GPR35

G protein-coupled receptor 35

Identifiers

External IDs

OMIM: 602646 MGI: 1929509 HomoloGene: 3874 IUPHAR: 102 ChEMBL: 1293267 GeneCards: GPR35 Gene

Gene ontology
Molecular function	• G-protein coupled receptor activity
Cellular component	• integral component of plasma membrane
Biological process	• G-protein coupled receptor signaling pathway
Sources: Amigo / QuickGO

RNA expression pattern

More reference expression data

Orthologs

Species

Human

Mouse

RefSeq (mRNA)

RefSeq (protein)

Location (UCSC)

Chr 2:
240.61 – 240.63 Mb

Chr 1:
92.95 – 92.99 Mb

PubMed search

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

Agonists

Selective agonists of GPR35 include:

5-nitro-2-(3-phenylpropylamino) benzoic acid^[2]
Kynurenic acid^[2]^[3]
Lysophosphatidic acid^[2]
Pamoic acid^[2]
Zaprinast^[2]^[4]

Antagonists

Antagonists of GPR35 include:

ML145 (CID-2286812)^[5]
ML144 (CID-1542103)^[5]

Clinical significance

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

↑ 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.
1 2 3 4 5 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 2981393. PMID 20826425.
↑ 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
↑ 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.
1 2 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.
↑ 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.
↑ 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.

Cell surface receptor: G protein-coupled receptors

Class A: Rhodopsin like

Neurotransmitter

Adrenergic	α1 (A B D) α2 (A B C) β1 β2 β3

Purinergic	Adenosine (A1 A2A A2B A3) P2Y (1 2 4 5 6 8 9 10 11 12 13 14)

Serotonin	(all but 5-HT3) 5-HT1 (A B D E F) 5-HT2 (A B C) 5-HT (4 5A 6 7)

Other	Acetylcholine (M1 M2 M3 M4 M5) Dopamine (D1 D2 D3 D4 D5) Histamine (H1 H2 H3 H4) Melatonin (1A 1B 1C) TAAR (1 2 3 5 6 8 9)

Metabolites and
signaling molecules

Eicosanoid	CysLT (1 2) LTB4 (1 2) FPRL1 OXE Prostaglandin (DP (1 2), EP (1 2 3 4), FP) Prostacyclin Thromboxane

Other	Bile acid Cannabinoid (CB1 CB2, GPR (18 55 119)) EBI2 Estrogen Free fatty acid (1 2 3 4) Lactate Lysophosphatidic acid (1 2 3 4 5 6) Lysophospholipid (1 2 3 4 5 6 7 8) Niacin (1 2) Oxoglutarate PAF Sphingosine-1-phosphate (1 2 3 4 5) Succinate

Peptide

Neuropeptide	B/W (1 2) FF (1 2) S Y (1 2 4 5) Neuromedin (B U (1 2)) Neurotensin (1 2)

Other	Anaphylatoxin (C3a C5a) Angiotensin (1 2) Apelin Bombesin (BRS3 GRPR NMBR) Bradykinin (B1 B2) Chemokine Cholecystokinin (A B) Endothelin (A B) Formyl peptide (1 2 3) FSH Galanin (1 2 3) GHB receptor Gonadotropin-releasing hormone (1 2) Ghrelin Kisspeptin Luteinizing hormone/choriogonadotropin MAS (1 1L D E F G X1 X2 X3 X4) Melanocortin (1 2 3 4 5) MCHR (1 2) Motilin Opioid (Delta Kappa Mu Nociceptin & Zeta, but not Sigma) Orexin (1 2) Oxytocin Prokineticin (1 2) Prolactin-releasing peptide Relaxin (1 2 3 4) Somatostatin (1 2 3 4 5) Tachykinin (1 2 3) Thyrotropin Thyrotropin-releasing hormone Urotensin-II Vasopressin (1A 1B 2)

Miscellaneous

Orphan	GPR (1 3 4 6 12 15 17 18 19 20 21 22 23 25 26 27 31 32 33 34 35 37 39 42 44 45 50 52 55 61 62 63 65 68 75 77 78 81 82 83 84 85 87 88 92 101 103 109A 109B 119 120 132 135 137B 139 141 142 146 148 149 150 151 152 153 160 161 162 171 173 174 176 177 182 183)

Other	Adrenomedullin Olfactory Opsin (3 4 5 1LW 1MW 1SW RGR RRH) Protease-activated (1 2 3 4) SREB (1 2 3)

Class B: Secretin like

Adhesion	ADGRG (1 2 3 4 5 6 7)

Orphan	GPR (56 64 97 98 110 111 112 113 114 115 116 123 124 125 126 128 133 143 144 155 157)

Other	Brain-specific angiogenesis inhibitor (1 2 3) Cadherin (1 2 3) Calcitonin CALCRL CD97 Corticotropin-releasing hormone (1 2) EMR (1 2 3) Glucagon (GR GIPR GLP1R GLP2R) Growth hormone releasing hormone PACAPR1 GPR Latrophilin (1 2 3 ELTD1) Methuselah-like proteins Parathyroid hormone (1 2) Secretin Vasoactive intestinal peptide (1 2)

Class C: Metabotropic glutamate / pheromone

Taste	TAS1R (1 2 3) TAS2R (1 3 4 5 7 8 9 10 13 14 16 19 20 30 31 38 39 40 41 42 43 45 46 50 60)

Other	Calcium-sensing receptor GABA B (1 2) Glutamate receptor (Metabotropic glutamate (1 2 3 4 5 6 7 8)) GPRC6A GPR (156 158 179) RAIG (1 2 3 4)

Class F: Frizzled / Smoothened

Frizzled	Frizzled (1 2 3 4 5 6 7 8 9 10)

Smoothened	Smoothened

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