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MCH2 receptor

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Target not currently curated in GtoImmuPdb

Target id: 281

Nomenclature: MCH2 receptor

Family: Melanin-concentrating hormone receptors

Contents:

Gene and Protein Information Click here for help
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 340 6q16.2 MCHR2 melanin concentrating hormone receptor 2 1,6,12-13
Gene and Protein Information Comments
MCHR2 genes have been identified in Xenopus [7], goldfish [11], flounder [15], zebrafish [9] and shark [10].
Previous and Unofficial Names Click here for help
GPR145 | GPRv17 | MCH2R | G protein-coupled receptor 145 | melanin-concentrating hormone receptor 2
Database Links Click here for help
Specialist databases
GPCRdb mchr2_human (Hs)
Other databases
Alphafold Q969V1 (Hs)
ChEMBL Target CHEMBL5038 (Hs)
Ensembl Gene ENSG00000152034 (Hs)
Entrez Gene 84539 (Hs)
Human Protein Atlas ENSG00000152034 (Hs)
KEGG Gene hsa:84539 (Hs)
OMIM 606111 (Hs)
Pharos Q969V1 (Hs)
RefSeq Nucleotide NM_032503 (Hs), NM_001040179 (Hs)
RefSeq Protein NP_115892 (Hs), NP_001035269 (Hs)
UniProtKB Q969V1 (Hs)
Wikipedia MCHR2 (Hs)
Natural/Endogenous Ligands Click here for help
melanin-concentrating hormone {Sp: Human, Mouse, Rat}

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Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[Phe13,Tyr19]MCH Peptide Click here for species-specific activity table Hs Full agonist 8.4 – 9.2 pIC50 14,16
⤷ pIC50 8.4 – 9.2 [14,16]
melanin-concentrating hormone {Sp: Human, Mouse, Rat} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Hs Full agonist 8.2 – 9.2 pIC50 14
⤷ pIC50 8.2 – 9.2 [14]
Ac-hMCH-(6-16)-NH2 Peptide Click here for species-specific activity table Hs Full agonist 8.4 – 8.8 pIC50 2
⤷ pIC50 8.4 – 8.8 [2]
MCH (salmon) Peptide Click here for species-specific activity table Hs Full agonist 6.2 – 7.1 pIC50 14,16
⤷ pIC50 6.2 – 7.1 [14,16]
Agonist Comments
Ligand rank potency: melanin-concentrating hormone = MCH (salmon) [6]
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 38 [PMID: 22123324] Small molecule or natural product Primary target of this compound Hs Antagonist 9.0 pIC50 4
⤷ pIC50 9.0 (IC50 1x10-9 M) [4]
[Ava9,10,Ava14,15]-Ac-hMCH6-16-NH2 Peptide Click here for species-specific activity table Hs Antagonist 7.3 pIC50 2
⤷ pIC50 7.3 [2]
ATC0065 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.8 – 5.9 pIC50 3
⤷ pIC50 5.8 – 5.9 [3]
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gq/G11 family Adenylyl cyclase inhibition
Phospholipase C stimulation
References:  14
Tissue Distribution Click here for help
Brain; frontal lobe, temporal lobe, occipital lobe, precentral gyrus, pons, hippocampus, amygdala, putamen, and the caudate nucleus, with relatively high levels in the cerebral cortex > thalamus, corpus callosum, and medulla oblongata.

Hypothalamus, adipocytes, pituitary, and pancreas.
Species:  Human
Technique:  RT-PCR, Northern hybridization and RNA dot array blot hybridization.
References:  1
Brain; arcuate nucleus and ventral medial hypothalamus.
Species:  Human
Technique:  Northern Blot and in situ hybridization.
References:  14
Brain (cortex, occipital lobe, frontal lobe, temporal lobe, parietal lobe, paracentral gyrus, cerebellum, amygdala, hippocampus, accumbens nucleus, thalamus).
Species:  Human
Technique:  Northern and dot blot.
References:  16
Brain > adipose tissue > prostate, lymphocytes, intestine. Cingulate gyrus > nucleus accumbens > medial frontal gyrus > superior frontal gyrus.
Species:  Human
Technique:  Quantitative RT-PCR.
References:  6
Brain (temporal lobe, cerebral cortex > hippocampus, parietal lobe, amygdala, corpus callosum, occipital lobe, frontal lobe, caudate nucleus) > tetis.
Species:  Human
Technique:  Quantitative RT-PCR.
References:  12-13
Hypothalamus (paraventricular nucleus (magnocellular part), dorsomedial, ventromedial, and arcuate nucleus), olfactory pathway, nucleus of the solitary tract.

Thyroid, kidney, lung, testis.
Species:  Mouse
Technique:  in situ hybridization.
References:  8
Functional Assays Click here for help
Measurement of IP3 production in CHO cells transfected with the human NCH2 receptors.
Species:  Human
Tissue:  CHO cells.
Response measured:  Stimulation of IP3 production.
References:  14,16
Measurement of intracellular Ca2+ levels in CHO cells transfected with the human MCH2 receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Increase in intracellular Ca2+.
References:  13-14,16
Measurement of intracellular Ca2+ levels in HEK 293 cells transfected with the human MCH2 receptor.
Species:  Human
Tissue:  HEK 293 cells.
Response measured:  Increase in intracellular Ca2+.
References:  6,14
Measurement of cellular extrusion of protons in HEK 293 cells transfected with the human MHC2 receptor.
Species:  Human
Tissue:  HEK 293 cells.
Response measured:  Increase in cellular extrusion of protons.
References:  6
Measurement of inositol phosphate turnover.
Species:  Human
Tissue: 
Response measured:  Stimulation of inositol phosphate turnover.
References:  14
Functional Assay Comments
Levels of cAMP accumulation, Ca2+ mobilisation and ERK phosphorylation for exogenously expressed goldfish MCH2 receptors have been measured [5]. Ca2+ mobilisation has been measured in exogenously expressed Xenopus [7] and flounder [15] MCH2 receptors.

References

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1. An S, Cutler G, Zhao JJ, Huang SG, Tian H, Li W, Liang L, Rich M, Bakleh A, Du J et al.. (2001) Identification and characterization of a melanin-concentrating hormone receptor. Proc Natl Acad Sci USA, 98 (13): 7576-81. [PMID:11416225]

2. Bednarek MA, Hreniuk DL, Tan C, Palyha OC, MacNeil DJ, Van der Ploeg LH, Howard AD, Feighner SD. (2002) Synthesis and biological evaluation in vitro of selective, high affinity peptide antagonists of human melanin-concentrating hormone action at human melanin-concentrating hormone receptor 1. Biochemistry, 41 (20): 6383-90. [PMID:12009900]

3. Chaki S, Funakoshi T, Hirota-Okuno S, Nishiguchi M, Shimazaki T, Iijima M, Grottick AJ, Kanuma K, Omodera K, Sekiguchi Y, Okuyama S, Tran TA, Semple G, Thomsen W. (2005) Anxiolytic- and antidepressant-like profile of ATC0065 and ATC0175: nonpeptidic and orally active melanin-concentrating hormone receptor 1 antagonists. J Pharmacol Exp Ther, 313: 831-839. [PMID:15677346]

4. Chen X, Mihalic J, Fan P, Liang L, Lindstrom M, Wong S, Ye Q, Fu Y, Jaen J, Chen JL et al.. (2012) Discovery and characterization of a potent and selective antagonist of melanin-concentrating hormone receptor 2. Bioorg Med Chem Lett, 22 (1): 363-6. [PMID:22123324]

5. Hamamoto A, Mizusawa K, Takahashi A, Saito Y. (2011) Signalling pathway of goldfish melanin-concentrating hormone receptors 1 and 2. Regul Pept, 169 (1-3): 6-12. [PMID:21539863]

6. Hill J, Duckworth M, Murdock P, Rennie G, Sabido-David C, Ames RS, Szekeres P, Wilson S, Bergsma DJ, Gloger IS et al.. (2001) Molecular cloning and functional characterization of MCH2, a novel human MCH receptor. J Biol Chem, 276 (23): 20125-9. [PMID:11274220]

7. Kobayashi Y, Hamamoto A, Hirayama T, Saito Y. (2015) Molecular cloning, expression, and signaling pathway of four melanin-concentrating hormone receptors from Xenopus tropicalis. Gen Comp Endocrinol, 212: 114-23. [PMID:24662390]

8. Kokkotou EG, Tritos NA, Mastaitis JW, Slieker L, Maratos-Flier E. (2001) Melanin-concentrating hormone receptor is a target of leptin action in the mouse brain. Endocrinology, 142 (2): 680-6. [PMID:11159839]

9. Logan DW, Bryson-Richardson RJ, Pagán KE, Taylor MS, Currie PD, Jackson IJ. (2003) The structure and evolution of the melanocortin and MCH receptors in fish and mammals. Genomics, 81 (2): 184-91. [PMID:12620396]

10. Mizusawa K, Amiya N, Yamaguchi Y, Takabe S, Amano M, Breves JP, Fox BK, Grau EG, Hyodo S, Takahashi A. (2012) Identification of mRNAs coding for mammalian-type melanin-concentrating hormone and its receptors in the scalloped hammerhead shark Sphyrna lewini. Gen Comp Endocrinol, 179 (1): 78-87. [PMID:22884735]

11. Mizusawa K, Saito Y, Wang Z, Kobayashi Y, Matsuda K, Takahashi A. (2009) Molecular cloning and expression of two melanin-concentrating hormone receptors in goldfish. Peptides, 30 (11): 1990-6. [PMID:19397943]

12. Mori M, Harada M, Terao Y, Sugo T, Watanabe T, Shimomura Y, Abe M, Shintani Y, Onda H, Nishimura O et al.. (2001) Cloning of a novel G protein-coupled receptor, SLT, a subtype of the melanin-concentrating hormone receptor. Biochem Biophys Res Commun, 283 (5): 1013-8. [PMID:11355873]

13. Rodriguez M, Beauverger P, Naime I, Rique H, Ouvry C, Souchaud S, Dromaint S, Nagel N, Suply T, Audinot V et al.. (2001) Cloning and molecular characterization of the novel human melanin-concentrating hormone receptor MCH2. Mol Pharmacol, 60 (4): 632-9. [PMID:11562423]

14. Sailer AW, Sano H, Zeng Z, McDonald TP, Pan J, Pong SS, Feighner SD, Tan CP, Fukami T, Iwaasa H et al.. (2001) Identification and characterization of a second melanin-concentrating hormone receptor, MCH-2R. Proc Natl Acad Sci USA, 98 (13): 7564-9. [PMID:11404457]

15. Takahashi A, Kosugi T, Kobayashi Y, Yamanome T, Schiöth HB, Kawauchi H. (2007) The melanin-concentrating hormone receptor 2 (MCH-R2) mediates the effect of MCH to control body color for background adaptation in the barfin flounder. Gen Comp Endocrinol, 151 (2): 210-9. [PMID:17324419]

16. Wang S, Behan J, O'Neill K, Weig B, Fried S, Laz T, Bayne M, Gustafson E, Hawes BE. (2001) Identification and pharmacological characterization of a novel human melanin-concentrating hormone receptor, mch-r2. J Biol Chem, 276 (37): 34664-70. [PMID:11459838]

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