<i>GPR20</i> | Class A Orphans | IUPHAR/BPS Guide to PHARMACOLOGY

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GPR20

Target id: 91

Nomenclature: GPR20

Family: Class A Orphans

Annotation status:  image of a green circle Annotated and expert reviewed. Please contact us if you can help with updates.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for GPR20 in GtoImmuPdb

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 358 8q24.2-8q24.3 GPR20 G protein-coupled receptor 20 2
Mouse 7 358 15 D3 Gpr20 G protein-coupled receptor 20
Rat 7 353 7q34 Gpr20 G protein-coupled receptor 20
Previous and Unofficial Names
Gpcr5-1 | P2Y4 | G protein-coupled receptor 5-1
Database Links
Specialist databases
GPCRDB gpr20_human (Hs), gpr20_mouse (Mm), o35797_rat (Rn)
Other databases
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Primary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family Adenylate cyclase inhibition
Comments:  GPR20 constitutively activates Gi proteins without ligand stimulation as confirmed by RNA interference and mitogenic response assays [1]
References:  1
Tissue Distribution
Brain (thalamus, putamen, caudate), liver
Species:  Human
Technique:  Northern Blot
References:  2
Ubiquitous expression, highest expression small intestine (cell lines: U937, HL60, COLO320)
Species:  Human
Technique:  Real-time PCR
References:  1
Intestine, colon, spleen, testis, ovary (neuroblastoma cell line)
Species:  Mouse
Technique:  Real-time PCR
References:  1
Expression Datasets

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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
Treatment of cells with pertussis toxin
Species:  Human
Tissue:  HEK-293 cells
Response measured:  Increased basal and prostaglandin E2 induced cAMP production
References:  1
Disruption of conserved DRY motif by substitution of Asp for Ala at position 148
Species:  Human
Tissue:  HEK-293 cells
Response measured:  Attenuates [35S]GTPγS incorporation and inhibition of prostanglandin E2-induced cAMP production
References:  1
Physiological Functions Comments
Receptor may be involved in intracellular control of cAMP levels and mitogenic signalling [1]
Physiological Consequences of Altering Gene Expression
GPR20 overexpression causes increased [35S]GTPγS binding to membrane preparations
Species:  Human
Tissue:  HEK-293 cells
Technique:  Gene over-expression
References:  1
GPR20 deficient mice exhibit hyperactivity disorder characterised by increased total distance travelled in an open field test
Species:  Mouse
Tissue: 
Technique: 
References:  1
GPR20 knockdown causes elevated basal cAMP levels
Species:  Rat
Tissue:  PC12h cells
Technique:  RNAi
References:  1
Biologically Significant Variants
Type:  Single nucleotide polymorphism
Species:  Human
Amino acid change:  H230R
SNP accession: 
Type:  Single nucleotide polymorphism
Species:  Human
Amino acid change:  G313S
Global MAF (%):  5
Subpopulation MAF (%):  AFR|AMR|EUR: 12|7|4
Minor allele count:  T=0.054/119
SNP accession: 
Validation:  1000 Genomes, Frequency
Type:  Single nucleotide polymorphism
Species:  Human
Amino acid change:  R260C
Global MAF (%):  7
Subpopulation MAF (%):  AFR|AMR|EUR: 26|3|3
Minor allele count:  A=0.075/163
SNP accession: 
Validation:  1000 Genomes, Frequency

References

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1. 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]

2. O'Dowd BF, Nguyen T, Jung BP, Marchese A, Cheng R, Heng HH, Kolakowski LF, Lynch KR, George SR. (1997) Cloning and chromosomal mapping of four putative novel human G-protein-coupled receptor genes. Gene, 187 (1): 75-81. [PMID:9073069]

Contributors

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How to cite this page

Anthony P. Davenport, Stephen Alexander, Joanna L. Sharman, Adam J. Pawson, Helen E. Benson, Amy E. Monaghan, Wen Chiy Liew, Chido Mpamhanga, Jim Battey, Richard V. Benya, Robert T. Jensen, Sadashiva Karnik, Evi Kostenis, Eliot Spindel, Laura Storjohann, Kalyan Tirupula, Tom I. Bonner, Richard Neubig, Jean-Philippe Pin, Michael Spedding, Anthony Harmar.
Class A Orphans: GPR20. Last modified on 30/07/2015. Accessed on 21/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=91.