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- G protein-coupled receptors
- Class A Orphans
- Class A Orphans with emerging pharmacology
Class A Orphans with emerging pharmacology C
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).
Receptors
Targets of relevance to immunopharmacology are highlighted in blue
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GPR3 C
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GPR4
C
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GPR6 C
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GPR12 C
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GPR15
C
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GPR19 C
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GPR25 C
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GPR31 C
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GPR32 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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GPR61 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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GPR83 C
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GPR87 C
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GPR101 C
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GPR132 C
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GPR139 C
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GPR142 C
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GPR146 C
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GPR151 C
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GPR160 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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GPR183
C
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MAS1L C
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MRGPRD C
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MRGPRF C
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MRGPRX1 C
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MRGPRX2
C
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MRGPRX4 C
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P2RY8 C
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P2RY10 C
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References
1. 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]
2. 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]
3. 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]
4. 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]
5. 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 USA, 106 (22): 9075-80. [PMID:19451647]
6. 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]
7. 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]
8. 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]
9. 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]
10. 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 USA, 94 (26): 14742-7. [PMID:9405683]
11. 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]
12. 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]
13. 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 USA, 110 (40): 16211-6. [PMID:24043826]
14. 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]
15. 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]
16. 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]
17. 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]
18. 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]
19. 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]
20. 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]
21. 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]
22. 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]
23. 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]
24. 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]
25. 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]
26. 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]
27. 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]
28. 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]
29. 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]
30. 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]
31. 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]
32. 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]
33. 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]
34. 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 USA, 107 (4): 1660-5. [PMID:20080636]
35. 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]
36. 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]
37. 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]
38. 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 USA, 102 (25): 8922-6. [PMID:15956199]
39. Lees JA, Dias JM, Rajamohan F, Fortin JP, O'Connor R, Kong JX, Hughes EAG, Fisher EL, Tuttle JB, Lovett G et al.. (2023) An inverse agonist of orphan receptor GPR61 acts by a G protein-competitive allosteric mechanism. Nat Commun, 14 (1): 5938. [PMID:37741852]
40. 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]
41. 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]
42. 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]
43. Lindqvist A, Abels M, Shcherbina L, Ngara M, Kryvokhyzha D, Chriett S, Riva M, Fajul A, Barghouth M, Luan C et al.. (2023) GPR162 is a beta cell CART receptor. iScience, 26 (12): 108416. [PMID:38077141]
44. 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]
45. 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]
46. 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]
47. 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]
48. 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]
49. 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 USA, 104 (23): 9846-51. [PMID:17519329]
50. 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 USA, 110 (23): 9529-34. [PMID:23690594]
51. 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]
52. 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]
53. 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]
54. 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]
55. 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]
56. 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]
57. 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]
58. Padmanabhan S, Myers AG, Prasad BM. (2009) Constitutively active GPR6 is located in the intracellular compartments. FEBS Lett, 583 (1): 107-12. [PMID:19059244]
59. 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]
60. 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]
61. 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]
62. 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]
63. 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]
64. 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]
65. 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]
66. 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]
67. 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]
68. 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]
69. 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]
70. 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]
71. 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]
72. 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]
73. 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]
74. 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]
75. 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]
76. 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]
77. 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]
78. 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]
79. 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]
80. 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]
81. Witte ON, Kabarowski JH, Xu Y, Le LQ, Zhu K. (2005) Retraction. Science, 307 (5707): 206. [PMID:15653487]
82. Xia A, Yong X, Zhang C, Lin G, Jia G, Zhao C, Wang X, Hao Y, Wang Y, Zhou P et al.. (2023) Cryo-EM structures of human GPR34 enable the identification of selective antagonists. Proc Natl Acad Sci U S A, 120 (39): e2308435120. [PMID:37733739]
83. 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]
84. 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]
85. 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]
86. 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]
87. 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]
88. 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]
89. 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]
90. 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]
91. 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]
92. (2006) Retraction. Sphingosylphosphorylcholine is a ligand for ovarian cancer G-protein-coupled receptor 1. Nat Cell Biol, 8 (3): 299. [PMID:16508674]
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Class A Orphans with emerging pharmacology. Accessed on 18/06/2025. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=1113.
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Alexander SPH, Christopoulos A, Davenport AP, Kelly E, Mathie AA, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Davies JA et al. (2023) The Concise Guide to PHARMACOLOGY 2023/24: G protein-coupled receptors. Br J Pharmacol. 180 Suppl 2:S23-S144.
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