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GPR35

Family: Class A Orphans

This receptor has a proposed ligand; see the Latest Pairings page for more information.

Contents:
Gene and Protein Information
Previous and Unofficial Names
Database Links
Agonists
Tissue Distribution
Expression Datasets
Biologically Significant Variants
General Comments
References
Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 309 2q37.3 GPR35 G protein-coupled receptor 35
Mouse 7 307 1 D Gpr35 G protein-coupled receptor 35
Rat 7 306 9q36 Gpr35 G protein-coupled receptor 35
Previous and Unofficial Names
GPR35
G-protein coupled receptor 35
G protein-coupled receptor 35
Kynurenic acid receptor
KYNA receptor
G-protein coupled receptor 3
Gpr35_predicted
LOC367315
G protein-coupled receptor 35 (predicted)
Database Links
Ensembl ENSG00000178623 (Hs), ENSMUSG00000026271 (Mm), ENSRNOG00000024030 (Rn)
Entrez Gene 2859 (Hs), 64095 (Mm), 367315 (Rn)
GeneCards GPR35 (Hs)
GenitoUrinary Development Molecular Anatomy Project Gpr35 (Mm)
HomoloGene 3874 (Hs)
Human Protein Reference Database 16003 (Hs)
InterPro Q9HC97 (Hs), Q9ES90 (Mm), Q33BM1 (Rn)
KEGG Gene hsa:2859 (Hs), mmu:64095 (Mm), rno:367315 (Rn)
OMIM 602646 (Hs)
PharmGKB Gene PA28880 (Hs)
PhosphoSitePlus Q9HC97 (Hs), Q9ES90 (Mm)
Protein Ontology (PRO) PRO:000001531 (Hs)
RefSeq Nucleotide NM_005301 (Hs), NM_022320 (Mm), NM_001037359 (Rn)
RefSeq Protein NP_005292 (Hs), NP_071715 (Mm), NP_001032436 (Rn)
TreeFam ENSG00000178623 (Hs), ENSMUSG00000026271 (Mm), ENSRNOG00000024030 (Rn)
UniGene Hs. 239891 (Hs)
UniProt Q9HC97 (Hs), Q9ES90 (Mm), Q33BM1 (Rn)
Wikipedia GPR35
Orphan and other 7TM receptors
Natural/Endogenous Ligand(s)
2-oleoyl-LPA
kynurenic acid
Comments: Proposed ligands, single publications
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
zaprinast Rn Agonist 7.8 pEC50 5
LPA Hs Agonist 7.3 – 7.52 pEC50 4
pamoic acid Hs Agonist 7.29 pEC50 2
zaprinast Hs Agonist 6.1 pEC50 5
furosemide Hs Agonist 5.21 – 5.63 pEC50 7
bumetanide Hs Agonist 5.0 – 5.54 pEC50 7
kynurenic acid Rn Agonist 5.15 pEC50 6
kynurenic acid Mm Agonist 4.96 pEC50 6
kynurenic acid Hs Agonist 4.41 pEC50 6
pamoic acid Rn Agonist 3.0 – 5.0 pEC50 2
View species-specific agonist tables
Agonist Comments
2-acetyl -LPA (2-Oleoyl-LPA) is also proposed to be an endogenous ligand by a single publication [4]. The activity of the potential endogenous ligands is yet to be confirmed.
Tissue Distribution
peripheral leukocytes, spleen, small intestine, colon, stomach
Expression level:  High
Species:  Human
Technique:  qRT-PCR
References:  6
iNKT cells
Expression level:  High
Species:  Human
Technique:  semi-quantitative RT-PCR, immunoblottings, western blot, immunofluorescence,confocal microscopy
References:  1
duodenum, ileum,colon
Species:  Mouse
Technique:  in situ hybridisation
References:  6
spleen , gastrointestinal tract (duodenum, jejunum, ileum, cecum, colon, and rectum)
Expression level:  High
Species:  Mouse
Technique:  qRT-PCR
References:  6
Intestine.
Species:  Rat
Technique:  Northern blot.
References:  3
lung, stomach, small intestine, colon, skeletal muscle, uteru, brain, cerebrum, heart, liver, bladder, and spinal cord
Species:  Rat
Technique:  semi-quantitative RT-PCR
References:  5
Expression Datasets

Click here to show/hide data

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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Biologically Significant Variants
V76M, low frequency (<10% in all tested populations)
SNP accession:  rs13387859 
Type:  Naturally occurring SNPs.
Species:  Human
References: 
T108M
SNP accession:  rs3749171 
Type:  Naturally occurring SNPs.
Species:  Human
References: 
T253M
SNP accession:  rs12468485 
Type:  Naturally occurring SNPs.
Species:  Human
References: 
A25T, low frequency (<10% in all tested populations)
SNP accession:  rs35146537 
Type:  Naturally occurring SNPs.
Species:  Human
References: 
R125S, low frequency (<10% in all tested populations)
SNP accession:  rs34778053 
Type:  Naturally occurring SNPs.
Species:  Human
References: 
R294S
SNP accession:  rs3749172 
Type:  Naturally occurring SNPs.
Species:  Human
References: 
General Comments
Proposed ligand (kynurenic acid), supported by one publication [6].
Available Assays
DiscoveRx PathHunter® CHO-K1 GPR35 (Orphan) High Expression β-Arrestin Cell Line Human Cat No. 93-0355C2
DiscoveRx PathHunter® eXpress GPR35 CHO-K1 β-Arrestin (Orphan) GPCR Assay Human Cat No. 93-0355E2C2

REFERENCES

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1. Fallarini, S; Magliulo, L; Paoletti, T; de Lalla, C; Lombardi, G. (2010) Expression of functional GPR35 in human iNKT cells. Biochem. Biophys. Res. Commun., 398 (3): 420-5. [PMID:20599711]

2. Jenkins, L; Brea, J; Smith, NJ; Hudson, BD; Reilly, G; Bryant, NJ; Castro, M; Loza, MI; Milligan, G. (2010) Identification of novel, species selective agonists of the G protein-coupled receptor GPR35 that promote recruitment of β-arrestin-2 and activate Gα13. Biochem J,  [Epub ahead of print]. [PMID:20919992]

3. O'Dowd, B. F., Nguyen, T., Marchese, A., Cheng, R., Lynch, K. R., Heng, H. H., Kolakowski, L. F. and George, S. R. (1998) Discovery of three novel G-protein-coupled receptor genes. Genomics, 47: 310-313. [PMID:9479505]

4. Oka, S; Ota, R; Shima, M; Yamashita, A; Sugiura, T. (2010) GPR35 is a novel lysophosphatidic acid receptor. Biochem. Biophys. Res. Commun., 395 (2): 232-7. [PMID:20361937]

5. Taniguchi, Y; Tonai-Kachi, H; Shinjo, K. (2006) Zaprinast, a well-known cyclic guanosine monophosphate-specific phosphodiesterase inhibitor, is an agonist for GPR35. FEBS Lett., 580 (21): 5003-8. [PMID:16934253]

6. Wang, J; Simonavicius, N; Wu, X; Swaminath, G; Reagan, J; Tian, H; Ling, L. (2006) Kynurenic acid as a ligand for orphan G protein-coupled receptor GPR35. J. Biol. Chem., 281 (31): 22021-8. [PMID:16754668]

7. Yang, Y; Fu, A; Wu, X; Reagan, JD. (2012) GPR35 is a target of the loop diuretic drugs bumetanide and furosemide. Pharmacology, 89 (1-2): 13-7. [PMID:22236570]

To cite this database page, please use the following:

Chido Mpamhanga.
Class A Orphans: GPR35. Last modified on 13/12/2012. Accessed on 19/05/2013. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=102.


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