<i>GPR182</i> | Class A Orphans | IUPHAR/BPS Guide to PHARMACOLOGY

GPR182

Target id: 146

Nomenclature: GPR182

Family: Class A Orphans

Annotation status:  image of a green circle Annotated and expert reviewed. Please contact us if you can help with updates.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for GPR182 in GtoImmuPdb

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 404 12q13.3 GPR182 G protein-coupled receptor 182 2
Mouse 7 395 10 Gpr182 G protein-coupled receptor 182
Rat 7 395 7q22 Gpr182 G protein-coupled receptor 182
Previous and Unofficial Names
ADMR | Gpcr22 | NOW | adrenomedullin receptor | L1-R [12] | Gpcr17
Database Links
Specialist databases
GPCRDB gp182_human (Hs), gp182_mouse (Mm), gp182_rat (Rn)
Other databases
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia

Download all structure-activity data for this target as a CSV file

Agonists
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Affinity Units Reference
adrenomedullin {Sp: Rat} Rn Partial agonist 8.1 pEC50 5
pEC50 8.1 (EC50 7x10-9 M) [5]
Agonist Comments
Rat GPR182 was first proposed as adrenomedullin receptor [5]. However, it was later reported that rat and human GPR182 did not respond to adrenomedullin [6].
Tissue Distribution
Pancreatic cancer cells
Species:  Human
Technique:  RT-PCR and Western blotting
References:  11
Human pancreatic stellate cells (HPSCs) and human umbilical vein endothelial cells (HUVECs)
Species:  Human
Technique:  RT-PCR
References:  11-12
High expression was detected in heart, skeletal muscle, liver, pancreas, stomach, spleen, lymph node, bone marrow, adrenal gland, thyroid. Low expression was detected in brain, lung, placenta, small intestine, thymus and leukocytes as well as fetal brain, lung, liver and kidney.
Species:  Human
Technique:  Northern blot
References:  2
Basal cells of the airway epithelium and Type II pneumocytes
Species:  Human
Technique:  in situ hybridisation
References:  8
Skin epithelium in both normal and malignant conditions
Species:  Human
Technique:  in situ hybridisation, immunohistochemistry and RT-PCR
References:  7
Lung, adrenal, ovary, heart, spleen, cerebellum and cerebral cortex
Species:  Human
Technique:  RT-PCR
References:  11-12
Brain, heart, lung, adrenal gland and some tumor cell lines
Species:  Human
Technique:  RT-PCR
References:  9
Mammary epithelial cells (luminal cells of ducts and alveoli, myoepithelial cells and cells comprising the terminal end bud), periductal fibroblasts
Species:  Mouse
Technique:  RT-PCR and in situ hybridisation
References:  3
Mouse primitive placenta (especially in the giant trophoblastic cells), maturing chondrocytes
Species:  Mouse
Technique:  In situ hybridisation
References:  10
Mouse lung endothelial cells (MLEC)
Species:  Mouse
Technique:  RT-PCR
References:  12
Lung, liver, heart, spleen and kidney. Not detected in extraembryonic tissues.
Species:  Mouse
Technique:  Northern blot
References:  13
Lung, liver, adrenal, kidney, aorta, heart, spinal cord, gut, testes and brain.
Species:  Rat
Technique:  Northern blot
References:  1
Rat embryonic tissue (whole embryo, placenta, yolk sac, heart, lung, liver, brain and gut)
Species:  Rat
Technique:  RT-PCR
References:  10
Prostate
Species:  Rat
Technique:  RT-PCR
References:  4
Tissue Distribution Comments
It is reported that the expression level of GPR182 in mouse embryonic tissue was low at 7 and 11 d.p.c, but drastically increased by 15 d.p.c. and stayed high until 17 d.p.c. [13]. In contrast to the previous report [10], Yotsumoto et al. did not detect the expression of GPR182 in the giant trophoblastic cells by Northern blot analyses [13]. It is found that the expression pattern of GPR182 in human tissue is considerably different from that of rat tissues [2].
Expression Datasets

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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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Physiological Functions
Mediate autocrine action of adrenomedullin in cell proliferation.
Species:  Human
Tissue:  Pancreatic cancer cell lines
References:  11
Physiological Consequences of Altering Gene Expression
SiRNA-mediated silencing of GPR182 reduces the cell growth.
Species:  Mouse
Tissue:  Mouse lung endothelial cells (MLEC)
Technique:  RNA interference
References:  12
SiRNA-mediated silencing of GPR182 abolishes adrenomedullin-mediated tube formation.
Species:  Mouse
Tissue:  Mouse lung endothelial cells (MLEC)
Technique:  RNA interference
References:  12
SiRNA-mediated silencing of GPR182 abolishes adrenomedullin-mediated tube formation.
Species:  Human
Tissue:  Human umbilical vein endothelial cells (HUVEC)
Technique:  RNA interference
References:  12
SiRNA-mediated silencing of GPR182 reduces the cell growth.
Species:  Human
Tissue:  Human pancreatic stellate cells (HPSC) and human umbilical vein endothelial cells (HUVEC)
Technique:  RNA interference
References:  12
SiRNA-mediated silencing of GPR182 strongly reduces tumour growth and metastasis in vivo.
Species:  Mouse
Tissue:  Lung and liver
Technique:  RNA interference
References:  12
Silencing of GPR182 inhibits basal- and adrenomedullin-induced growth and invasion in pancreatic cancer cells.
Species:  Human
Tissue:  Pancreatic cancer cells
Technique:  RNA interference
References:  11
SiRNA-mediated silencing of GPR182 reduces tumour growth and metastasis in vivo.
Species:  Human
Tissue:  Pancreatic cancer cells
Technique:  RNA interference
References:  12
Gene Expression and Pathophysiology Comments
It is proposed that adrenomedullin/GPR182 may involve in respiratory physiology and lung carcinogenesis [8].
Biologically Significant Variants
Type:  Single nucleotide polymorphism
Species:  Human
Amino acid change:  C349R
Global MAF (%):  13
Subpopulation MAF (%):  AFR|AMR|ASN|EUR: 13|12|17|11
Minor allele count:  C=0.132/288
SNP accession: 
Validation:  1000 Genomes, Frequency

References

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1. Harrison JK, Barber CM, Lynch KR. (1993) Molecular cloning of a novel rat G-protein-coupled receptor gene expressed prominently in lung, adrenal, and liver. FEBS Lett., 318 (1): 17-22. [PMID:8382168]

2. Hänze J, Dittrich K, Dötsch J, Rascher W. (1997) Molecular cloning of a novel human receptor gene with homology to the rat adrenomedullin receptor and high expression in heart and immune system. Biochem. Biophys. Res. Commun., 240 (1): 183-8. [PMID:9367907]

3. Jahnke GD, Miller MJ, Martínez A, Montuenga L, Cuttitta F. (1997) Adrenomedullin expression in the mouse mammary gland: evidence for the mature form in milk. J. Mol. Endocrinol., 19 (3): 279-89. [PMID:9460649]

4. Jiménez N, Calvo A, Martínez A, Rosell D, Cuttitta F, Montuenga LM. (1999) Expression of adrenomedullin and proadrenomedullin N-terminal 20 peptide in human and rat prostate. J. Histochem. Cytochem., 47 (9): 1167-78. [PMID:10449538]

5. Kapas S, Catt KJ, Clark AJ. (1995) Cloning and expression of cDNA encoding a rat adrenomedullin receptor. J. Biol. Chem., 270 (43): 25344-7. [PMID:7592696]

6. Kennedy SP, Sun D, Oleynek JJ, Hoth CF, Kong J, Hill RJ. (1998) Expression of the rat adrenomedullin receptor or a putative human adrenomedullin receptor does not correlate with adrenomedullin binding or functional response. Biochem Biophys Res Commun, 244: 832-837. [PMID:9535752]

7. Martínez A, Elsasser TH, Muro-Cacho C, Moody TW, Miller MJ, Macri CJ, Cuttitta F. (1997) Expression of adrenomedullin and its receptor in normal and malignant human skin: a potential pluripotent role in the integument. Endocrinology, 138 (12): 5597-604. [PMID:9389548]

8. Martínez A, Miller MJ, Catt KJ, Cuttitta F. (1997) Adrenomedullin receptor expression in human lung and in pulmonary tumors. J. Histochem. Cytochem., 45 (2): 159-64. [PMID:9016306]

9. Miller MJ, Martínez A, Unsworth EJ, Thiele CJ, Moody TW, Elsasser T, Cuttitta F. (1996) Adrenomedullin expression in human tumor cell lines. Its potential role as an autocrine growth factor. J. Biol. Chem., 271 (38): 23345-51. [PMID:8798536]

10. Montuenga LM, Martínez A, Miller MJ, Unsworth EJ, Cuttitta F. (1997) Expression of adrenomedullin and its receptor during embryogenesis suggests autocrine or paracrine modes of action. Endocrinology, 138 (1): 440-51. [PMID:8977434]

11. Ramachandran V, Arumugam T, Hwang RF, Greenson JK, Simeone DM, Logsdon CD. (2007) Adrenomedullin is expressed in pancreatic cancer and stimulates cell proliferation and invasion in an autocrine manner via the adrenomedullin receptor, ADMR. Cancer Res., 67 (6): 2666-75. [PMID:17363587]

12. Ramachandran V, Arumugam T, Langley R, Hwang RF, Vivas-Mejia P, Sood AK, Lopez-Berestein G, Logsdon CD. (2009) The ADMR receptor mediates the effects of adrenomedullin on pancreatic cancer cells and on cells of the tumor microenvironment. PLoS ONE, 4 (10): e7502. [PMID:19847298]

13. Yotsumoto S, Shimada T, Cui CY, Nakashima H, Fujiwara H, Ko MS. (1998) Expression of adrenomedullin, a hypotensive peptide, in the trophoblast giant cells at the embryo implantation site in mouse. Dev. Biol., 203 (2): 264-75. [PMID:9808778]

Contributors

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How to cite this page

Anthony P. Davenport, Stephen Alexander, Joanna L. Sharman, Adam J. Pawson, Helen E. Benson, Amy E. Monaghan, Wen Chiy Liew, Chido Mpamhanga, Jim Battey, Richard V. Benya, Robert T. Jensen, Sadashiva Karnik, Evi Kostenis, Eliot Spindel, Laura Storjohann, Kalyan Tirupula, Tom I. Bonner, Richard Neubig, Jean-Philippe Pin, Michael Spedding, Anthony Harmar.
Class A Orphans: GPR182. Last modified on 30/07/2015. Accessed on 18/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=146.