Design of novel melanotropin agonists and antagonists with high potency and selectivity for human melanocortin receptors.
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.
Cai
Minying
M
Biochemistry and Molecular Biophysics, University of Arizona, Tucson, AZ 85721, USA.
Mayorov
Alexander V
AV
Ying
Jinfa
J
Stankova
Magda
M
Trivedi
Dev
D
Cabello
Chris
C
Hruby
Victor J
VJ
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
D008024:Ligands; D044101:Receptors, Melanocortin; D009074:Melanocyte-Stimulating Hormones