title: Progress in the development of melanocortin receptor selective ligands.
abstract: The melanocortin pathway consists of endogenous agonists, antagonists, G-protein coupled receptors (GPCRs), and auxiliary proteins. This pathway has been identified to participate physiologically in numerous biological pathways including energy homeostasis, pigmentation, sexual function, inflammation, cardiovascular function, adrenal function, sebaceous gland lipid production, just to list a few. During this past decade, a clear link between the melanocortin-4 receptor (MC4R) and obesity, in both mice and humans via the regulation of food intake and energy homeostasis, has made this pathway the target of many academic and industrial research endeavors in attempts to develop potent and selective MC4R small molecules as anti-obesity therapeutic agents. Herein, we attempt to summarize the known proteins that constitute the melanocortin system and discuss advances in peptide and non-peptide drug discovery.
authors.affiliation: University of Florida, Department of Medicinal Chemistry, PO Box 100485, Gainesville, FL 32610-0485, USA. jholder@amgen.com
authors.forename: Boman G
authors.initials: BG
authors.lastname: Irani
authors.forename: Jerry R
authors.initials: JR
authors.lastname: Holder
authors.forename: Aleksandar
authors.initials: A
authors.lastname: Todorovic
authors.forename: Andrzej M
authors.initials: AM
authors.lastname: Wilczynski
authors.forename: Christine G
authors.initials: CG
authors.lastname: Joseph
authors.forename: Krista R
authors.initials: KR
authors.lastname: Wilson
authors.forename: Carrie
authors.initials: C
authors.lastname: Haskell-Luevano
mesh_terms: D000818:Animals; D006801:Humans; D008024:Ligands; D010455:Peptides / Q000737:chemistry / Q000494:pharmacology; D044101:Receptors, Melanocortin / Q000819:agonists* / Q000037:antagonists & inhibitors* / Q000235:genetics; D013329:Structure-Activity Relationship
chemical_list: D008024:Ligands; D010455:Peptides; D044101:Receptors, Melanocortin