Ligands of the melanocortin receptors, 2002 – 2003 update

Bibliography

• WIKBERG JES: Melanocortin receptors: new opportunities in drug discovery. Expert Opin. The]: Patents (2001) 11:1429–1441.
   Web of Science ®Google Scholar
• ANDERSON PM, BOMAN A, SEIFER E, SKOTTNER A, LUNDSTEDT T: Ligands to the melanocortin receptors. Expert Opin. Ther. Patents (2001) 11:1583–1592.
   Web of Science ®Google Scholar
• •Review of the patent literature on ligands for the melanocortin receptors.
   Google Scholar
• SPEAKE JD, BISHOP MJ: Recent advances in the development of melanocortin-4 receptor agonists. Expert Opin. The]: Patents (2002) 12:1631–1638.
   Google Scholar
• •Review of the patent literature on MC4R ligands.
   Google Scholar
• CONE RD (Ed.): The melanocortin receptors Humana, Totowa, NJ, USA (2000).
   Google Scholar
• CONE RD (Ed.): The melanocortin system. Ann. NY Acad. Sci. Vol 994. New York, NY, USA (2003).
   Google Scholar
• SEBHAT I, YE Z, BEDNAREK M et al: Melanocortin receptor agonists and antagonists: chemistry and potential therapeutic utilities. Ann. Rep. Med. Chem. (2003) 38:31–40.
   Web of Science ®Google Scholar
• GANTZ I, FONG TM: The melanocortin system. Am. Physiol Endocrinol Metab. (2003) 284:E468–E474.
   PubMedGoogle Scholar
• MACNEIL DJ, HOWARD AD, GUAN X et al.: The role of melanocortins in body weight regulation: opportunities for the treatment of obesity. Ear: .1. Pharmacol (2002) 450:93–109.
   Google Scholar
• VAN DER PLOEG LH, MARTIN WJ, HOWARD AD et al: A role for the melanocortin 4 receptor in sexual function. Proc. Natl. Acad. Sci. (2002) 17:11381–11386.
   Google Scholar
• STAROWICZ K, PRZEWLOCKA B: The role of melanocortins and their receptors in inflammatory processes, nerve regeneration and nociception. Life Sci (2003) 73:823–847.
   PubMed Web of Science ®Google Scholar
• GETTING SJ: Melanocortin peptides and their receptors: new targets for anti-inflammatory therapy. Trends Pharmacol Sci (2002) 23:447–449.
   PubMed Web of Science ®Google Scholar
• CATANIA A, AIRAGHI L, COLOMBO G et al.: a-Melanocyte-stimulating hormone in normal human physiology and disease states. Trends Endocrinol Metab. (2000) 11:304–308.
   PubMed Web of Science ®Google Scholar
• FAROOQI IS, KEOGH JM, YEO GS et al.: Clinical spectrum of obesity and mutations in the melanocortin 4 receptor gene. N Engl. I Med. (2003). 348:1085–1095.
   PubMed Web of Science ®Google Scholar
• BRANSON R, POTOCZNA N, KRAL JG et al.: Binge eating as a major phenotype of melanocortin 4 receptor gene mutations. N. Eng] Med. (2003) 348:1096–1103.
   PubMed Web of Science ®Google Scholar
• LUBRANO-BERTHELIER C, DURAND E, DUBERN B et al: Intracellular retention is a common characteristic of childhood obesity-associated MC4R mutations. Hum. Ma Genet. (2003) 12:145–153.
   PubMed Web of Science ®Google Scholar
• NIJENHUIS WA, GARNER KM, VAN ROZEN RJ et al.: Poor cell surface expression of human melanocortin-4 receptor mutations associated with obesity. J. Biol. Chem. (2003) 278(25):22939–22945.
   Google Scholar
• TAO YX, SEGALOFF DL: Functional characterization of melanocortin-4 receptor mutations associated with childhood obesity. Endocrinology (2003) 144:4544–4551.
   PubMed Web of Science ®Google Scholar
• MARKS DL, BUTLER AA, TURNER R et al.: Differential role of melanocortin receptor subtypes in cachexia. Endocrinology (2003) 144:1513–1523.
   PubMed Web of Science ®Google Scholar
• CHEN AS, MARSH DJ, TRUMBAUER ME et al.: Inactivation of the mouse melanocortin-3 receptor results in increased fat mass and reduced lean body mass. Nat. Genet. (2000) 26:97–102.
   PubMed Web of Science ®Google Scholar
• BUTLER AA, KESTERSON RA, KHONG K et al.: A unique metabolic syndrome causes obesity in the melanocortin-3 receptor-deficient mouse. Endocrinology (2000) 141:3518–3521.
   PubMed Web of Science ®Google Scholar
• MOGIL JS, WILSON SG, CHESLER EJ et al.: The melanocortin-1 receptor gene mediates female-specific mechanisms of analgesia in mice and humans. Proc. Nat] Acad. Sci.USA (2003) 100:4867–4872.
   PubMed Web of Science ®Google Scholar
• STURM RA, TEASDALE RD, BOX NF: Human pigmentation genes: identification, structure and consequences of polymorphic variation. Gene (2001) 277:49–62.
   PubMed Web of Science ®Google Scholar
• SCHAFFER JV, BOLOGNIA JL: The melanocortin-1 receptor: red hair and beyond. Arch. Dermatol (2001) 137:1477–1485.
   PubMed Web of Science ®Google Scholar
• STURM RA, BOX NE RAMSAY M: Human pigmentation genetics: the difference is only skin deep. Bioassays (1998) 20:712–721.
   PubMed Web of Science ®Google Scholar
• COLOMBO G, BUFFA R, BARDELLA MT et al.: Anti-inflammatory effects of alpha-melanocyte-stimulating hormone in celiac intestinal mucosa. Neuroirnmunomodulation (2002) 10:208–216.
   PubMed Web of Science ®Google Scholar
• HERPIN TF, YU G, CARLSON KE et al: Discovery of tyrosine-based potent and selective melanocortin-1 receptor small-molecule agonists with anti-inflammatory properties.j Med. Chem. (2003) 46:1123–1126.
   PubMed Web of Science ®Google Scholar
• UJJAINWALLA F, WARNER D, WALSH T et al.: Design and synthesis of melanocortin subtype-4 receptor agonists: evolution of the pyridazinone archetype. Bioorg. Med. Chem. Lett. (2003) 13:4431–4435.
   PubMed Web of Science ®Google Scholar
• ••A new template for MC4R agonists isreported.
   Google Scholar
• XI N, HALE C, KELY MN et al: Synthesis of novel melanocortin 4 receptor agonists and antagonists containing a succinamide core. Bioorg. Med. Chem. Lett. (2003) 14:377–381.
   Web of Science ®Google Scholar
• DYCK B, PARKER J, PHILLIPS T et al:Aryl piperazine melanocortin MC4 receptor agonists. Bioorg. Med. Chem. Lett. (2003) 13:3793–3796.
   PubMed Web of Science ®Google Scholar
• CHAKI S, OGAWA S, TODAY, FUNAKOSHI T et al: Involvement of the melanocortin MC4 receptor in stress-related behavior in rodents. Eui: Pharmacol (3002) 474:95–101.
   Google Scholar
• CHAKI S, HIROTA S, FUNAKOSHI T et al.: Amdolytic-like and antidepressant-like activities of MCL-0129 (1-[(5)-2- (4-fluorophenyl) 2-(4-isopropylpiperadin-1-y1)ethy11-4- [4 (2-methoxynaphthalen-1-yflbutyl]piperazine), a novel and potent non-peptide antagonist of the melanocortin-4 receptor.' Pharmcol. Exper. Ther. (2003) 304:818–826.
   Google Scholar
• ••A non-peptide MC4R antagonist isreported.
   Google Scholar
• ARASASIGHAM PN, FOTSCH C, OUYANG X et al.: Structure-activity relationship of (1-ary1-2-piperazinylethyl)piperazines: antagonists for the AGRP/melanocortin receptor binding. Med . Chem. (2003) 46:9–11.
   Web of Science ®Google Scholar
• ••Non-peptide MC4R antagonists arereported.
   Google Scholar
• PAN K, SCOTT MK, LEE DHS et a]: 2,3-Diary1-5-anilino [1,2,4]thiadiazoles as melanocortin MC4 receptor agonists and their effects on feeding behavior in rats. Bioorg. Med. Chem. (2003) 11:185–192.
   PubMed Web of Science ®Google Scholar
• ••A new template for MC4R agonists isreported.
   Google Scholar
• BEDNAREK MA, MACNEIL T, TANG R et al.: Selective, high affinity peptide antagonists of a-melanotropin action at human melanocortin receptor 4: their synthesis and biological evaluation M vitro. Med . Chem. (2001) 44:3665–3672.
   Web of Science ®Google Scholar
• FOSTER AC, JOPPA M, MARKISON S et al.: Body weight regulation by selective MC4 receptor agonists and antagonists. Ann. NY Acad. ScL (2003) 994:103–110.
   PubMed Web of Science ®Google Scholar
• HOLDER JR, BAUZO PM, XIANG Z et al: Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arh-Trp-NH2 at the mouse melanocortin receptors. 1. Modifications at the His position. Med . Chem. (2002) 45:2801–2810.
   Google Scholar
• HOLDER JR, BAUZO R, XIANG Z et al: Structure-activity relationships of the melanocortin tetrapeptide Ac-His-D-Phe-Arh-Trp-NH2 at the mouse melanocortin receptors. Part 2. Modifications at the Phe position I Med. Chem. (2002) 45:3073–3081.
   Google Scholar
• WESSELLS H, FUCIARELLI K, HANSEN J et al.: Synthetic melanotropic peptide initiates erections in man with psychogenic erectile dysfunction: double-blind, placebo controlled crossover study. Urol . (1998) 160:389–393.
   Web of Science ®Google Scholar
• MOLINOFF PB, SHADIACK AM, EARLE D et al: PT-141: a melanocortin agonist for the treatment of sexual dysfunction. Ann. NY Acad. ScL (2003) 994:96–102.
   PubMed Web of Science ®Google Scholar
• FEHM HL, SMOLNIK R, KERN W et al.: The melanocortin melanocyte-stimulating hormone/ adrenocorticotropin 4_10 decreases body fat in humans. j Clin. Endocrinol Metabol (2001) 86:1144–1148.
   PubMed Web of Science ®Google Scholar
• SZARDENINGS M, MUCENIECE R, MUTULE I et al.: New highly specific agonistic peptides for human melanocortin MC1 receptor. Peptides (2000) 21:239–243.
   PubMed Web of Science ®Google Scholar
• BALSE-SRINIVASAN P, GRIECO P, CAI M et al.: Structure-activity relationships of novel cyclic a-MSH/ p-msH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R. I Med. Chem. (2003) 46:3728–3733.
   PubMedGoogle Scholar
• HASKELL-LUEVANO C, LIM S, YUAN W et al.: Structure activity studies of the melanocortin antagonist SHU-9119 modified at the 6, 7, 8, and 9 positions. Peptides (2000) 21:49–57.
   PubMed Web of Science ®Google Scholar
• BALSE-SRINIVASAN P, GRIECO P, CAI M et al.: Structure-activity relationships of y-MSH analogues at the human melanocortin MC3, MC4, and MC5 receptors. Discovery of highly selective hMC3R, hMC4R, and hMC5R analogues.' Med. Chem. (2003) 46:4965–4973.
   Google Scholar
• •A peptide MC5R antagonist is reported.
   Google Scholar
• HAN G, QUILLAN JM, CARLSON K et al.: Design of novel chimeric melanotropin-deltorphin analogues. Discovery of the first potent human melanocortin 1 receptor antagonist. Med . Chem. (2003) 46:810–819.
   Google Scholar
• •A peptide MC1R antagonist is reported.
   Google Scholar
• KOIKOV LN, EBETINO FH, SOLINSKY MG et al.: Sub-nanomolar hMC1R agonists by end-capping of the melanocortin tetrapeptide His-D-Phe-Arg-NH2. Bioorg. Med. Chem. Lett. (2003) 13:2647–2650.
   PubMed Web of Science ®Google Scholar
• GRIECO P, ROSSI C, COLOMBO G et al.: Novel a-melanocyte-stimulating hormone peptide analogues with high candidacidal activity.' Med. Chem. (2003) 46:850–855.
   Web of Science ®Google Scholar