Design of novel melanotropin agonists and antagonists with high potency and selectivity for human melanocortin receptors |
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Authors: | Cai Minying Mayorov Alexander V Ying Jinfa Stankova Magda Trivedi Dev Cabello Chris Hruby Victor J |
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Institution: | Biochemistry and Molecular Biophysics, University of Arizona, Tucson, AZ 85721, USA. |
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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. |
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