GPR35

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G protein-coupled receptor 35
Identifiers
Symbol GPR35
External IDs OMIM602646 MGI1929509 HomoloGene3874 IUPHAR: GPR35 ChEMBL: 1293267 GeneCards: GPR35 Gene
RNA expression pattern
PBB GE GPR35 210264 at tn.png
More reference expression data
Orthologs
Species Human Mouse
Entrez 2859 64095
Ensembl ENSG00000178623 ENSMUSG00000026271
UniProt Q9HC97 Q9ES90
RefSeq (mRNA) NM_001195381 NM_001104529
RefSeq (protein) NP_001182310 NP_001097999
Location (UCSC) Chr 2:
241.54 – 241.57 Mb
Chr 1:
92.97 – 92.99 Mb
PubMed search [1] [2]

G protein-coupled receptor 35 also known as GPR35 is a G protein-coupled receptor which in humans is encoded by the GPR35 gene.[1] 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)[5]
  • ML144 (CID-1542103)[5]

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.[6] In one study GPR35 has been recognised as a potential oncogene in stomach cancer.[7]

References[edit]

  1. ^ 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. 
  2. ^ 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). doi:10.1124/mol.110.066746. PMC 2981393. PMID 20826425. 
  3. ^ 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
  4. ^ 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. 
  5. ^ 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, and Lawrence S Barak (2010). "Selective GPR35 Antagonists - Probes 1 & 2". PMID 21433393. Bookshelf ID NBK50703. 
  6. ^ 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. 
  7. ^ 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.