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

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GPR20

Target not currently curated in GtoImmuPdb

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

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
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
Treatment of cells with pertussis toxin
Species:  Human
Tissue:  HEK-293 cells
Response measured:  Increased basal and prostaglandin 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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