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Target not currently curated in GtoImmuPdb

Target id: 194

Nomenclature: ADGRG5

Family: Adhesion Class GPCRs

Gene and Protein Information Click here for help
Adhesion G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 528 16q21 ADGRG5 adhesion G protein-coupled receptor G5
Mouse 7 524 8 C5 Adgrg5 adhesion G protein-coupled receptor G5
Rat 7 523 19p13 Adgrg5 adhesion G protein-coupled receptor G5
Previous and Unofficial Names Click here for help
Gm1109 | GPR114 (G protein-coupled receptor 114) | PGR27 | UNQ2524/PRO6017
Database Links Click here for help
Specialist databases
GPCRDB agrg5_human (Hs), agrg5_mouse (Mm)
Other databases
Ensembl Gene
Entrez Gene
Human Protein Atlas
RefSeq Nucleotide
RefSeq Protein
Agonist Comments
Peptides derived from the Stachel sequence: TYFAVLMQLSGDPVPAEL [8-9].
Antagonist Comments
Dihydromunduletone, a rotenoid derivative, is an antagonist at ADGRG5 [8].
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gs family
References:  5,8-9
Tissue Distribution Click here for help
Unigene expression profile highest in lymph node, bone marrow, tonsil, thymus, colon, pancreas.
Species:  Human
Colon, lung, spleen, thymus, pancreas islets of Langerhans, leukocytes, leukemia cells
Species:  Human
Technique:  EST
References:  1-3
Species:  Human
Technique:  Microarray analysis
References:  7
Unigene expression proifile highest in blood, spleen, inner ear, thymus.
Species:  Mouse
Expression Datasets Click here for help

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Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Functional Assays Click here for help
Elevated levels of cAMP
Species:  Human
Tissue:  293T cell line
Response measured:  Receptor causes constitutive activation of GαS G protein
References:  5
ADGRG5 couples to Gs protein.
Species:  Human
Tissue:  COS-7 cells.
Response measured:  Proximity luminescence (AlphaScreen assay), GTPγS binding
References:  8
General Comments
ADGRG5 (formerly GPR114) is an orphan receptor belonging to Family VIII Adhesion-GPCRs together with ADGRG1-4, 6 and 7 [3]. The genes of ADGRG1, ADGRG3 and ADGRG5 are syntenically clustered on human chromosome 16 and mouse chromosome 8 suggesting the evolution from an ancestral gene through gene duplication and exon shuffling [7]. Adgrg5 is mechano-sensitive and has two splice variants in mouse which significantly differ in their Gs-mediated basal activity [9].

Full coding sequence human cDNA is publicly available, IMAGE:5210813 [6], in mammalian expression vector pCMV-SPORT6.

Original human gene prediction, AY140956 [4] incorrectly predicts the 3' end of the gene resulting in a longer protein, (Swiss-Prot ID: Q8IZF4, 570 aa), than the observed cDNAs.


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1. Bjarnadóttir TK, Fredriksson R, Höglund PJ, Gloriam DE, Lagerström MC, Schiöth HB. (2004) The human and mouse repertoire of the adhesion family of G-protein-coupled receptors. Genomics, 84 (1): 23-33. [PMID:15203201]

2. Bjarnadóttir TK, Geirardsdóttir K, Ingemansson M, Mirza MA, Fredriksson R, Schiöth HB. (2007) Identification of novel splice variants of Adhesion G protein-coupled receptors. Gene, 387 (1-2): 38-48. [PMID:17056209]

3. Fredriksson R, Gloriam DE, Höglund PJ, Lagerström MC, Schiöth HB. (2003) There exist at least 30 human G-protein-coupled receptors with long Ser/Thr-rich N-termini. Biochem. Biophys. Res. Commun., 301 (3): 725-34. [PMID:12565841]

4. Fredriksson R, Lagerström MC, Höglund PJ, Schiöth HB. (2002) Novel human G protein-coupled receptors with long N-terminals containing GPS domains and Ser/Thr-rich regions. FEBS Lett., 531 (3): 407-14. [PMID:12435584]

5. Gupte J, Swaminath G, Danao J, Tian H, Li Y, Wu X. (2012) Signaling property study of adhesion G-protein-coupled receptors. FEBS Lett., 586 (8): 1214-9. [PMID:22575658]

6. Lennon G, Auffray C, Polymeropoulos M, Soares MB. (1996) The I.M.A.G.E. Consortium: an integrated molecular analysis of genomes and their expression. Genomics, 33 (1): 151-2. [PMID:8617505]

7. Peng YM, van de Garde MD, Cheng KF, Baars PA, Remmerswaal EB, van Lier RA, Mackay CR, Lin HH, Hamann J. (2011) Specific expression of GPR56 by human cytotoxic lymphocytes. J. Leukoc. Biol., 90 (4): 735-40. [PMID:21724806]

8. Stoveken HM, Bahr LL, Anders MW, Wojtovich AP, Smrcka AV, Tall GG. (2016) Dihydromunduletone Is a Small-Molecule Selective Adhesion G Protein-Coupled Receptor Antagonist. Mol. Pharmacol., 90 (3): 214-24. [PMID:27338081]

9. Wilde C, Fischer L, Lede V, Kirchberger J, Rothemund S, Schöneberg T, Liebscher I. (2016) The constitutive activity of the adhesion GPCR GPR114/ADGRG5 is mediated by its tethered agonist. FASEB J., 30 (2): 666-73. [PMID:26499266]


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