, Clark AJ. (1995) Cloning and expression of cDNA encoding a rat adrenomedullin receptor. J. Biol. Chem., 270 (43): 25344-7. [PMID:7592696]
59. Kapur A, Zhao P, Sharir H, Bai Y, Caron MG, Barak LS, Abood ME. (2009) Atypical responsiveness of the orphan receptor GPR55 to cannabinoid ligands. J. Biol. Chem., 284 (43): 29817-27. [PMID:19723626]
60. Kargl J, Brown AJ, Andersen L, Dorn G, Schicho R, Waldhoer M, Heinemann A. (2013) A selective antagonist reveals a potential role of G protein-coupled receptor 55 in platelet and endothelial cell function. J. Pharmacol. Exp. Ther., 346 (1): 54-66. [PMID:23639801]
61. Kelly LM, Pereira JP, Yi T, Xu Y, Cyster JG. (2011) EBI2 guides serial movements of activated B cells and ligand activity is detectable in lymphoid and nonlymphoid tissues. J. Immunol., 187 (6): 3026-32. [PMID:21844396]
62. Kennedy SP, Sun D, Oleynek JJ, Hoth CF, Kong J, Hill RJ. (1998) Expression of the rat adrenomedullin receptor or a putative human adrenomedullin receptor does not correlate with adrenomedullin binding or functional response. Biochem. Biophys. Res. Commun., 244 (3): 832-7. [PMID:9535752]
63. Kerkhof HJ, Lories RJ, Meulenbelt I, Jonsdottir I, Valdes AM, Arp P, Ingvarsson T, Jhamai M, Jonsson H, Stolk L, Thorleifsson G, Zhai G, Zhang F, Zhu Y, van der Breggen R, Carr A, Doherty M, Doherty S, Felson DT, Gonzalez A, Halldorsson BV, Hart DJ, Hauksson VB, Hofman A, Ioannidis JP, Kloppenburg M, Lane NE, Loughlin J, Luyten FP, Nevitt MC, Parimi N, Pols HA, Rivadeneira F, Slagboom EP, Styrkársdóttir U, Tsezou A, van de Putte T, Zmuda J, Spector TD, Stefansson K, Uitterlinden AG, van Meurs JB. (2010) A genome-wide association study identifies an osteoarthritis susceptibility locus on chromosome 7q22. Arthritis Rheum., 62 (2): 499-510. [PMID:20112360]
64. Kim SV, Xiang WV, Kwak C, Yang Y, Lin XW, Ota M, Sarpel U, Rifkin DB, Xu R, Littman DR. (2013) GPR15-mediated homing controls immune homeostasis in the large intestine mucosa. Science, 340 (6139): 1456-9. [PMID:23661644]
65. Kitamura H, Makide K, Shuto A, Ikubo M, Inoue A, Suzuki K, Sato Y, Nakamura S, Otani Y, Ohwada T et al.. (2012) GPR34 is a receptor for lysophosphatidylserine with a fatty acid at the sn-2 position. J. Biochem., 151 (5): 511-8. [PMID:22343749]
66. Kohno M, Hasegawa H, Inoue A, Muraoka M, Miyazaki T, Oka K, Yasukawa M. (2006) Identification of N-arachidonylglycine as the endogenous ligand for orphan G-protein-coupled receptor GPR18. Biochem. Biophys. Res. Commun., 347 (3): 827-32. [PMID:16844083]
67. Korstanje R, Desai J, Lazar G, King B, Rollins J, Spurr M, Joseph J, Kadambi S, Li Y, Cherry A, Matteson PG, Paigen B, Millonig JH. (2008) Quantitative trait loci affecting phenotypic variation in the vacuolated lens mouse mutant, a multigenic mouse model of neural tube defects. Physiol. Genomics, 35 (3): 296-304. [PMID:18796533]
68. Kottyan LC, Collier AR, Cao KH, Niese KA, Hedgebeth M, Radu CG, Witte ON, Khurana Hershey GK, Rothenberg ME, Zimmermann N. (2009) Eosinophil viability is increased by acidic pH in a cAMP- and GPR65-dependent manner. Blood, 114 (13): 2774-82. [PMID:19641187]
69. Krishnamoorthy S, Recchiuti A, Chiang N, Yacoubian S, Lee CH, Yang R, Petasis NA, Serhan CN. (2010) Resolvin D1 binds human phagocytes with evidence for proresolving receptors. Proc. Natl. Acad. Sci. U.S.A., 107 (4): 1660-5. [PMID:20080636]
70. Ku GM, Pappalardo Z, Luo CC, German MS, McManus MT. (2012) An siRNA screen in pancreatic beta cells reveals a role for Gpr27 in insulin production. PLoS Genet., 8 (1): e1002449. [PMID:22253604]
71. Kuc D, Zgrajka W, Parada-Turska J, Urbanik-Sypniewska T, Turski WA. (2008) Micromolar concentration of kynurenic acid in rat small intestine. Amino Acids, 35 (2): 503-5. [PMID:18235993]
72. Lansu K, Karpiak J, Liu J, Huang XP, McCorvy JD, Kroeze WK, Che T, Nagase H, Carroll FI, Jin J et al.. (2017) In silico design of novel probes for the atypical opioid receptor MRGPRX2. Nat. Chem. Biol., 13 (5): 529-536. [PMID:28288109]
73. Lautner RQ, Villela DC, Fraga-Silva RA, Silva N, Verano-Braga T, Costa-Fraga F, Jankowski J, Jankowski V, Sousa F, Alzamora A et al.. (2013) Discovery and characterization of alamandine: a novel component of the Renin-Angiotensin system. Circ. Res., 112 (8): 1104-11. [PMID:23446738]
74. Ledent C, Demeestere I, Blum D, Petermans J, Hämäläinen T, Smits G, Vassart G. (2005) Premature ovarian aging in mice deficient for Gpr3. Proc. Natl. Acad. Sci. U.S.A., 102 (25): 8922-6. [PMID:15956199]
75. Lembo PM, Grazzini E, Groblewski T, O'Donnell D, Roy MO, Zhang J, Hoffert C, Cao J, Schmidt R, Pelletier M et al.. (2002) Proenkephalin A gene products activate a new family of sensory neuron--specific GPCRs. Nat. Neurosci., 5 (3): 201-9. [PMID:11850634]
76. Leung T, Humbert JE, Stauffer AM, Giger KE, Chen H, Tsai HJ, Wang C, Mirshahi T, Robishaw JD. (2008) The orphan G protein-coupled receptor 161 is required for left-right patterning. Dev. Biol., 323 (1): 31-40. [PMID:18755178]
77. Levoye A, Dam J, Ayoub MA, Guillaume JL, Couturier C, Delagrange P, Jockers R. (2006) The orphan GPR50 receptor specifically inhibits MT1 melatonin receptor function through heterodimerization. EMBO J., 25 (13): 3012-23. [PMID:16778767]
78. Liebscher I, Müller U, Teupser D, Engemaier E, Engel KM, Ritscher L, Thor D, Sangkuhl K, Ricken A, Wurm A et al.. (2011) Altered immune response in mice deficient for the G protein-coupled receptor GPR34. J. Biol. Chem., 286 (3): 2101-10. [PMID:21097509]
79. Lindfors L, Sundström L, Fröderberg Roth L, Meuller J, Andersson S, Kihlberg J. (2020) Is GPR146 really the receptor for proinsulin C-peptide?. Bioorg. Med. Chem. Lett., 30 (13): 127208. [PMID:32354568]
80. Liu C, Yang XV, Wu J, Kuei C, Mani NS, Zhang L, Yu J, Sutton SW, Qin N, Banie H et al.. (2011) Oxysterols direct B-cell migration through EBI2. Nature, 475 (7357): 519-23. [PMID:21796211]
81. Liu Q, Tang Z, Surdenikova L, Kim S, Patel KN, Kim A, Ru F, Guan Y, Weng HJ, Geng Y, Undem BJ, Kollarik M, Chen ZF, Anderson DJ, Dong X. (2009) Sensory neuron-specific GPCR Mrgprs are itch receptors mediating chloroquine-induced pruritus. Cell, 139 (7): 1353-65. [PMID:20004959]
82. Lobo MK, Cui Y, Ostlund SB, Balleine BW, Yang XW. (2007) Genetic control of instrumental conditioning by striatopallidal neuron-specific S1P receptor Gpr6. Nat. Neurosci., 10 (11): 1395-7. [PMID:17934457]
83. Logue SF, Grauer SM, Paulsen J, Graf R, Taylor N, Sung MA, Zhang L, Hughes Z, Pulito VL, Liu F, Rosenzweig-Lipson S, Brandon NJ, Marquis KL, Bates B, Pausch M. (2009) The orphan GPCR, GPR88, modulates function of the striatal dopamine system: a possible therapeutic target for psychiatric disorders?. Mol. Cell. Neurosci., 42 (4): 438-47. [PMID:19796684]
84. Luo J, Zhou W, Zhou X, Li D, Weng J, Yi Z, Cho SG, Li C, Yi T, Wu X, Li XY, de Crombrugghe B, Höök M, Liu M. (2009) Regulation of bone formation and remodeling by G-protein-coupled receptor 48. Development, 136 (16): 2747-56. [PMID:19605502]
85. Maekawa A, Balestrieri B, Austen KF, Kanaoka Y. (2009) GPR17 is a negative regulator of the cysteinyl leukotriene 1 receptor response to leukotriene D4. Proc. Natl. Acad. Sci. U.S.A., 106 (28): 11685-90. [PMID:19561298]
86. Mantey SA, Coy DH, Entsuah LK, Jensen RT. (2004) Development of bombesin analogs with conformationally restricted amino acid substitutions with enhanced selectivity for the orphan receptor human bombesin receptor subtype 3. J. Pharmacol. Exp. Ther., 310 (3): 1161-70. [PMID:15102928]
87. Mantey SA, Weber HC, Sainz E, Akeson M, Ryan RR, Pradhan TK, Searles RP, Spindel ER, Battey JF, Coy DH et al.. (1997) Discovery of a high affinity radioligand for the human orphan receptor, bombesin receptor subtype 3, which demonstrates that it has a unique pharmacology compared with other mammalian bombesin receptors. J. Biol. Chem., 272 (41): 26062-71. [PMID:9325344]
88. Marazziti D, Di Pietro C, Golini E, Mandillo S, Matteoni R, Tocchini-Valentini GP. (2009) Macroautophagy of the GPR37 orphan receptor and Parkinson disease-associated neurodegeneration. Autophagy, 5 (5): 741-2. [PMID:19398891]
89. Marazziti D, Di Pietro C, Mandillo S, Golini E, Matteoni R, Tocchini-Valentini GP. (2011) Absence of the GPR37/PAEL receptor impairs striatal Akt and ERK2 phosphorylation, DeltaFosB expression, and conditioned place preference to amphetamine and cocaine. FASEB J., 25 (6): 2071-81. [PMID:21372109]
90. Marazziti D, Mandillo S, Di Pietro C, Golini E, Matteoni R, Tocchini-Valentini GP. (2007) GPR37 associates with the dopamine transporter to modulate dopamine uptake and behavioral responses to dopaminergic drugs. Proc. Natl. Acad. Sci. U.S.A., 104 (23): 9846-51. [PMID:17519329]
91. Marsango S, Barki N, Jenkins L, Tobin AB, Milligan G. (2020) Therapeutic validation of an orphan G protein-coupled receptor: The case of GPR84. Br. J. Pharmacol., [Epub ahead of print]. [PMID:32869860]
92. Matsufuji T, Shimada K, Kobayashi S, Ichikawa M, Kawamura A, Fujimoto T, Arita T, Hara T, Konishi M, Abe-Ohya R et al.. (2015) Synthesis and biological evaluation of novel chiral diazepine derivatives as bombesin receptor subtype-3 (BRS-3) agonists incorporating an antedrug approach. Bioorg. Med. Chem., 23 (1): 89-104. [PMID:25497965]
93. Matsufuji T, Shimada K, Kobayashi S, Kawamura A, Fujimoto T, Arita T, Hara T, Konishi M, Abe-Ohya R, Izumi M et al.. (2014) Discovery of novel chiral diazepines as bombesin receptor subtype-3 (BRS-3) agonists with low brain penetration. Bioorg. Med. Chem. Lett., 24 (3): 750-5. [PMID:24412111]
94. Matteson PG, Desai J, Korstanje R, Lazar G, Borsuk TE, Rollins J, Kadambi S, Joseph J, Rahman T, Wink J, Benayed R, Paigen B, Millonig JH. (2008) The orphan G protein-coupled receptor, Gpr161, encodes the vacuolated lens locus and controls neurulation and lens development. Proc. Natl. Acad. Sci. U.S.A., 105 (6): 2088-93. [PMID:18250320]
95. Meyer RC, Giddens MM, Schaefer SA, Hall RA. (2013) GPR37 and GPR37L1 are receptors for the neuroprotective and glioprotective factors prosaptide and prosaposin. Proc. Natl. Acad. Sci. U.S.A., 110 (23): 9529-34. [PMID:23690594]
96. Moody TW, Mantey SA, Moreno P, Nakamura T, Lacivita E, Leopoldo M, Jensen RT. (2015) ML-18 is a non-peptide bombesin receptor subtype-3 antagonist which inhibits lung cancer growth. Peptides, 64: 55-61. [PMID:25554218]
97. Moreno P, Mantey SA, Nuche-Berenguer B, Reitman ML, Gonzalez N, , Coy DH, Jensen RT. (2013) Comparative Pharmacology of Bombesin Receptor Subtype-3, Nonpeptide Agonist MK-5046, a Universal Peptide Agonist, and Peptide Antagonist Bantag-1 for Human Bombesin Receptors. Pharmacol Exp Therap, 347 (1): 100-116. [PMID:23892571]
98. Murakami M, Shiraishi A, Tabata K, Fujita N. (2008) Identification of the orphan GPCR, P2Y(10) receptor as the sphingosine-1-phosphate and lysophosphatidic acid receptor. Biochem. Biophys. Res. Commun., 371 (4): 707-12. [PMID:18466763]
99. Müller A, Kleinau G, Piechowski CL, Müller TD, Finan B, Pratzka J, Grüters A, Krude H, Tschöp M, Biebermann H. (2013) G-protein coupled receptor 83 (GPR83) signaling determined by constitutive and zinc(II)-induced activity. PLoS ONE, 8 (1): e53347. [PMID:23335960]
100. Müller A, Leinweber B, Fischer J, Müller TD, Grüters A, Tschöp MH, Knäuper V, Biebermann H, Kleinau G. (2014) The extracellular N-terminal domain of G-protein coupled receptor 83 regulates signaling properties and is an intramolecular inverse agonist. BMC Res Notes, 7: 913. [PMID:25516095]
101. Nambu H, Fukushima M, Hikichi H, Inoue T, Nagano N, Tahara Y, Nambu T, Ito J, Ogawa Y, Ozaki S et al.. (2011) Characterization of metabolic phenotypes of mice lacking GPR61, an orphan G-protein coupled receptor. Life Sci., 89 (21-22): 765-72. [PMID:21971119]
102. Niedernberg A, Tunaru S, Blaukat A, Ardati A, Kostenis E. (2003) Sphingosine 1-phosphate and dioleoylphosphatidic acid are low affinity agonists for the orphan receptor GPR63. Cell. Signal., 15 (4): 435-46. [PMID:12618218]
103. Nikaido Y, Koyama Y, Yoshikawa Y, Furuya T, Takeda S. (2015) Mutation analysis and molecular modeling for the investigation of ligand-binding modes of GPR84. J. Biochem., 157 (5): 311-20. [PMID:25425658]
104. Ning Y, O'Neill K, Lan H, Pang L, Shan LX, Hawes BE, Hedrick JA. (2008) Endogenous and synthetic agonists of GPR119 differ in signalling pathways and their effects on insulin secretion in MIN6c4 insulinoma cells. Br. J. Pharmacol., 155 (7): 1056-65. [PMID:18724386]
105. Nio Y, Hotta N, Maruyama M, Hamagami K, Nagi T, Funata M, Sakamoto J, Nakakariya M, Amano N, Okawa T et al.. (2017) A Selective Bombesin Receptor Subtype 3 Agonist Promotes Weight Loss in Male Diet-Induced-Obese Rats With Circadian Rhythm Change. Endocrinology, 158 (5): 1298-1313. [PMID:28324017]
106. No authors listed. (2005) Sphingosylphosphorylcholine and lysophosphatidylcholine are ligands for the G protein-coupled receptor GPR4. (Retraction). J. Biol. Chem., 280 (52): 43280. [PMID:16498716]
107. Oka S, Nakajima K, Yamashita A, Kishimoto S, Sugiura T. (2007) Identification of GPR55 as a lysophosphatidylinositol receptor. Biochem. Biophys. Res. Commun., 362 (4): 928-34. [PMID:17765871]
108. Oka S, Ota R, Shima M, Yamashita A, Sugiura T. (2010) GPR35 is a novel lysophosphatidic acid receptor. Biochem. Biophys. Res. Commun., 395 (2): 232-7. [PMID:20361937]
109. Oka S, Toshida T, Maruyama K, Nakajima K, Yamashita A, Sugiura T. (2009) 2-Arachidonoyl-sn-glycero-3-phosphoinositol: a possible natural ligand for GPR55. J. Biochem., 145 (1): 13-20. [PMID:18845565]
110. Osborn O, Oh da Y, McNelis J, Sanchez-Alavez M, Talukdar S, Lu M, Li P, Thiede L, Morinaga H, Kim JJ et al.. (2012) G protein-coupled receptor 21 deletion improves insulin sensitivity in diet-induced obese mice. J. Clin. Invest., 122 (7): 2444-53. [PMID:22653059]
111. Overton HA, Babbs AJ, Doel SM, Fyfe MC, Gardner LS, Griffin G, Jackson HC, Procter MJ, Rasamison CM, Tang-Christensen M et al.. (2006) Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents. Cell Metab., 3 (3): 167-75. [PMID:16517404]
112. Padmanabhan S, Myers AG, Prasad BM. (2009) Constitutively active GPR6 is located in the intracellular compartments. FEBS Lett., 583 (1): 107-12. [PMID:19059244]
113. Pereira JP, Kelly LM, Xu Y, Cyster JG. (2009) EBI2 mediates B cell segregation between the outer and centre follicle. Nature, 460 (7259): 1122-6. [PMID:19597478]
114. Petersen PS, Jin C, Madsen AN, Rasmussen M, Kuhre R, Egerod KL, Nielsen LB, Schwartz TW, Holst B. (2011) Deficiency of the GPR39 receptor is associated with obesity and altered adipocyte metabolism. FASEB J., 25 (11): 3803-14. [PMID:21784784]
115. Pringle KG, Tadros MA, Callister RJ, Lumbers ER. (2011) The expression and localization of the human placental prorenin/renin-angiotensin system throughout pregnancy: roles in trophoblast invasion and angiogenesis?. Placenta, 32 (12): 956-62. [PMID:22018415]
116. Ramachandran V, Arumugam T, Langley R, Hwang RF, Vivas-Mejia P, Sood AK, Lopez-Berestein G, Logsdon CD. (2009) The ADMR receptor mediates the effects of adrenomedullin on pancreatic cancer cells and on cells of the tumor microenvironment. PLoS ONE, 4 (10): e7502. [PMID:19847298]
117. Ramos-Alvarez I, Lee L, Mantey SA, Jensen RT. (2019) Development and Characterization of a Novel, High-Affinity, Specific, Radiolabeled Ligand for BRS-3 Receptors. J. Pharmacol. Exp. Ther., 369 (3): 454-465. [PMID:30971479]
118. Ramos-Álvarez I, Nakamura T, Mantey SA, Moreno P, Nuche-Berenguer B, Jensen RT. (2016) Novel chiral-diazepines function as specific, selective receptor agonists with variable coupling and species variability in human, mouse and rat BRS-3 receptor cells. Peptides, 75: 8-17. [PMID:26524625]
119. Rao A, Herr DR. (2017) G protein-coupled receptor GPR19 regulates E-cadherin expression and invasion of breast cancer cells. Biochim. Biophys. Acta, 1864 (7): 1318-1327. [PMID:28476646]
120. Rezgaoui M, Süsens U, Ignatov A, Gelderblom M, Glassmeier G, Franke I, Urny J, Imai Y, Takahashi R, Schaller HC. (2006) The neuropeptide head activator is a high-affinity ligand for the orphan G-protein-coupled receptor GPR37. J. Cell. Sci., 119 (Pt 3): 542-9. [PMID:16443751]
121. Robas N, Mead E, Fidock M. (2003) MrgX2 is a high potency cortistatin receptor expressed in dorsal root ganglion. J. Biol. Chem., 278 (45): 44400-4. [PMID:12915402]
122. Ruffner H, Sprunger J, Charlat O, Leighton-Davies J, Grosshans B, Salathe A, Zietzling S, Beck V, Therier M, Isken A et al.. (2012) R-Spondin potentiates Wnt/β-catenin signaling through orphan receptors LGR4 and LGR5. PLoS ONE, 7 (7): e40976. [PMID:22815884]
123. Ruiz-Medina J, Ledent C, Valverde O. (2011) GPR3 orphan receptor is involved in neuropathic pain after peripheral nerve injury and regulates morphine-induced antinociception. Neuropharmacology, 61 (1-2): 43-50. [PMID:21352831]
124. Russell JL, Goetsch SC, Aguilar HR, Coe H, Luo X, Liu N, van Rooij E, Frantz DE, Schneider JW. (2012) Regulated expression of pH sensing G Protein-coupled receptor-68 identified through chemical biology defines a new drug target for ischemic heart disease. ACS Chem. Biol., 7 (6): 1077-83. [PMID:22462679]
125. Ryberg E, Larsson N, Sjögren S, Hjorth S, Hermansson NO, Leonova J, Elebring T, Nilsson K, Drmota T, Greasley PJ. (2007) The orphan receptor GPR55 is a novel cannabinoid receptor. Br. J. Pharmacol., 152 (7): 1092-101. [PMID:17876302]
126. Römpler H, Schulz A, Pitra C, Coop G, Przeworski M, Pääbo S, Schöneberg T. (2005) The rise and fall of the chemoattractant receptor GPR33. J. Biol. Chem., 280 (35): 31068-75. [PMID:15987686]
127. Sebhat IK, Franklin C, Lo MM, Chen D, Jewell JP, Miller R, Pang J, Palyha O, Kan Y, Kelly TM et al.. (2011) Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity. ACS Med Chem Lett, 2 (1): 43-7. [PMID:24900253]
128. Setoh M, Ishii N, Kono M, Miyanohana Y, Shiraishi E, Harasawa T, Ota H, Odani T, Kanzaki N, Aoyama K et al.. (2014) Discovery of the first potent and orally available agonist of the orphan G-protein-coupled receptor 52. J. Med. Chem., 57 (12): 5226-37. [PMID:24884590]
129. Seuwen K, Ludwig MG, Wolf RM. (2006) Receptors for protons or lipid messengers or both?. J. Recept. Signal Transduct. Res., 26 (5-6): 599-610. [PMID:17118800]
130. Shinohara T, Harada M, Ogi K, Maruyama M, Fujii R, Tanaka H, Fukusumi S, Komatsu H, Hosoya M, Noguchi Y et al.. (2004) Identification of a G protein-coupled receptor specifically responsive to beta-alanine. J. Biol. Chem., 279 (22): 23559-64. [PMID:15037633]
131. Shore DM, Reggio PH. (2015) The therapeutic potential of orphan GPCRs, GPR35 and GPR55. Front Pharmacol, 6: 69. [PMID:25926795]
132. Sikand P, Dong X, LaMotte RH. (2011) BAM8-22 peptide produces itch and nociceptive sensations in humans independent of histamine release. J. Neurosci., 31 (20): 7563-7. [PMID:21593341]
133. Solinski HJ, Gudermann T, Breit A. (2014) Pharmacology and signaling of MAS-related G protein-coupled receptors. Pharmacol. Rev., 66 (3): 570-97. [PMID:24867890]
134. Song H, Luo J, Luo W, Weng J, Wang Z, Li B, Li D, Liu M. (2008) Inactivation of G-protein-coupled receptor 48 (Gpr48/Lgr4) impairs definitive erythropoiesis at midgestation through down-regulation of the ATF4 signaling pathway. J. Biol. Chem., 283 (52): 36687-97. [PMID:18955481]
135. Southern C, Cook JM, Neetoo-Isseljee Z, Taylor DL, Kettleborough CA, Merritt A, Bassoni DL, Raab WJ, Quinn E, Wehrman TS et al.. (2013) Screening β-Arrestin Recruitment for the Identification of Natural Ligands for Orphan G-Protein-Coupled Receptors. J Biomol Screen, 18 (5): 599-609. [PMID:23396314]
136. Sugo T, Tachimoto H, Chikatsu T, Murakami Y, Kikukawa Y, Sato S, Kikuchi K, Nagi T, Harada M, Ogi K, Ebisawa M, Mori M. (2006) Identification of a lysophosphatidylserine receptor on mast cells. Biochem. Biophys. Res. Commun., 341 (4): 1078-87. [PMID:16460680]
137. Suzuki M, Takaishi S, Nagasaki M, Onozawa Y, Iino I, Maeda H, Komai T, Oda T. (2013) Medium-chain Fatty Acid-sensing Receptor, GPR84, Is a Proinflammatory Receptor. J. Biol. Chem., 288 (15): 10684-91. [PMID:23449982]
138. Tabata K, Baba K, Shiraishi A, Ito M, Fujita N. (2007) The orphan GPCR GPR87 was deorphanized and shown to be a lysophosphatidic acid receptor. Biochem. Biophys. Res. Commun., 363 (3): 861-6. [PMID:17905198]
139. Takeda S, Okada T, Okamura M, Haga T, Isoyama-Tanaka J, Kuwahara H, Minamino N. (2004) The receptor-Galpha fusion protein as a tool for ligand screening: a model study using a nociceptin receptor-Galphai2 fusion protein. J. Biochem., 135 (5): 597-604. [PMID:15173198]
140. Taniguchi Y, Tonai-Kachi H, Shinjo K. (2006) Zaprinast, a well-known cyclic guanosine monophosphate-specific phosphodiesterase inhibitor, is an agonist for GPR35. FEBS Lett., 580 (21): 5003-8. [PMID:16934253]
141. Thathiah A, Spittaels K, Hoffmann M, Staes M, Cohen A, Horré K, Vanbrabant M, Coun F, Baekelandt V, Delacourte A, Fischer DF, Pollet D, De Strooper B, Merchiers P. (2009) The orphan G protein-coupled receptor 3 modulates amyloid-beta peptide generation in neurons. Science, 323: 946-951. [PMID:19213921]
142. Tobo A, Tobo M, Nakakura T, Ebara M, Tomura H, Mogi C, Im DS, Murata N, Kuwabara A, Ito S et al.. (2015) Characterization of Imidazopyridine Compounds as Negative Allosteric Modulators of Proton-Sensing GPR4 in Extracellular Acidification-Induced Responses. PLoS ONE, 10 (6): e0129334. [PMID:26070068]
143. Toda N, Hao X, Ogawa Y, Oda K, Yu M, Fu Z, Chen Y, Kim Y, Lizarzaburu M, Lively S et al.. (2013) Potent and Orally Bioavailable GPR142 Agonists as Novel Insulin Secretagogues for the Treatment of Type 2 Diabetes. ACS Med Chem Lett, 4 (8): 790-4. [PMID:24900747]
144. Trivellin G, Daly AF, Faucz FR, Yuan B, Rostomyan L, Larco DO, Schernthaner-Reiter MH, Szarek E, Leal LF, Caberg JH et al.. (2014) Gigantism and acromegaly due to Xq26 microduplications and GPR101 mutation. N. Engl. J. Med., 371 (25): 2363-74. [PMID:25470569]
145. Uhlenbrock K, Gassenhuber H, Kostenis E. (2002) Sphingosine 1-phosphate is a ligand of the human gpr3, gpr6 and gpr12 family of constitutively active G protein-coupled receptors. Cell Signal, 14: 941-953. [PMID:12220620]
146. Valdes AM, Spector TD. (2010) The genetic epidemiology of osteoarthritis. Curr Opin Rheumatol, 22 (2): 139-43. [PMID:20090528]
147. Vanti WB, Muglia P, Nguyen T, Cheng R, Kennedy JL, George SR, O'Dowd BF. (2003) Discovery of a null mutation in a human trace amine receptor gene. Genomics, 82: 531-536. [PMID:14559210]
148. Wallrabenstein I, Kuklan J, Weber L, Zborala S, Werner M, Altmüller J, Becker C, Schmidt A, Hatt H, Hummel T et al.. (2013) Human trace amine-associated receptor TAAR5 can be activated by trimethylamine. PLoS ONE, 8 (2): e54950. [PMID:23393561]
149. Wang J, Simonavicius N, Wu X, Swaminath G, Reagan J, Tian H, Ling L. (2006) Kynurenic acid as a ligand for orphan G protein-coupled receptor GPR35. J. Biol. Chem., 281 (31): 22021-8. [PMID:16754668]
150. Wang J, Wu X, Simonavicius N, Tian H, Ling L. (2006) Medium-chain fatty acids as ligands for orphan G protein-coupled receptor GPR84. J. Biol. Chem., 281 (45): 34457-64. [PMID:16966319]
151. Weng J, Luo J, Cheng X, Jin C, Zhou X, Qu J, Tu L, Ai D, Li D, Wang J, Martin JF, Amendt BA, Liu M. (2008) Deletion of G protein-coupled receptor 48 leads to ocular anterior segment dysgenesis (ASD) through down-regulation of Pitx2. Proc. Natl. Acad. Sci. U.S.A., 105 (16): 6081-6. [PMID:18424556]
152. Witte ON, Kabarowski JH, Xu Y, Le LQ, Zhu K. (2005) Retraction. Science, 307 (5707): 206. [PMID:15653487]
153. Xu Y, Zhu K, Hong G, Wu W, Baudhuin LM, Xiao Y, Damron DS. (2000) Sphingosylphosphorylcholine is a ligand for ovarian cancer G-protein-coupled receptor 1. Nat. Cell Biol., 2 (5): 261-7. [PMID:10806476]
154. Yang LV, Radu CG, Roy M, Lee S, McLaughlin J, Teitell MA, Iruela-Arispe ML, Witte ON. (2007) Vascular abnormalities in mice deficient for the G protein-coupled receptor GPR4 that functions as a pH sensor. Mol. Cell. Biol., 27 (4): 1334-47. [PMID:17145776]
155. Yasuda H, Hirata S, Inoue K, Mashima H, Ohnishi H, Yoshiba M. (2007) Involvement of membrane-type bile acid receptor M-BAR/TGR5 in bile acid-induced activation of epidermal growth factor receptor and mitogen-activated protein kinases in gastric carcinoma cells. Biochem. Biophys. Res. Commun., 354 (1): 154-9. [PMID:17214962]
156. Ye C, Zhang Z, Wang Z, Hua Q, Zhang R, Xie X. (2014) Identification of a novel small-molecule agonist for human G protein-coupled receptor 3. J. Pharmacol. Exp. Ther., 349 (3): 437-43. [PMID:24633425]
157. Yin H, Chu A, Li W, Wang B, Shelton F, Otero F, Nguyen DG, Caldwell JS, Chen YA. (2009) Lipid G protein-coupled receptor ligand identification using beta-arrestin PathHunter assay. J Biol Chem, 284: 12328-12338. [PMID:19286662]
158. Yoshida S, Ohishi T, Matsui T, Shibasaki M. (2010) Identification of a novel GPR119 agonist, AS1269574, with in vitro and in vivo glucose-stimulated insulin secretion. Biochem. Biophys. Res. Commun., 400 (3): 437-41. [PMID:20804735]
159. Yosten GL, Kolar GR, Redlinger LJ, Samson WK. (2013) Evidence for an interaction between proinsulin C-peptide and GPR146. J. Endocrinol., 218 (2): B1-8. [PMID:23759446]
160. Yu M, Lizarzaburu M, Motani A, Fu Z, Du X, Liu JJ, Jiao X, Lai S, Fan P, Fu A et al.. (2013) Aminopyrazole-Phenylalanine Based GPR142 Agonists: Discovery of Tool Compound and in Vivo Efficacy Studies. ACS Med Chem Lett, 4 (9): 829-34. [PMID:24900757]
161. Zhang LL, Wang JJ, Liu Y, Lu XB, Kuang Y, Wan YH, Chen Y, Yan HM, Fei J, Wang ZG. (2011) GPR26-deficient mice display increased anxiety- and depression-like behaviors accompanied by reduced phosphorylated cyclic AMP responsive element-binding protein level in central amygdala. Neuroscience, 196: 203-14. [PMID:21924326]
162. Zhao P, Sharir H, Kapur A, Cowan A, Geller EB, Adler MW, Seltzman HH, Reggio PH, Heynen-Genel S, Sauer M, Chung TD, Bai Y, Chen W, Caron MG, Barak LS, Abood ME. (2010) Targeting of the orphan receptor GPR35 by pamoic acid: a potent activator of extracellular signal-regulated kinase and β-arrestin2 with antinociceptive activity. Mol. Pharmacol., 78 (4): 560-8. [PMID:20826425]
163. Zhu K, Baudhuin LM, Hong G, Williams FS, Cristina KL, Kabarowski JH, Witte ON, Xu Y. (2001) Sphingosylphosphorylcholine and lysophosphatidylcholine are ligands for the G protein-coupled receptor GPR4. J. Biol. Chem., 276 (44): 41325-35. [PMID:11535583]
164. (2006) Retraction. Sphingosylphosphorylcholine is a ligand for ovarian cancer G-protein-coupled receptor 1. Nat. Cell Biol., 8 (3): 299. [PMID:16508674]
Stephen P.H. Alexander
Jim Battey (BB3)
Helen E. Benson
Richard V. Benya (BB3)
Tom I. Bonner
Anthony P. Davenport
Khuraijam Dhanachandra Singh
Satoru Eguchi
Anthony Harmar
Nick Holliday
Robert T. Jensen (BB3)
Sadashiva Karnik (MAS1)
Evi Kostenis (GPR17)
Wen Chiy Liew
Amy E. Monaghan
Chido Mpamhanga
Richard Neubig
Adam J. Pawson
Jean-Philippe Pin
Joanna L. Sharman
Michael Spedding
Eliot Spindel (BB3)
Leigh Stoddart
Laura Storjohann (GPR39)
Walter G. Thomas
Kalyan Tirupula (MAS1)
Patrick Vanderheyden |
Database page citation (select format):
Concise Guide to PHARMACOLOGY citation:
Alexander SPH, Christopoulos A, Davenport AP, Kelly E, Mathie A, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Pawson AJ, Sharman JL, Southan C, Davies JA; CGTP Collaborators. (2019) The Concise Guide to PHARMACOLOGY 2019/20: G protein-coupled receptors. Br J Pharmacol. 176 Issue S1: S21-S141.
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