title: Design of novel melanotropin agonists and antagonists with high potency and selectivity for human melanocortin receptors.
abstract: alpha-MSH and gamma-MSH are the natural endogenous hormones for the human melanocortin-1, 3, 4 and 5 receptors (hMC1R, hMC3R, hMC4R and hMC5R). These and more potent, stable and prolonged acting analogues such as NDP-alpha-MSH, MT-II and SHU-9119 are not very receptor selective. To develop potent and selective agonist and antagonist ligands for the melanocortin receptors we have used state-of-the-art biophysical studies, computational chemistry, and design of conformational and topographical constraints with novel templates.
authors.affiliation: Biochemistry and Molecular Biophysics, University of Arizona, Tucson, AZ 85721, USA.
authors.forename: Minying
authors.initials: M
authors.lastname: Cai
authors.forename: Alexander V
authors.initials: AV
authors.lastname: Mayorov
authors.forename: Jinfa
authors.initials: J
authors.lastname: Ying
authors.forename: Magda
authors.initials: M
authors.lastname: Stankova
authors.forename: Dev
authors.initials: D
authors.lastname: Trivedi
authors.forename: Chris
authors.initials: C
authors.lastname: Cabello
authors.forename: Victor J
authors.initials: VJ
authors.lastname: Hruby
mesh_terms: D015195:Drug Design; D006801:Humans; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy; D009074:Melanocyte-Stimulating Hormones / Q000819:agonists* / Q000737:chemistry / Q000494:pharmacology*; D008968:Molecular Conformation; D044101:Receptors, Melanocortin / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000502:physiology; D013329:Structure-Activity Relationship
chemical_list: D008024:Ligands; D044101:Receptors, Melanocortin; D009074:Melanocyte-Stimulating Hormones