187
Views
2
CrossRef citations to date
0
Altmetric
Review Article

Cellular models for the study of the pharmacology and signaling of melanin-concentrating hormone receptors

, &
Pages 385-402 | Received 29 Aug 2010, Accepted 13 Sep 2010, Published online: 18 Nov 2010

References

  • Adamantidis A, de Lecea L. Physiological arousal: a role for hypothalamic systems. Cell Mol Life Sci 2008, 65, 1475–1488.
  • Adamantidis A, Salvert D, Goutagny R, Lakaye B, Gervasoni D, Grisar T, Luppi PH, Fort P. Sleep architecture of the melanin-concentrating hormone receptor 1-knockout mice. Eur J Neurosci 2008, 27, 1793–1800.
  • Aizaki Y, Maruyama K, Nakano-Tetsuka M, Saito Y. Distinct roles of the DRY motif in rat melanin-concentrating hormone receptor 1 in signaling control. Peptides 2009, 30, 974–981.
  • Amano M, Takahashi A. Melanin-concentrating hormone: A neuropeptide hormone affecting the relationship between photic environment and fish with special reference to background color and food intake regulation. Peptides 2009, 30, 1979–1984.
  • An S, Cutler G, Zhao JJ, Huang SG, Tian H, Li W, Liang L, Rich M, Bakleh A, Du J, Chen JL, Dai K. Identification and characterization of a melanin-concentrating hormone receptor. Proc Natl Acad Sci USA 2001, 98, 7576–7581.
  • Antal-Zimanyi I, Khawaja X. The role of melanin-concentrating hormone in energy homeostasis and mood disorders. J Mol Neurosci 2009, 39, 86–98.
  • Astrand A, Bohlooly-Y M, Larsdotter S, Mahlapuu M, Andersén H, Tornell J, Ohlsson C, Snaith M, Morgan DG. Mice lacking melanin-concentrating hormone receptor 1 demonstrate increased heart rate associated with altered autonomic activity. Am J Physiol Regul Integr Comp Physiol 2004, 287, R749–R758.
  • Audinot V, Beauverger P, Lahaye C, Suply T, Rodriguez M, Ouvry C, Lamamy V, Imbert J, Rique H, Nahon JL, Galizzi JP, Canet E, Levens N, Fauchere JL, Boutin JA. Structure-activity relationship studies of melanin-concentrating hormone (MCH)-related peptide ligands at SLC-1, the human MCH receptor. J Biol Chem 2001, 276, 13554–13562.
  • Audinot V, Zuana OD, Fabry N, Ouvry C, Nosjean O, Henlin JM, Fauchère JL, Boutin JA. S38151 [p-guanidinobenzoyl-[des-Gly(10)]-MCH(7-17)] is a potent and selective antagonist at the MCH(1) receptor and has anti-feeding properties in vivo. Peptides 2009, 30, 1997–2007.
  • Audinot V, Lahaye C, Suply T, Beauverger P, Rodriguez M, Galizzi JP, Fauchère JL, Boutin JA. [125I]-S36057: a new and highly potent radioligand for the melanin-concentrating hormone receptor. Br J Pharmacol 2001, 133, 371–378.
  • Audinot V, Lahaye C, Suply T, Rovère-Jovène C, Rodriguez M, Nicolas JP, Beauverger P, Cardinaud B, Galizzi JP, Fauchère JL, Nahon JL, Boutin JA. SVK14 cells express an MCH binding site different from the MCH1 or MCH2 receptor. Biochem Biophys Res Commun 2002, 295, 841–848.
  • Bächner D, Kreienkamp HJ, Richter D. MIZIP, a highly conserved, vertebrate specific melanin-concentrating hormone receptor 1 interacting zinc-finger protein. FEBS Lett 2002, 526, 124–128.
  • Bächner D, Kreienkamp H, Weise C, Buck F, Richter D. Identification of melanin concentrating hormone (MCH) as the natural ligand for the orphan somatostatin-like receptor 1 (SLC-1). FEBS Lett 1999, 457, 522–524.
  • Baker BI. Melanin-concentrating hormone: a general vertebrate neuropeptide. Int Rev Cytol 1991, 126, 1–47.
  • Baker BI. Melanin-concentration hormone updated functional considerations. Trends Endocrinol Metab 1994, 5, 120–126.
  • Baker BI. From melanin-concentration to mega-consumption. Peptides 2009, 30, 1967–1968.
  • Baker BI, Eberle AN, Baumann JB, Siegrist W, Girard J. Effect of melanin concentrating hormone on pigment and adrenal cells in vitro. Peptides 1985, 6, 1125–1130.
  • Bednarek MA, Feighner SD, Hreniuk DL, Palyha OC, Morin NR, Sadowski SJ, MacNeil DJ, Howard AD, Van der Ploeg LH. Short segment of human melanin-concentrating hormone that is sufficient for full activation of human melanin-concentrating hormone receptors 1 and 2. Biochemistry 2001, 40, 9379–9386.
  • Bednarek MA, Hreniuk DL, Tan C, Palyha OC, MacNeil DJ, Van der Ploeg LH, Howard AD, Feighner SD. 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 2002, 41, 6383–6390.
  • Bednarek MA, Tan C, Hreniuk DL, Palyha OC, MacNeil DJ, Van der Ploeg LH, Howard AD, Feighner SD. 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. J Biol Chem 2002, 277, 13821–13826.
  • Bell CG, Meyre D, Samson C, Boyle C, Lecoeur C, Tauber M, Jouret B, Jaquet D, Levy-Marchal C, Charles MA, Weill J, Gibson F, Mein CA, Froguel P, Walley AJ. Association of melanin-concentrating hormone receptor 1 5′ polymorphism with early-onset extreme obesity. Diabetes 2005, 54, 3049–3055.
  • Berbari NF, Johnson AD, Lewis JS, Askwith CC, Mykytyn K. Identification of ciliary localization sequences within the third intracellular loop of G protein-coupled receptors. Mol Biol Cell 2008, 19, 1540–1547.
  • Bjursell M, Gerdin AK, Ploj K, Svensson D, Svensson L, Oscarsson J, Snaith M, Törnell J, Bohlooly-Y M. Melanin-concentrating hormone receptor 1 deficiency increases insulin sensitivity in obese leptin-deficient mice without affecting body weight. Diabetes 2006, 55, 725–733.
  • Bohlooly-Y M, Mahlapuu M, Andersén H, Astrand A, Hjorth S, Svensson L, Törnell J, Snaith MR, Morgan DG, Ohlsson C. Osteoporosis in MCHR1-deficient mice. Biochem Biophys Res Commun 2004, 318, 964–969.
  • Borowsky B, Durkin MM, Ogozalek K, Marzabadi MR, DeLeon J, Lagu B, Heurich R, Lichtblau H, Shaposhnik Z, Daniewska I, Blackburn TP, Branchek TA, Gerald C, Vaysse PJ, Forray C. Antidepressant, anxiolytic and anorectic effects of a melanin-concentrating hormone-1 receptor antagonist. Nat Med 2002, 8, 825–830.
  • Boutin JA, Suply T, Audinot V, Rodriguez M, Beauverger P, Nicolas JP, Galizzi JP, Fauchère JL. Melanin-concentrating hormone and its receptors: state of the art. Can J Physiol Pharmacol 2002, 80, 388–395.
  • Bradley RL, Kokkotou EG, Maratos-Flier E, Cheatham B. Melanin-concentrating hormone regulates leptin synthesis and secretion in rat adipocytes. Diabetes 2000, 49, 1073–1077.
  • Bradley RL, Mansfield JP, Maratos-Flier E, Cheatham B. Melanin-concentrating hormone activates signaling pathways in 3T3-L1 adipocytes. Am J Physiol Endocrinol Metab 2002, 283, E584–E592.
  • Burgaud JL, Poosti R, Fehrentz JA, Martinez J, Nahon JL. Melanin-concentrating hormone binding sites in human SVK14 keratinocytes. Biochem Biophys Res Commun 1997, 241, 622–629.
  • Cardinaud B, Darré-Toulemonde F, Duhault J, Boutin JA, Nahon JL. Comparative analysis of melanin-concentrating hormone structure and activity in fishes and mammals. Peptides 2009, 25, 1623–1632.
  • Cavasotto CN, Orry AJ, Murgolo NJ, Czarniecki MF, Kocsi SA, Hawes BE, O’Neill KA, Hine H, Burton MS, Voigt JH, Abagyan RA, Bayne ML, Monsma FJ Jr. Discovery of novel chemotypes to a G-protein-coupled receptor through ligand-steered homology modeling and structure-based virtual screening. J Med Chem 2008, 51, 581–588.
  • Chambers J, Ames RS, Bergsma D, Muir A, Fitzgerald LR, Hervieu G, Dytko GM, Foley JJ, Martin J, Liu WS, Park J, Ellis C, Ganguly S, Konchar S, Cluderay J, Leslie R, Wilson S, Sarau HM. Melanin-concentrating hormone is the cognate ligand for the orphan G-protein-coupled receptor SLC-1. Nature 1999, 400, 261–265.
  • Chen Y, Hu C, Hsu CK, Zhang Q, Bi C, Asnicar M, Hsiung HM, Fox N, Slieker LJ, Yang DD, Heiman ML, Shi Y. Targeted disruption of the melanin-concentrating hormone receptor-1 results in hyperphagia and resistance to diet-induced obesity. Endocrinology 2002, 143, 2469–2477.
  • Chung S, Saito Y, Civelli O. MCH receptors/gene structure-in vivo expression. Peptides 2009, 30, 1985–1989.
  • Cook LB, Delorme-Axford EB, Robinson K. Caveolae as potential mediators of MCH-signaling pathways. Biochem Biophys Res Commun 2008, 375, 592–595.
  • Cotta-Grand N, Rovère C, Guyon A, Cervantes A, Brau F, Nahon JL. Melanin-concentrating hormone induces neurite outgrowth in human neuroblastoma SH-SY5Y cells through p53 and MAPKinase signaling pathways. Peptides 2009, 30, 2014–2024.
  • Drozdz R, Eberle AN. Binding sites for melanin-concentrating hormone (MCH) in brain synaptosomes and membranes from peripheral tissues identified with highly tritiated MCH. J Recept Signal Transduct Res 1995, 15, 487–502.
  • Drozdz R, Eberle AN. Synthesis and iodination of human (phenylalanine 13, tyrosine 19) melanin-concentrating hormone for radioreceptor assay. J Pept Sci 1995, 1, 58–65.
  • Drozdz R, Hintermann E, Eberle AN. Characterization of the receptor for melanin-concentrating hormone on melanoma cells by photocrosslinking. Ann N Y Acad Sci 1998, 839, 210–213.
  • Drozdz R, Hintermann E, Tanner H, Zumsteg U, Eberle AN. (D-(p-benzoylphenylalanine)13, tyrosine19)-melanin-concentrating hormone, a potent analogue for MCH receptor crosslinking. J Pept Sci 1999, 5, 234–242.
  • Drozdz R, Siegrist W, Baker BI, Chluba-de Tapia J, Eberle AN. Melanin-concentrating hormone binding to mouse melanoma cells in vitro. FEBS Lett 1995, 359, 199–202.
  • Eberle AN. Proopiomelanocortin and the melanocortin peptides. In: Cone RD, editor. The Melanocortin Receptors. Totowa, NJ, Humana Press, 2000, 3–67.
  • Eberle AN, Atherton E, Dryland A, Sheppard RC. Peptide synthesis. Part 9. Solid-phase synthesis of melanin concentrating hormone using a continuous-flow polyamide method. J Chem Soc Perkin Trans 1986, 1, 361–367.
  • Eberle AN, Mild G, Schlumberger S, Drozdz R, Hintermann E, Zumsteg U. Expression and characterization of melanin-concentrating hormone receptors on mammalian cell lines. Peptides 2004, 25, 1585–1595.
  • Elliott JC, Harrold JA, Brodin P, Enquist K, Bäckman A, Byström M, Lindgren K, King P, Williams G. Increases in melanin-concentrating hormone and MCH receptor levels in the hypothalamus of dietary-obese rats. Brain Res Mol Brain Res 2004, 128, 150–159.
  • Evans NA, Groarke DA, Warrack J, Greenwood CJ, Dodgson K, Milligan G, Wilson S. Visualizing differences in ligand-induced β-arrestin-GFP interactions and trafficking between three recently characterized G protein-coupled receptors. J Neurochem 2001, 77, 4764–4785.
  • Fan J, Perry SJ, Gao Y, Schwarz DA, Maki RA. A point mutation in the human melanin concentrating hormone receptor 1 reveals an important domain for cellular trafficking. Mol Endocrinol 2005, 19, 2579–2590.
  • Forray C. The MCH receptor family: feeding brain disorders? Curr Opin Pharmacol 2003, 3, 85–89.
  • Francke F, Buck F, Bächner D. MYND domain specific interaction of the melanin-concentrating hormone receptor 1 interacting zinc-finger protein with α- and β-tubulin. Biochem Biophys Res Commun 2005, 334, 1292–1298.
  • Francke F, Ward RJ, Jenkins L, Kellett E, Richter D, Milligan G, Bächner D. Interaction of neurochondrin with the melanin-concentrating hormone receptor 1 interferes with G protein-coupled signal transduction but not agonist-mediated internalization. J Biol Chem 2006, 281, 32496–32507.
  • Fried S, O’Neill K, Hawes BE. Cloning and characterization of rhesus monkey MCH-R1 and MCH-R2. Peptides 2002, 23, 1401–1408.
  • Fry D, Dayton B, Brodjian S, Ogiela C, Sidorowicz H, Frost LJ, McNally T, Reilly RM, Collins CA. Characterization of a neuronal cell line expressing native human melanin-concentrating hormone receptor 1 (MCHR1). Int J Biochem Cell Biol 2006, 38, 1290–1299.
  • Gao X, Hsu CK, Heinz LJ, Morin J, Shi Y, Shukla NK, Smiley DL, Xu J, Zhong B, Slieker LJ. Europium-labeled melanin-concentrating hormone analogues: ligands for measuring binding to melanin-concentrating hormone receptors 1 and 2. Anal Biochem 2004, 328, 187–195.
  • Gavalas NG, Gottumukkala RV, Gawkrodger DJ, Watson PF, Weetman AP, Kemp EH. Mapping of melanin-concentrating hormone receptor 1 B cell epitopes predicts two major binding sites for vitiligo patient autoantibodies. Exp Dermatol 2009, 18, 454–463.
  • Gehlert DR, Rasmussen K, Shaw J, Li X, Ardayfio P, Craft L, Coskun T, Zhang HY, Chen Y, Witkin JM. Preclinical evaluation of melanin-concentrating hormone receptor 1 antagonism for the treatment of obesity and depression. J Pharmacol Exp Ther 2009, 329, 429–438.
  • Ghoussaini M, Vatin V, Lecoeur C, Abkevich V, Younus A, Samson C, Wachter C, Heude B, Tauber M, Tounian P, Hercberg S, Weill J, Levy-Marchal C, Le Stunff C, Bougnères P, Froguel P, Meyre D. Genetic study of the melanin-concentrating hormone receptor 2 in childhood and adulthood severe obesity. J Clin Endocrinol Metab 2007, 92, 4403–4409.
  • Gibson WT, Pissios P, Trombly DJ, Luan J, Keogh J, Wareham NJ, Maratos-Flier E, O’Rahilly S, Farooqi IS. Melanin-concentrating hormone receptor mutations and human obesity: functional analysis. Obes Res 2004, 12, 743–749.
  • Gottumukkala RV, Waterman EA, Herd LM, Gawkrodger DJ, Watson PF, Weetman AP, Kemp EH. Autoantibodies in vitiligo patients recognize multiple domains of the melanin-concentrating hormone receptor. J Invest Dermatol 2003, 121, 765–770.
  • GPCRDB (G Protein-Coupled Receptor Data Base) Cross-references at www.gpcr.org/seq/DRlist.html#001_002.
  • Griffond B, Baker BI. Cell and molecular cell biology of melanin-concentrating hormone. Int Rev Cytol 2002, 213, 233–277.
  • Harrison C, Traynor JR. The [35S]GTPgammaS binding assay: approaches and applications in pharmacology. Life Sci 2003, 74, 489–508.
  • Hawes BE, Green B, O’Neill K, Fried S, Arreaza MG, Qiu P, Simon JS. Identification and characterization of single-nucleotide polymorphisms in MCH-R1 and MCH-R2. Obes Res 2004, 12, 1327–1334.
  • Hawes BE, Kil E, Green B, O’Neill K, Fried S, Graziano MP. The melanin-concentrating hormone receptor couples to multiple G proteins to activate diverse intracellular signaling pathways. Endocrinology 2000, 141, 4524–4532.
  • Hervieu GJ, Cluderay JE, Harrison D, Meakin J, Maycox P, Nasir S, Leslie RA. The distribution of the mRNA and protein products of the melanin-concentrating hormone (MCH) receptor gene, slc-1, in the central nervous system of the rat. Eur J Neurosci 2000, 12, 1194–1216.
  • Hill J, Duckworth M, Murdock P, Rennie G, Sabido-David C, Ames RS, Szekeres P, Wilson S, Bergsma DJ, Gloger IS, Levy DS, Chambers JK, Muir AI. Molecular cloning and functional characterization of MCH2, a novel human MCH receptor. J Biol Chem 2001, 276, 20125–20129.
  • Hintermann E, Drozdz R, Tanner H, Eberle AN. Synthesis and characterization of new radioligands for the mammalian melanin-concentrating hormone (MCH) receptor. J Recept Signal Transduct Res 1999, 19, 411–422.
  • Hintermann E, Drozdz R, Tanner H, Zumsteg U, Eberle AN. Radioligands for the receptor of mammalian melanin-concentrating hormone (MCH). In: Shimonishi Y, ed. Peptide Science, Present and Future. Dordrecht, Kluwer, 1999, 226–227.
  • Hintermann E, Erb C, Talke-Messerer C, Liu R, Tanner H, Flammer J, Eberle AN. Expression of the melanin-concentrating hormone receptor in porcine and human ciliary epithelial cells. Invest Ophthalmol Vis Sci 2001, 42, 206–209.
  • Hintermann E, Tanner H, Talke-Messerer C, Schlumberger S, Zumsteg U, Eberle AN. Interaction of melanin-concentrating hormone (MCH), neuropeptide E-I (NEI), neuropeptide G-E (NGE), and α-MSH with melanocortin and MCH receptors on mouse B16 melanoma cells. J Recept Signal Transduct Res 2001, 21, 93–116.
  • Hoogduijn MJ, Ancans J, Suzuki I, Estdale S, Thody AJ. Melanin-concentrating hormone and its receptor are expressed and functional in human skin. Biochem Biophys Res Commun 2002, 296, 698–701.
  • Ito M, Ishihara A, Gomori A, Egashira S, Matsushita H, Mashiko S, Ito J, Ito M, Nakase K, Haga Y, Iwaasa H, Suzuki T, Ohtake N, Moriya M, Sato N, MacNeil DJ, Takenaga N, Tokita S, Kanatani A. Melanin-concentrating hormone 1-receptor antagonist suppresses body weight gain correlated with high receptor occupancy levels in diet-induced obesity mice. Eur J Pharmacol 2009, 624, 77–83.
  • Ito M, Sakamoto T, Suzuki T, Egashira S, Moriya M, Ishihara A, Iwaasa H, Matsushita H, Nakase K, Wallace MA, Dean D, Sato N, Tokita S, Kanatani A. Identification and characterization of a selective radioligand for melanin-concentrating hormone 1-receptor (MCH1R). Bioorg Med Chem Lett 2009, 19, 2835–2839.
  • Jiang M, Bajpayee NS. Molecular mechanisms of go signaling. Neurosignals 2009, 17, 23–41.
  • Kawauchi H. Functions of melanin-concentrating hormone in fish. J Exp Zoolog Part A Comp Exp Biol 2006, 305, 751–760.
  • Kawauchi H, Baker BI. Melanin-concentrating hormone signaling systems in fish. Peptides 2004, 25, 1577–1584.
  • Kawauchi H, Kawazoe I, Tsubokawa M, Kishida M, Baker BI. Characterization of melanin-concentrating hormone in chum salmon pituitaries. Nature 1983, 305, 321–323.
  • Kemp EH, Weetman AP. Melanin-concentrating hormone and melanin-concentrating hormone receptors in mammalian skin physiopathology. Peptides 2009, 30, 2071–2075.
  • Kemp EH, Waterman EA, Hawes BE, O’Neill K, Gottumukkala RV, Gawkrodger DJ, Weetman AP, Watson PF. The melanin-concentrating hormone receptor 1, a novel target of autoantibody responses in vitiligo. J Clin Invest 2002, 109, 923–930.
  • Kokkotou E, Mastaitis JW, Qu D, Hoersch D, Slieker L, Bonter K, Tritos NA, Maratos-Flier E. Characterization of [Phe(13), Tyr(19)]-MCH analog binding activity to the MCH receptor. Neuropeptides 2000, 34, 240–247.
  • Kokkotou EG, Tritos NA, Mastaitis JW, Slieker L, Maratos-Flier E. Melanin-concentrating hormone receptor is a target of leptin action in the mouse brain. Endocrinology 2001, 142, 680–686.
  • Kolakowski LF Jr, Jung BP, Nguyen T, Johnson MP, Lynch KR, Cheng R, Heng HH, George SR, O’Dowd BF. Characterization of a human gene related to genes encoding somatostatin receptors. FEBS Lett 1996, 398, 253–258.
  • Kowalski TJ, Sasikumar T. Melanin-concentrating hormone receptor-1 antagonists as antiobesity therapeutics: current status. BioDrugs 2007, 21, 311–321.
  • Kym PR, Judd AS, Lynch JK, Iyengar R, Vasudevan A, Souers AJ. Lead optimization strategies and tactics applied to the discovery of melanin concentrating hormone receptor 1 antagonists. Curr Top Med Chem 2007, 7, 1471–1488.
  • Lee S. Development of a vacuum filtration system for the conventional microplate washer. J Pharmacol Toxicol Methods 2006, 53, 272–276.
  • Lee S, Kim GD, Park WK, Cho H, Byung Ho Lee Yoo, SE, Jae Yang Kong. Development of a time-resolved fluorometric assay for the high throughput screening of melanin concentrating hormone receptor antagonists. J Pharmacol Toxicol Methods 2006, 53, 242–247.
  • Lembo PM, Grazzini E, Cao J, Hubatsch DA, Pelletier M, Hoffert C, St-Onge S, Pou C, Labrecque J, Groblewski T, O’Donnell D, Payza K, Ahmad S, Walker P. The receptor for the orexigenic peptide melanin-concentrating hormone is a G-protein-coupled receptor. Nat Cell Biol 1999, 1, 267–271.
  • Logan DW, Bryson-Richardson RJ, Pagán KE, Taylor MS, Currie PD, Jackson IJ. The structure and evolution of the melanocortin and MCH receptors in fish and mammals. Genomics 2003, 81, 184–191.
  • Luthin DR. Anti-obesity effects of small molecule melanin-concentrating hormone receptor 1 (MCHR1) antagonists. Life Sci 2007, 81, 423–440.
  • Macdonald D, Murgolo N, Zhang R, Durkin JP, Yao X, Strader CD, Graziano MP. Molecular characterization of the melanin-concentrating hormone/receptor complex: identification of critical residues involved in binding and activation. Mol Pharmacol 2000, 58, 217–225.
  • Marsh DJ, Weingarth DT, Novi DE, Chen HY, Trumbauer ME, Chen AS, Guan XM, Jiang MM, Feng Y, Camacho RE, Shen Z, Frazier EG, Yu H, Metzger JM, Kuca SJ, Shearman LP, Gopal-Truter S, MacNeil DJ, Strack AM, MacIntyre DE, Van der Ploeg LH, Qian S. Melanin-concentrating hormone 1 receptor-deficient mice are lean, hyperactive, and hyperphagic and have altered metabolism. Proc Natl Acad Sci USA 2002, 99, 3240–3245.
  • Marsteller DA, Gerald CP, Kong R, Cajina M, Craig DA, Swanson CJ. The MCH1 receptor antagonist SNAP 94847 induces sensitivity to dopamine D2/D3 receptor agonists in rats and mice. Eur J Pharmacol 2009, 602, 66–72.
  • McBriar MD, Guzik H, Shapiro S, Paruchova J, Xu R, Palani A, Clader JW, Cox K, Greenlee WJ, Hawes BE, Kowalski TJ, O’neill K, Spar BD, Weig B, Weston DJ, Farley C, Cook J. Discovery of orally efficacious melanin-concentrating hormone receptor-1 antagonists as antiobesity agents. Synthesis, SAR, and biological evaluation of bicyclo[3.1.0]hexyl ureas. J Med Chem 2006, 49, 2294–2310.
  • Milligan G, Murdoch H, Kellett E, White JH, Feng GJ. Interactions between G-protein-coupled receptors and periplakin: a selective means to regulate G-protein activation. Biochem Soc Trans 2004, 32, 878–880.
  • Miyamoto-Matsubara M, Saitoh O, Maruyama K, Aizaki Y, Saito Y. Regulation of melanin-concentrating hormone receptor 1 signaling by RGS8 with the receptor third intracellular loop. Cell Signal 2008, 20, 2084–2094.
  • Miyamoto-Matsubara M, Chung S, Saito Y. Functional interaction of regulator of G protein signaling-2 with melanin-concentrating hormone receptor 1. Ann N Y Acad Sci 2010, 1200, 112–119.
  • Mori M, Harada M, Terao Y, Sugo T, Watanabe T, Shimomura Y, Abe M, Shintani Y, Onda H, Nishimura O, Fujino M. Cloning of a novel G protein-coupled receptor, SLT, a subtype of the melanin-concentrating hormone receptor. Biochem Biophys Res Commun 2001, 283, 1013–1018.
  • Murdoch H, Feng GJ, Bächner D, Ormiston L, White JH, Richter D, Milligan G. Periplakin interferes with G protein activation by the melanin-concentrating hormone receptor-1 by binding to the proximal segment of the receptor C-terminal tail. J Biol Chem 2005, 280, 8208–8220.
  • Nagasaki H, Chung S, Dooley CT, Wang Z, Li C, Saito Y, Clark SD, Houghten RA, Civelli O. The pharmacological properties of a novel MCH1 receptor antagonist isolated from combinatorial libraries. Eur J Pharmacol 2009, 602, 194–202.
  • Nahon JL, Presse F, Bittencourt JC, Sawchenko PE, Vale W. The rat melanin-concentrating hormone messenger ribonucleic acid encodes multiple putative neuropeptides coexpressed in the dorsolateral hypothalamus. Endocrinology 1989, 125, 2056–2065.
  • Oh KS, Ryu SY, Lee S, Seo HW, Oh BK, Kim YS, Lee BH. Melanin-concentrating hormone-1 receptor antagonism and anti-obesity effects of ethanolic extract from Morus alba leaves in diet-induced obese mice. J Ethnopharmacol 2009, 122, 216–220.
  • Okamoto K, Yasumura K, Fujitani K, Kiso Y, Kawauchi H, Kawazoe I, Yajima H. Synthesis of the heptadecapeptide corresponding to the entire amino acid sequence of salmon melanin-concentrating hormone (MCH). Chem Pharm Bull 1984, 32, 2963–2970.
  • Pissios P, Bradley RL, Maratos-Flier E. Expanding the scales: The multiple roles of MCH in regulating energy balance and other biological functions. Endocr Rev 2006, 27, 606–620.
  • Pissios P, Maratos-Flier E. Melanin-concentrating hormone: from fish skin to skinny mammals. Trends Endocrinol Metab 2003, 14, 243–248.
  • Pissios P, Ozcan U, Kokkotou E, Okada T, Liew CW, Liu S, Peters JN, Dahlgren G, Karamchandani J, Kudva YC, Kurpad AJ, Kennedy RT, Maratos-Flier E, Kulkarni RN. Melanin concentrating hormone is a novel regulator of islet function and growth. Diabetes 2007, 56, 311–319.
  • Pissios P, Trombly DJ, Tzameli I, Maratos-Flier E. Melanin-concentrating hormone receptor 1 activates extracellular signal-regulated kinase and synergizes with G(s)-coupled pathways. Endocrinology 2003, 144, 3514–3523.
  • Presse F, Nahon JL, Fischer WH, Vale W. Structure of the human melanin concentrating hormone mRNA. Mol Endocrinol 1990, 4, 632–637.
  • Rance T, Baker BI. The teleost melanin-concentrating hormone – a pituitary hormone of hypothalamic origin. Gen Comp Endocrinol 1979, 37, 64–73.
  • Receveur JM, Bjurling E, Ulven T, Little PB, Nørregaard PK, Högberg T. 4-Acylamino-and 4-ureidobenzamides as melanin-concentrating hormone (MCH) receptor 1 antagonists. Bioorg Med Chem Lett 2004, 14, 5075–5080.
  • Rhee SG. Regulation of phosphoinositide-specific phospholipase C. Annu Rev Biochem 2001, 70, 281–312.
  • Rivera G, Bocanegra-García V, Galiano S, Cirauqui N, Ceras J, Pérez S, Aldana I, Monge A. Melanin-concentrating hormone receptor 1 antagonists: a new perspective for the pharmacologic treatment of obesity. Curr Med Chem 2008, 15, 1025–1043.
  • Rodriguez M, Beauverger P, Naime I, Rique H, Ouvry C, Souchaud S, Dromaint S, Nagel N, Suply T, Audinot V, Boutin JA, Galizzi JP. Cloning and molecular characterization of the novel human melanin-concentrating hormone receptor MCH2. Mol Pharmacol 2001, 60, 632–639.
  • Rokosz LL, Hobbs DW. Biological examination of melanin concentrating hormone receptor 1: multi-tasking from the hypothalamus. Drug News Perspect 2006, 19, 273–286.
  • Rutanen J, Pihlajamäki J, Vänttinen M, Salmenniemi U, Ruotsalainen E, Kuulasmaa T, Kainulainen S, Kuusisto J, Laakso M. Single nucleotide polymorphisms of the MCHR1 gene do not affect metabolism in humans. Obesity 2007, 15, 2902–2907.
  • Sailer AW, Sano H, Zeng Z, McDonald TP, Pan J, Pong SS, Feighner SD, Tan CP, Fukami T, Iwaasa H, Hreniuk DL, Morin NR, Sadowski SJ, Ito M, Ito M, Bansal A, Ky B, Figueroa DJ, Jiang Q, Austin CP, MacNeil DJ, Ishihara A, Ihara M, Kanatani A, Van der Ploeg LH, Howard AD, Liu Q. Identification and characterization of a second melanin-concentrating hormone receptor, MCH-2R. Proc Natl Acad Sci USA 2001, 98, 7564–7569.
  • Saito Y, Cheng M, Leslie FM, Civelli O. Expression of the melanin-concentrating hormone (MCH) receptor mRNA in the rat brain. J Comp Neurol 2001, 435, 26–40.
  • Saito Y, Maruyama K. Identification of melanin-concentrating hormone receptor and its impact on drug discovery. J Exp Zoolog Part A Comp Exp Biol 2006, 305, 761–768.
  • Saito Y, Nagasaki H. The melanin-concentrating hormone system and its physiological functions. Results Probl Cell Differ 2008, 46, 159–179.
  • Saito Y, Nothacker HP, Civelli O. Melanin-concentrating hormone receptor: an orphan receptor fits the key. Trends Endocrinol Metab 2000, 11, 299–303.
  • Saito Y, Nothacker HP, Wang Z, Lin SH, Leslie F, Civelli O. Molecular characterization of the melanin-concentrating-hormone receptor. Nature 1999, 400, 265–269.
  • Saito Y, Tetsuka M, Li Y, Kurose H, Maruyama K. Properties of rat melanin-concentrating hormone receptor 1 internalization. Peptides 2004, 25, 1597–1604.
  • Saito Y, Tetsuka M, Saito S, Imai K, Yoshikawa A, Doi H, Maruyama K. Arginine residue 155 in the second intracellular loop plays a critical role in rat melanin-concentrating hormone receptor 1 activation. Endocrinology 2005, 146, 3452–3462.
  • Saito Y, Tetsuka M, Yue L, Kawamura Y, Maruyama K. Functional role of N-linked glycosylation on the rat melanin-concentrating hormone receptor 1. FEBS Lett 2003, 533, 29–34.
  • Saito Y, Wang Z, Hagino-Yamagishi K, Civelli O, Kawashima S, Maruyama K. Endogenous melanin-concentrating hormone receptor SLC-1 in human melanoma SK-MEL-37 cells. Biochem Biophys Res Commun 2001, 289, 44–50.
  • Schlumberger SE, Jäggin V, Tanner H, Eberle AN. Endogenous receptor for melanin-concentrating hormone in human neuroblastoma Kelly cells. Biochem Biophys Res Commun 2002, 298, 54–59.
  • Schlumberger SE, Saito Y, Giller T, Hintermann E, Tanner H, Jäggin V, Zumsteg U, Civelli O, Eberle AN. Different structural requirements for melanin-concentrating hormone (MCH) interacting with rat MCH-R1 (SLC-1) and mouse B16 cell MCH-R. J Recept Signal Transduct Res 2003, 23, 69–81.
  • Schlumberger SE, Talke-Messerer C, Zumsteg U, Eberle AN. Expression of receptors for melanin-concentrating hormone (MCH) in different tissues and cell lines. J Recept Signal Transduct Res 2002, 22, 509–531.
  • Segal-Lieberman G, Bradley RL, Kokkotou E, Carlson M, Trombly DJ, Wang X, Bates S, Myers MG Jr, Flier JS, Maratos-Flier E. Melanin-concentrating hormone is a critical mediator of the leptin-deficient phenotype. Proc Natl Acad Sci USA 2003, 100, 10085–10090.
  • Shearman LP, Camacho RE, Sloan Stribling D, Zhou D, Bednarek MA, Hreniuk DL, Feighner SD, Tan CP, Howard AD, Van der Ploeg LH, MacIntyre DE, Hickey GJ, Strack AM. Chronic MCH-1 receptor modulation alters appetite, body weight and adiposity in rats. Eur J Pharmacol 2003, 475, 37–47.
  • Shimada M, Tritos NA, Lowell BB, Flier JS, Maratos-Flier E. Mice lacking melanin-concentrating hormone are hypophagic and lean. Nature 1998, 396, 670–674.
  • Shimomura Y, Mori M, Sugo T, Ishibashi Y, Abe M, Kurokawa T, Onda H, Nishimura O, Sumino Y, Fujino M. Isolation and identification of melanin-concentrating hormone as the endogenous ligand of the SLC-1 receptor. Biochem Biophys Res Commun 1999, 261, 622–626.
  • Siegrist W, Eberle AN. Homologous regulation of the MSH receptor in melanoma cells. J Recept Res 1993, 13, 263–281.
  • Siegrist W, Stutz S, Eberle AN. Homologous and heterologous regulation of α-melanocyte-stimulating hormone receptors in human and mouse melanoma cell lines. Cancer Res 1994, 54, 2604–2610.
  • Smith DG, Hegde LG, Wolinsky TD, Miller S, Papp M, Ping X, Edwards T, Gerald CP, Craig DA. The effects of stressful stimuli and hypothalamic-pituitary-adrenal axis activation are reversed by the melanin-concentrating hormone 1 receptor antagonist SNAP 94847 in rodents. Behav Brain Res 2009, 197, 284–291.
  • Solca F, Siegrist W, Drozdz R, Girard J, Eberle AN. The receptor for α-melanotropin of mouse and human melanoma cells. Application of a potent α-melanotropin photoaffinity label. J Biol Chem 1989, 264, 14277–14281.
  • Souers AJ, Wodka D, Gao J, Lewis JC, Vasudevan A, Gentles R, Brodjian S, Dayton B, Ogiela CA, Fry D, Hernandez LE, Marsh KC, Collins CA, Kym PR. Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 1. Bioorg Med Chem Lett 2004, 14, 4873–4877.
  • Suply T, Cardinaud B, Kanamori S, Dal Farra C, Ricois S, Nahon JL. Ligand binding profile and effects of melanin-concentrating hormone on fish and mammalian skin cells. Ann N Y Acad Sci 1999, 885, 455–458.
  • Suply T, Della Zuana O, Audinot V, Rodriguez M, Beauverger P, Duhault J, Canet E, Galizzi JP, Nahon JL, Levens N, Boutin JA. SLC-1 receptor mediates effect of melanin-concentrating hormone on feeding behavior in rat: a structure-activity study. J Pharmacol Exp Ther 2001, 299, 137–146.
  • Tadayyon M, Welters HJ, Haynes AC, Cluderay JE, Hervieu G. Expression of melanin-concentrating hormone receptors in insulin-producing cells: MCH stimulates insulin release in RINm5F and CRI-G1 cell-lines. Biochem Biophys Res Commun 2000, 275, 709–712.
  • Takahashi K. Translational medicine in fish-derived peptides: from fish endocrinology to human physiology and diseases. Endocr J 2004, 51, 1–17.
  • Takahashi A, Kosugi T, Kobayashi Y, Yamanome T, Schiöth HB, Kawauchi H. 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 2007, 151, 210–219.
  • Takahashi K, Totsune K, Murakami O, Sone M, Satoh F, Kitamuro T, Noshiro T, Hayashi Y, Sasano H, Shibahara S. Expression of melanin-concentrating hormone receptor messenger ribonucleic acid in tumor tissues of pheochromocytoma, ganglioneuroblastoma, and neuroblastoma. J Clin Endocrinol Metab 2001, 86, 369–374.
  • Takekawa S, Asami A, Ishihara Y, Terauchi J, Kato K, Shimomura Y, Mori M, Murakoshi H, Kato K, Suzuki N, Nishimura O, Fujino M. T-226296: a novel, orally active and selective melanin-concentrating hormone receptor antagonist. Eur J Pharmacol 2002, 438, 129–135.
  • Tan CP, Sano H, Iwaasa H, Pan J, Sailer AW, Hreniuk DL, Feighner SD, Palyha OC, Pong SS, Figueroa DJ, Austin CP, Jiang MM, Yu H, Ito J, Ito M, Ito M, Guan XM, MacNeil DJ, Kanatani A, Van der Ploeg LH, Howard AD. Melanin-concentrating hormone receptor subtypes 1 and 2: species-specific gene expression. Genomics 2002, 79, 785–792.
  • Tetsuka M, Saito Y, Imai K, Doi H, Maruyama K. The basic residues in the membrane-proximal C-terminal tail of the rat melanin-concentrating hormone receptor 1 are required for receptor function. Endocrinology 2004, 145, 3712–3723.
  • Unmehopa UA, van Heerikhuize JJ, Spijkstra W, Woods JW, Howard AD, Zycband E, Feighner SD, Hreniuk DL, Palyha OC, Guan XM, Macneil DJ, Van der Ploeg LH, Swaab DF. Increased melanin concentrating hormone receptor type I in the human hypothalamic infundibular nucleus in cachexia. J Clin Endocrinol Metab 2005, 90, 2412–2419.
  • Vaughan JM, Fischer WH, Hoeger C, Rivier J, Vale W. Characterization of melanin-concentrating hormone from rat hypothalamus. Endocrinology 1989, 125, 1660–1665.
  • Verlaet M, Adamantidis A, Coumans B, Chanas G, Zorzi W, Heinen E, Grisar T, Lakaye B. Human immune cells express ppMCH mRNA and functional MCHR1 receptor. FEBS Lett 2002, 527, 205–210.
  • Wang S, Behan J, O’Neill K, Weig B, Fried S, Laz T, Bayne M, Gustafson E, Hawes BE. Identification and pharmacological characterization of a novel human melanin-concentrating hormone receptor, mch-r2. J Biol Chem 2001, 276, 34664–34670.
  • Warrior U, Gopalakrishnan S, Vanhauwe J, Burns D. High throughput screening assays for G protein-coupled receptors. In: Lundstrom KH, Chiu ML, eds. G Protein-coupled Receptors in Drug Discovery. Boca Raton, FL, CRC Press, 2006, 159–190.
  • Wermter AK, Reichwald K, Büch T, Geller F, Platzer C, Huse K, Hess C, Remschmidt H, Gudermann T, Preibisch G, Siegfried W, Goldschmidt HP, Li WD, Price RA, Biebermann H, Krude H, Vollmert C, Wichmann HE, Illig T, Sørensen TI, Astrup A, Larsen LH, Pedersen O, Eberlé D, Clément K, Blundell J, Wabitsch M, Schäfer H, Platzer M, Hinney A, Hebebrand J. Mutation analysis of the MCHR1 gene in human obesity. Eur J Endocrinol 2005, 152, 851–862.
  • Wilkes BC, Hruby VJ, Sherbrooke WC, Castrucci AM, Hadley ME. Synthesis and biological actions of melanin concentrating hormone. Biochem Biophys Res Commun 1984, 122, 613–619.
  • Wu S, Liu B. Application of scintillation proximity assay in drug discovery. BioDrugs 2005, 19, 383–392.
  • Yan JH, Li QY, Boutin JA, Renard MP, Ding YX, Hao XJ, Zhao WM, Wang MW. High-throughput screening of novel antagonists on melanin-concentrating hormone receptor-1. Acta Pharmacol Sin 2008, 29, 752–758.
  • Yang J, Yuan C, Wei L, Yi F, Song F. Melanin-concentrating hormone receptor 2 affects 3T3-L1 preadipocyte differentiation. Mol Cell Endocrinol 2009, 311, 11–17.
  • Zhang Q, Yuan CF, Wu MJ, Wang YG, Qin Q, Shi YY, Liu GL, Song FZ. Comparative proteomic analysis of proteins influenced by melanin-concentrating hormone and melanin-concentrating hormone receptor 2 interaction. Horm Metab Res 2010, 42, 521–527.

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.