Putative Orphan G Protein-Coupled Receptors
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(Updated 08/09/07)

GPCRDB Link/
Receptors

Endogenous Ligand(s)

Articles

 GeneCard Link/
Amino Acids in Protein 		Swiss-Prot or TrEMBL Link/ Molecular Weight of Protein OMIM
Link/ Locus

Human
Homologues
GPR1   [An orphan G protein-coupled receptor, GPR1, acts as a coreceptor to allow replication of human immunodeficiency virus types 1 and 2 in brain-derived cells.] [Infection of mesangial cells with HIV and SIV: identification of GPR1 as a coreceptor.] [Senescence-associated genes in normal human oral keratinocytes.] 355 aa 41431 Da 2q33.3  
GPR2 (CCR10) CCL27 (SCYA27 or ESkine), SCYA28 [Identification of a novel chemokine (CCL28), which binds CCR10 (GPR2).] [Cutting edge: the orphan chemokine receptor G protein-coupled receptor-2 (GPR-2, CCR10) binds the skin-associated chemokine CCL27 (CTACK/ALP/ILC).] 362 aa

38416 Da

 17q21.1-q21.3
 Known chemokine receptors
GPR3 (ACCA) Sphingosine 1-phosphate (S1P), dihydrosphingosine 1-phosphate (DHS1P) [Molecular cloning of an orphan G-protein-coupled receptor that constitutively activates adenylate cyclase.] [Sphingosine 1-phosphate is a ligand of the human gpr3, gpr6 and gpr12 family of constitutively active G protein-coupled receptors.] [Molecular cloning and chromosomal localization of human genes encoding three closely related G protein-coupled receptors.] [Molecular cloning and chromosomal localization of human genes encoding three closely related G protein-coupled receptors.] 330 aa 35010 Da 1p36.1-p35
 GPR6 (60%), GPR12 (60%)
GPR4 Protons [Proton-sensing G-protein-coupled receptors.] 362 aa 40982 Da 19q13.2-q13.3 OGR1 (51%)
GPR5 (XCR1 or lymphotactin receptor) SCYC1 (lymphotactin), SCYC2 (XCL2) [Up-regulation of XCR1 expression in rheumatoid joints.] [Identification of single C motif-1/lymphotactin receptor XCR1.] 333 aa 38508 Da 3p21.3  
GPR6 Sphingosine 1-phosphate (S1P), dihydrosphingosine 1-phosphate (DHS1P) [Sphingosine 1-phosphate is a ligand of the human gpr3, gpr6 and gpr12 family of constitutively active G protein-coupled receptors.] [Molecular cloning and chromosomal localization of human genes encoding three closely related G protein-coupled receptors.] [Molecular cloning and chromosomal localization of human genes encoding three closely related G protein-coupled receptors.] 363 aa 37881 Da 6q21-q22.1 GPR3 (60%), GPR12 (60%)

GPR7 (NPBW1 or Neuropeptides B/W receptor type 1)

 Neuropeptide B, Neuropeptide W [The cloning and chromosomal mapping of two novel human opioid-somatostatin-like receptor genes, GPR7 and GPR8, expressed in discrete areas of the brain.] [G Protein Receptors (GPR) 7 and 8 are Expressed in Human Adrenocortical Cells, and their Endogenous Ligands Neuropeptides B and W Enhance Cortisol Secretion by Activating Adenylate Cyclase- and Phospholipase C-dependent Signaling Cascades.] 328 aa 36117 Da 8p22-q21.13 GPR8 (70%)

GPR8 (NPBW2 or Neuropeptides B/W receptor type 2)

 Neuropeptide B, Neuropeptide W [The cloning and chromosomal mapping of two novel human opioid-somatostatin-like receptor genes, GPR7 and GPR8, expressed in discrete areas of the brain.] [G Protein Receptors (GPR) 7 and 8 are Expressed in Human Adrenocortical Cells, and their Endogenous Ligands Neuropeptides B and W Enhance Cortisol Secretion by Activating Adenylate Cyclase- and Phospholipase C-dependent Signaling Cascades.] 333 aa 36903 Da 20q13.3 GPR7 (70%)
GPR9 (CXCR3) [Splice variants: CXCR3-A & CXCR3-B] CXCL9 (Mig), CXCL10 (IP-10), CXCL11 (I-TAC), CXCL4 (PF4) [The latter only exhibits high affinity for the CXCR3-B splice variant] [An alternatively spliced variant of CXCR3 mediates the inhibition of endothelial cell growth induced by IP-10, Mig, and I-TAC, and acts as functional receptor for platelet factor 4.] [CXCR3-binding chemokines: novel multifunctional therapeutic targets.] [Lymphocyte-specific chemokine receptor CXCR3: regulation, chemokine binding and gene localization.] 368 aa 40660 Da Xq13 IL8RB (38%, 53% TM), IL8RA (36%, 51% TM)
GPR10 (PrRPR or Prolactin-releasing peptide receptor) Prolactin-releasing peptide (PrRP) [Characterization of the binding of [(125)I]-human prolactin releasing peptide (PrRP) to GPR10, a novel G protein coupled receptor.] [Cloning and chromosomal mapping of three novel genes, GPR9, GPR10, and GPR14, encoding receptors related to interleukin 8, neuropeptide Y, and somatostatin receptors.] 370 aa 41107 Da 10q26.13 NPY1R (31%, 46% TM)
GPR11 (PAR2 or Proteinase-activated receptor 2) Trypsin and trypsin-like serine proteases [Proteinase-activated Receptor 2 (PAR2): a challenging new target for treatment of vascular diseases.] [Protease-Activated Receptors: New Concepts in Regulation of G Protein-Coupled Receptor Signaling and Trafficking] [International Union of Pharmacology. XXVIII. Proteinase-Activated Receptors]
397 aa 44126 Da 5q13  
GPR12 (GPCR21)

Sphingosylphosphorylcholine, Sphingosine 1-phosphate (S1P), dihydrosphingosine 1-phosphate (DHS1P)

[Role of the G-Protein-Coupled Receptor GPR12 as High-Affinity Receptor for Sphingosylphosphorylcholine and Its Expression and Function in Brain Development] [Sphingosine 1-phosphate is a ligand of the human gpr3, gpr6 and gpr12 family of constitutively active G protein-coupled receptors.] [Molecular cloning and chromosomal localization of human genes encoding three closely related G protein-coupled receptors.] [Molecular cloning and chromosomal localization of human genes encoding three closely related G protein-coupled receptors.]

334 aa 36730 Da 13q12 GPR3 (60%), GPR6 (60%)
GPR13 (CX3CR1) CX3CL1 (fractalkine)

[Fractalkine in vascular biology: from basic research to clinical disease.] [Two Novel Fully Functional Isoforms of CX3CR1 Are Potent HIV Coreceptors]

 355 aa 40396 Da 3p21.3 CCR1 (40%)
GPR14 (UTS2R or Urotensin II receptor) Urotensin II-related peptide, Urotensin II [Urotensin II-related peptide, the endogenous ligand for the urotensin II receptor in the rat brain.] [Architecture of the human urotensin II receptor: comparison of the binding domains of peptide and non-peptide urotensin II agonists.] 389 aa 42130 Da 17q25.3 SSTR4 (27%, 41% TM)
GPR15 (Bob)   [A novel human gene encoding a G-protein-coupled receptor (GPR15) is located on chromosome 3.] [ Gp120-induced Bob/GPR15 activation: a possible cause of human immunodeficiency virus enteropathy.] 360 aa 40787 Da 3q11.2-q13.1  
GPR16 (BLT1 or Leukotriene B4 receptor 1) Leukotriene B4 [International Union of Pharmacology XXXVII. Nomenclature for Leukotriene and Lipoxin Receptors] [Exploring the pharmacology of the leukotriene B4 receptor BLT1, without the confounding effects of BLT2.] 352 aa 37557 Da 14q11.2-q12
 BLT2 (45.2%)
GPR17   [A novel orphan G protein-coupled receptor primarily expressed in the brain is localized on human chromosomal band 2q21.] 367 aa 40989 Da 2q21  
GPR18   [Cloning and chromosomal localization of a gene (GPR18) encoding a novel seven transmembrane receptor highly expressed in spleen and testis.] 331 aa 38062 Da 13q32  
GPR19   [Physical mapping of the G-protein coupled receptor 19 (GPR19) in the chromosome 12p12.3 region frequently rearranged in cancer cells.] [The orphan G-protein-coupled receptor GPR19 is expressed predominantly in neuronal cells during mouse embryogenesis.] [Identification of signal transduction pathways used by orphan g protein-coupled receptors.] 415 aa 47701 Da 12p12.3  
GPR20   [Cloning and chromosomal mapping of four putative novel human G-protein-coupled receptor genes.] 358 aa 38406 Da 8q24.2-q24.3  
GPR21   [Cloning and chromosomal mapping of four putative novel human G-protein-coupled receptor genes.] [Identification of signal transduction pathways used by orphan g protein-coupled receptors.]
349 aa 39515 Da 9q33  
GPR22   [Cloning and chromosomal mapping of four putative novel human G-protein-coupled receptor genes.] 433 aa 49319 Da 7q22-q31.1  
GPR23 (LPA4) Lysophosphatidic acid [Identification of p2y9/GPR23 as a novel G protein-coupled receptor for lysophosphatidic acid, structurally distant from the Edg family.] [Cloning of a human heptahelical receptor closely related to the P2Y5 receptor.]
370 aa 41895 Da Xq13-q21.1  
GPR24 (MCH1) Melanin-concentrating hormone [Antidepressant, anxiolytic and anorectic effects of a melanin-concentrating hormone-1 receptor antagonist.] [Characterization of a human gene related to genes encoding somatostatin receptors.] 422 aa 45963 Da 22q13.2 All 5 SSTR receptors (40% TM)
GPR25   [Discovery of a novel human G protein-coupled receptor gene (GPR25) located on chromosome 1.] 361 aa 38779 Da 1q32.1 GPR15 (30%, 41% TM), AT2 (27%, 38% TM), SSTR5 (33%, 34 % TM)
GPR26   [Cloning and characterization of additional members of the G protein-coupled receptor family.] [Identification of signal transduction pathways used by orphan g protein-coupled receptors.] 337 aa 37604 Da 10q26.2-q26.3 GPR78 (56% TM)
GPR27   [Discovery of three novel G-protein-coupled receptor genes.] 375 aa 39818 Da 3p21-p14  
GPR28 (CCR9) CCL25 (TECK) [Cutting edge: identification of the orphan chemokine receptor GPR-9-6 as CCR9, the receptor for the chemokine TECK.] 357 aa 40713 Da 3p21.3  
GPR29 (CCR6) CCL20 (MIP-3alpha) [Molecular characterization of CCR6: involvement of multiple domains in ligand binding and receptor signaling.] 374 aa 42494 Da 6q27  
GPR30 17Beta-estradiol [A transmembrane intracellular estrogen receptor mediates rapid cell signaling.] [The G protein-coupled receptor GPR30 mediates c-fos up-regulation by 17beta-estradiol and phytoestrogens in breast cancer cells.] 375 aa 42248 Da 7p22  
GPR31   [Isolation and chromosomal localization of GPR31, a human gene encoding a putative G protein-coupled receptor.] 319 aa 35075 Da 6q27 GPR109B (33%)
GPR32   [Cloning genes encoding receptors related to chemoattractant receptors.] 356 aa 40087 Da 19q13.3  
GPR33   [GPR33 is a pseudogene]        
GPR34   [Discovery of three novel orphan G-protein-coupled receptors.] [A novel subgroup of class I G-protein-coupled receptors.] 381 aa 43860 Da Xp11.4-p11.3  
GPR35   [Discovery of three novel G-protein-coupled receptor genes.] [Cloning of a G-protein-coupled receptor that shows an activity to transform NIH3T3 cells and is expressed in gastric cancer cells.] 309 aa 34141 Da 2q37.3  
GPR37 (Parkin-associated endothelin-like receptor)   [Cloning of GPR37, a gene located on chromosome 7 encoding a putative G-protein-coupled peptide receptor, from a human frontal brain EST library.] [Altered dopamine signaling and MPTP resistance in mice lacking the Parkinson's disease-associated GPR37/parkin-associated endothelin-like receptor.] 613 aa 67114 Da 7q31 ETB (27%)
GPR37L1 (ETBR2)     481 aa 52829 Da 1q32.1  
GPR38 (MTLR1 or motilin receptor) [Splice variants exist: MTLR1A & MTLR1B] Motilin [Receptor for motilin identified in the human gastrointestinal system.] 412 aa 45344 Da 13q14-q21 GHSR (52%)
GPR39   [Cloning and characterization of two human G protein-coupled receptor genes (GPR38 and GPR39) related to the growth hormone secretagogue and neurotensin receptors.] [ Common structural basis for constitutive activity of the ghrelin receptor family.] 453 aa 51329 Da 2q21-q22
 NTS1 (32%), GHSR (27%)

GPR40 (FFAR1 or free fatty acid receptor 1)

 Medium and long chain fatty acids: docosahexaenoic acid (DHA), palmitate, oleate, stearate, linoleate, linolenate, etc. [Free fatty acids regulate insulin secretion from pancreatic beta cells through GPR40.] [The orphan G protein-coupled receptor GPR40 is activated by medium and long chain fatty acids.] [GPR40 gene Arg211His polymorphism may contribute to the variation of insulin secretory capacity in Japanese men.] 300 aa 31457 Da 19q13.1 GPR43 (28%)
GPR41 (FFAR3 or free fatty acid receptor 3) Short chain fatty acids: pentanoate, propionate, butyrate, isobutyrate, formate, etc.

[A cluster of four novel human G protein-coupled receptor genes occurring in close proximity to CD22 gene on chromosome 19q13.1.] [The Orphan G protein-coupled receptors GPR41 and GPR43 are activated by propionate and other short chain carboxylic acids.] [Short-chain fatty acids stimulate leptin production in adipocytes through the G protein-coupled receptor GPR41] [Functional characterization of human receptors for short chain fatty acids and their role in polymorphonuclear cell activation.]

 346 aa 38649 Da 19q13.1 GPR43 (43%), GPR42 (98%)
GPR42  

[A cluster of four novel human G protein-coupled receptor genes occurring in close proximity to CD22 gene on chromosome 19q13.1.] ["A third family member, GPR42, is most likely a recent gene duplication of GPR41 and may be a pseudogene."]

346 aa 38695 Da 19q13.1 GPR1 (98%)
GPR43 (FFAR2 or free fatty acid receptor 2) Short chain fatty acids: pentanoate, propionate, butyrate, isobutyrate, formate, etc. [A cluster of four novel human G protein-coupled receptor genes occurring in close proximity to CD22 gene on chromosome 19q13.1.] [The Orphan G protein-coupled receptors GPR41 and GPR43 are activated by propionate and other short chain carboxylic acids.] [Functional characterization of human receptors for short chain fatty acids and their role in polymorphonuclear cell activation.] 330 aa 37144 Da 19q13.1 GPR41 (43%), GPR40 (28%)
GPR44 (CRTH2) Prostaglandin D2 (PGD2), delta12-prostaglandin D2 (delta12-PGD2) [Discovery of three novel orphan G-protein-coupled receptors.] [The second PGD(2) receptor CRTH2: structure, properties, and functions in leukocytes.] [Cutting edge: agonistic effect of indomethacin on a prostaglandin D2 receptor, CRTH2.] [Delta12-prostaglandin D2 is a potent and selective CRTH2 receptor agonist and causes activation of human eosinophils and Th2 lymphocytes.] 395 aa 43240 Da 11q12-q13.3  
GPR45 (human PSP24 alpha)   [Discovery of three novel orphan G-protein-coupled receptors.] [Brain-specific expression of novel G-protein-coupled receptors, with homologies to Xenopus PSP24 and human GPR45.] 372 aa   2q11.1-q12 GPR63 (54%)
GPR48 (LGR4)   [Chromosomal localization of GPR48, a novel glycoprotein hormone receptor like GPCR, in human and mouse with radiation hybrid and interspecific backcross mapping.] [ Molecular characterization of a novel glycoprotein hormone G-protein-coupled receptor.] [Leucine-rich repeat-containing, G protein-coupled receptor 4 null mice exhibit intrauterine growth retardation associated with embryonic and perinatal lethality.] 951 aa [Length of unprocessed precursor] 104461 Da [MW of unprocessed precursor] 11p14-p13  
GPR49 (LGR5 or HG38)   [Identification and cloning of an orphan G protein-coupled receptor of the glycoprotein hormone receptor subfamily.] [Characterization of Two LGR Genes Homologous to Gonadotropin and Thyrotropin Receptors with Extracellular Leucine-Rich Repeats and a G Protein-Coupled, Seven-Transmembrane Region] [Overexpression of orphan G-protein-coupled receptor, Gpr49, in human hepatocellular carcinomas with beta-catenin mutations.] 907 aa [Length of unprocessed precursor]