Biology:Melanin-concentrating hormone receptor 1
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Short description: Protein-coding gene in the species Homo sapiens
 Generic protein structure example |
Melanin-concentrating hormone receptor 1, also known as MCH1, is one of the melanin-concentrating hormone receptors found in all mammals.[1]
The protein encoded by this gene, a member of the G protein-coupled receptor family 1, is an integral plasma membrane protein which binds melanin-concentrating hormone. The encoded protein can inhibit cAMP accumulation and stimulate intracellular calcium flux, and is probably involved in the neuronal regulation of food consumption. Although structurally similar to somatostatin receptors, this protein does not seem to bind somatostatin.[1]
Function
MCH1 is thought to have a number of functions including in the regulation of appetite,[2][3] and in stress, anxiety and depression.[4][5][6][7][8][9]
Selective ligands
Agonists
- Melanin concentrating hormone (MCH)
- S-36057 - modified MCH 6-13 fragment substituted with 3-iodotyrosine at N-terminus via dioxyoctanoyl linker, used as 125I radioligand for mapping MCH1 in vivo.[10][11]
- LK-184 (Procter & Gamble) is one pick[12]
Antagonists
See also
References
- ↑ 1.0 1.1 "Entrez Gene: MCHR1 melanin-concentrating hormone receptor 1". https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=2847.
- ↑ "Anti-obesity effects of small molecule melanin-concentrating hormone receptor 1 (MCHR1) antagonists". Life Sciences 81 (6): 423–40. Jul 2007. doi:10.1016/j.lfs.2007.05.029. PMID 17655875.
- ↑ "Melanin-concentrating hormone receptor 1 antagonists: a new perspective for the pharmacologic treatment of obesity". Current Medicinal Chemistry 15 (10): 1025–43. 2008. doi:10.2174/092986708784049621. PMID 18393860.
- ↑ "Melanin-concentrating hormone functions in the nervous system: food intake and stress". Expert Opinion on Therapeutic Targets 7 (4): 495–511. Aug 2003. doi:10.1517/14728222.7.4.495. PMID 12885269.
- ↑ "Melanin-concentrating hormone MCH1 receptor antagonists: a potential new approach to the treatment of depression and anxiety disorders". CNS Drugs 20 (10): 801–11. 2006. doi:10.2165/00023210-200620100-00002. PMID 16999451.
- ↑ "Further insights into the neurobiology of melanin-concentrating hormone in energy and mood balances". Expert Opinion on Therapeutic Targets 10 (2): 211–29. Apr 2006. doi:10.1517/14728222.10.2.211. PMID 16548771.
- ↑ "Melanin-concentrating hormone-1 receptor modulates neuroendocrine, behavioral, and corticolimbic neurochemical stress responses in mice". Neuropsychopharmacology 31 (6): 1135–45. Jun 2006. doi:10.1038/sj.npp.1300913. PMID 16205780.
- ↑ "A study of the involvement of melanin-concentrating hormone receptor 1 (MCHR1) in murine models of depression". Biological Psychiatry 61 (2): 174–80. Jan 2007. doi:10.1016/j.biopsych.2006.03.076. PMID 16934771.
- ↑ "The melanin-concentrating hormone system and its physiological functions". Orphan G Protein-Coupled Receptors and Novel Neuropeptides. Results and Problems in Cell Differentiation. 46. 2008. pp. 159–79. doi:10.1007/400_2007_052. ISBN 978-3-540-78350-3.
- ↑ "[125I-S36057: a new and highly potent radioligand for the melanin-concentrating hormone receptor"]. British Journal of Pharmacology 133 (3): 371–8. Jun 2001. doi:10.1038/sj.bjp.0704085. PMID 11375253.
- ↑ "Localisation of melanin-concentrating hormone receptor 1 in rat brain and evidence that sleep parameters are not altered despite high central receptor occupancy". European Journal of Pharmacology 616 (1–3): 101–6. Aug 2009. doi:10.1016/j.ejphar.2009.06.009. PMID 19540226.
- ↑ "Analogs of sub-nanomolar hMC1R agonist LK-184 [Ph(CH2)3CO-His-d-Phe-Arg-Trp-NH2]. An additional binding site within the human melanocortin receptor 1?". Bioorganic & Medicinal Chemistry Letters 14 (15): 3997–4000. 2004. doi:10.1016/j.bmcl.2004.05.039. PMID 15225714.
- ↑ "ATC0175: an orally active melanin-concentrating hormone receptor 1 antagonist for the potential treatment of depression and anxiety". CNS Drug Reviews 11 (4): 341–52. 2005. doi:10.1111/j.1527-3458.2005.tb00052.x. PMID 16614734.
- ↑ "Preclinical evaluation of melanin-concentrating hormone receptor 1 antagonism for the treatment of obesity and depression". The Journal of Pharmacology and Experimental Therapeutics 329 (2): 429–38. May 2009. doi:10.1124/jpet.108.143362. PMID 19182070.
- ↑ "Does the melanin-concentrating hormone antagonist SNAP-7941 deserve 3As?". Expert Opinion on Investigational Drugs 12 (6): 1035–8. Jun 2003. doi:10.1517/13543784.12.6.1035. PMID 12783607.
- ↑ "Efficacy of the MCHR1 antagonist N-[3-(1-{[4-(3,4-difluorophenoxy)phenyl]methyl}(4-piperidyl))-4-methylphenyl]-2-methylpropanamide (SNAP 94847) in mouse models of anxiety and depression following acute and chronic administration is independent of hippocampal neurogenesis". The Journal of Pharmacology and Experimental Therapeutics 321 (1): 237–48. Apr 2007. doi:10.1124/jpet.106.109678. PMID 17237257.
- ↑ "T-226296: a novel, orally active and selective melanin-concentrating hormone receptor antagonist". European Journal of Pharmacology 438 (3): 129–35. Mar 2002. doi:10.1016/S0014-2999(02)01314-6. PMID 11909603.
Further reading
- "Characterization of a human gene related to genes encoding somatostatin receptors". FEBS Letters 398 (2–3): 253–8. Dec 1996. doi:10.1016/S0014-5793(96)01160-X. PMID 8977118.
- "Melanin-concentrating hormone is the cognate ligand for the orphan G-protein-coupled receptor SLC-1". Nature 400 (6741): 261–5. Jul 1999. doi:10.1038/22313. PMID 10421367. Bibcode: 1999Natur.400..261C.
- "Molecular characterization of the melanin-concentrating-hormone receptor". Nature 400 (6741): 265–9. Jul 1999. doi:10.1038/22321. PMID 10421368. Bibcode: 1999Natur.400..265S.
- "Isolation and identification of melanin-concentrating hormone as the endogenous ligand of the SLC-1 receptor". Biochemical and Biophysical Research Communications 261 (3): 622–6. Aug 1999. doi:10.1006/bbrc.1999.1104. PMID 10441476.
- "The DNA sequence of human chromosome 22". Nature 402 (6761): 489–95. Dec 1999. doi:10.1038/990031. PMID 10591208. Bibcode: 1999Natur.402..489D.
- "Molecular characterization of the melanin-concentrating hormone/receptor complex: identification of critical residues involved in binding and activation". Molecular Pharmacology 58 (1): 217–25. Jul 2000. doi:10.1124/mol.58.1.217. PMID 10860944.
- "Identification and characterization of a melanin-concentrating hormone receptor". Proceedings of the National Academy of Sciences of the United States of America 98 (13): 7576–81. Jun 2001. doi:10.1073/pnas.131200698. PMID 11416225. Bibcode: 2001PNAS...98.7576A.
- "Short segment of human melanin-concentrating hormone that is sufficient for full activation of human melanin-concentrating hormone receptors 1 and 2". Biochemistry 40 (31): 9379–86. Aug 2001. doi:10.1021/bi010867p. PMID 11478907.
- "Synthesis and biological evaluation in vitro of a selective, high potency peptide agonist of human melanin-concentrating hormone action at human melanin-concentrating hormone receptor 1". The Journal of Biological Chemistry 277 (16): 13821–6. Apr 2002. doi:10.1074/jbc.M200563200. PMID 11839762.
- "SVK14 cells express an MCH binding site different from the MCH1 or MCH2 receptor". Biochemical and Biophysical Research Communications 295 (4): 841–8. Jul 2002. doi:10.1016/S0006-291X(02)00763-5. PMID 12127971.
- "Melanin-concentrating hormone and its receptor are expressed and functional in human skin". Biochemical and Biophysical Research Communications 296 (3): 698–701. Aug 2002. doi:10.1016/S0006-291X(02)00932-4. PMID 12176038.
- "MIZIP, a highly conserved, vertebrate specific melanin-concentrating hormone receptor 1 interacting zinc-finger protein". FEBS Letters 526 (1–3): 124–8. Aug 2002. doi:10.1016/S0014-5793(02)03115-0. PMID 12208518.
- "Human immune cells express ppMCH mRNA and functional MCHR1 receptor". FEBS Letters 527 (1–3): 205–10. Sep 2002. doi:10.1016/S0014-5793(02)03232-5. PMID 12220661. https://orbi.uliege.be/bitstream/2268/26241/1/Human%20immune%20cells%20express%20Verlaet%20Heinen.pdf.
- "The structure and evolution of the melanocortin and MCH receptors in fish and mammals". Genomics 81 (2): 184–91. Feb 2003. doi:10.1016/S0888-7543(02)00037-X. PMID 12620396.
- "Melanin-concentrating hormone receptor 1 activates extracellular signal-regulated kinase and synergizes with G(s)-coupled pathways". Endocrinology 144 (8): 3514–23. Aug 2003. doi:10.1210/en.2002-0004. PMID 12865333.
- "Autoantibodies in vitiligo patients recognize multiple domains of the melanin-concentrating hormone receptor". The Journal of Investigative Dermatology 121 (4): 765–70. Oct 2003. doi:10.1046/j.1523-1747.2003.12494.x. PMID 14632194.
- "Melanin-concentrating hormone receptor mutations and human obesity: functional analysis". Obesity Research 12 (5): 743–9. May 2004. doi:10.1038/oby.2004.89. PMID 15166293.
- "Identification and characterization of single-nucleotide polymorphisms in MCH-R1 and MCH-R2". Obesity Research 12 (8): 1327–34. Aug 2004. doi:10.1038/oby.2004.167. PMID 15340116.
- "A genome annotation-driven approach to cloning the human ORFeome". Genome Biology 5 (10): R84. 2005. doi:10.1186/gb-2004-5-10-r84. PMID 15461802.
External links
- "Melanin-Concentrating Hormone Receptors: MCH1". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2998.
This article incorporates text from the United States National Library of Medicine, which is in the public domain.
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