GPR35

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GPR35
Identifiers
Aliases GPR35
External IDs MGI: 1929509 HomoloGene: 3874 GeneCards: GPR35
Genetically Related Diseases
inflammatory bowel disease, ulcerative colitis, sclerosing cholangitis[1]
Targeted by Drug
bumetanide, furosemide, kynurenic acid, pamoic acid, zaprinast[2]
RNA expression pattern
PBB GE GPR35 210264 at tn.png
More reference expression data
Orthologs
Species Human Mouse
Entrez
Ensembl
UniProt
RefSeq (mRNA)

NM_005301
NM_001195381
NM_001195382

NM_001104529
NM_001271766
NM_022320

RefSeq (protein)

NP_001182310
NP_001182311
NP_005292

NP_001097999.1
NP_001258695.1
NP_071715.3

Location (UCSC) Chr 2: 240.61 – 240.63 Mb Chr 1: 92.95 – 92.99 Mb
PubMed search [3] [4]
Wikidata
View/Edit Human View/Edit Mouse

G protein-coupled receptor 35 also known as GPR35 is a G protein-coupled receptor which in humans is encoded by the GPR35 gene.[5] Heightened expression of GPR35 is found in immune and gastrointestinal tissues, including the crypts of Lieberkühn.

Ligands[edit]

Agonists[edit]

Selective agonists of GPR35 include:

Antagonists[edit]

Antagonists of GPR35 include:

  • ML145 (CID-2286812)[9]
  • ML144 (CID-1542103)[9]

Clinical significance[edit]

Deletion of GPR35 gene may be responsible for brachydactyly mental retardation syndrome and is mutated in 2q37 monosomy and 2q37 deletion syndrome.[10] In one study GPR35 has been recognised as a potential oncogene in stomach cancer.[11]

References[edit]

  1. ^ "Diseases that are genetically associated with GPR35 view/edit references on wikidata". 
  2. ^ "Drugs that physically interact with G protein-coupled receptor 35 view/edit references on wikidata". 
  3. ^ "Human PubMed Reference:". 
  4. ^ "Mouse PubMed Reference:". 
  5. ^ O'Dowd BF, Nguyen T, Marchese A, Cheng R, Lynch KR, Heng HH, Kolakowski LF, George SR (1998). "Discovery of three novel G-protein-coupled receptor genes". Genomics. 47 (2): 310–3. doi:10.1006/geno.1998.5095. PMID 9479505. 
  6. ^ a b c d e Zhao, Pingwei; Sharir, Haleli; Kapur, Ankur; Cowan, Alan; Geller, Ellen B; Adler, Martin W; Seltzman, Herbert H; Reggio, Patricia H; Heynen-Genel, Susanne; Sauer, Michelle; Chung, Thomas D Y; Bai, Yushi; Chen, Wei; Caron, Marc G; Barak, Larry S; Abood, Mary E (2010). "Targeting of the orphan receptor GPR35 by pamoic acid: a potent activator of extracellular signal-regulated kinase and β-arrestin2 with antinociceptive activity.". Molecular Pharmacology. 78 (4): 560–568. doi:10.1124/mol.110.066746. PMC 2981393Freely accessible. PMID 20826425. 
  7. ^ 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. doi:10.1074/jbc.M603503200. PMID 16754668. free fulltext
  8. ^ 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. doi:10.1016/j.febslet.2006.08.015. PMID 16934253. 
  9. ^ a b Susanne Heynen-Genel; Russell Dahl; Shenghua Shi; Michelle Sauer; Santosh Hariharan; Eduard Sergienko; Shakeela Dad; Thomas DY Chung; Derek Stonich; Ying Su; Marc Caron; Pingwei Zhao; Mary E Abood; Lawrence S Barak (2010). "Selective GPR35 Antagonists - Probes 1 & 2". PMID 21433393. Bookshelf ID NBK50703. 
  10. ^ Shrimpton AE, Braddock BR, Thomson LL, Stein CK, Hoo JJ (2004). "Molecular delineation of deletions on 2q37.3 in three cases with an Albright hereditary osteodystrophy-like phenotype". Clin. Genet. 66 (6): 537–44. doi:10.1111/j.1399-0004.2004.00363.x. PMID 15521982. 
  11. ^ Okumura S, Baba H, Kumada T, Nanmoku K, Nakajima H, Nakane Y, Hioki K, Ikenaka K (2004). "Cloning of a G-protein-coupled receptor that shows an activity to transform NIH3T3 cells and is expressed in gastric cancer cells". Cancer Sci. 95 (2): 131–5. doi:10.1111/j.1349-7006.2004.tb03193.x. PMID 14965362.