Gene and Protein Information
class A G protein-coupled receptor
Species	TM	AA	Chromosomal Location	Gene Symbol	Gene Name	Reference
Human	7	358	8q24.3	GPR20	G protein-coupled receptor 20	4
Mouse	7	358	15 D3	Gpr20	G protein-coupled receptor 20
Rat	6	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
Alphafold	Q99678 (Hs), Q8BYC4 (Mm), O35797 (Rn)
ChEMBL Target	CHEMBL4523912 (Hs)
Ensembl Gene	ENSG00000204882 (Hs), ENSMUSG00000045281 (Mm), ENSRNOG00000007795 (Rn)
Entrez Gene	2843 (Hs), 239530 (Mm), 60667 (Rn)
Human Protein Atlas	ENSG00000204882 (Hs)
KEGG Gene	hsa:2843 (Hs), mmu:239530 (Mm), rno:60667 (Rn)
OMIM	601908 (Hs)
Pharos	Q99678 (Hs)
RefSeq Nucleotide	NM_005293 (Hs), NM_173365 (Mm), NM_022216 (Rn)
RefSeq Protein	NP_005284 (Hs), NP_775541 (Mm), NP_071552 (Rn)
UniProtKB	Q99678 (Hs), Q8BYC4 (Mm), O35797 (Rn)
Wikipedia	GPR20 (Hs)

Antibody Comments

Based on evidence of GPR20's selective expression in gastrointestinal stromal tumours (GISTs), Daiichi Sankyo developed an anti-GPR20 antibody drug conjugate (DS-6157a) to deliver a derivative of the cytotoxic DNA topoisomerase I inhibitor exatecan to tumours [2]. DS-6157a was intended as an alternative to tyrosine kinase inhibitor class GIST therapeutics. Clinical development was discontinued in late 2021, following failure of DS-6157a treatment to demonstrate efficacy in a phase 1 study (NCT04276415) in patients with advanced GIST.

Primary Transduction Mechanisms
Transducer	Effector/Response
Gi/Go family
Comments:  GPR20 constitutively activates Gi proteins without ligand stimulation as confirmed by RNA interference and mitogenic response assays [1]
References:  1,3

Tissue Distribution
Brain (thalamus, putamen, caudate), liver Species:  Human Technique:  Northern Blot References:  4
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
Show »« Hide 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] There should be a chart of expression data here, you may need to enable JavaScript!

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 knockdown causes elevated basal cAMP levels Species:  Rat Tissue:  PC12h cells Technique:  RNAi 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

Biologically Significant Variants
Type:  Single nucleotide polymorphism Species:  Human Amino acid change:  H230R SNP accession:  rs10875472
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:  VAR_055919, rs34591516 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:  VAR_055918, rs36092215 Validation:  1000 Genomes, Frequency