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.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, U.S. Gov't, P.H.S.
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Review
MeSH terms
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Drug Design
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Humans
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Ligands
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Magnetic Resonance Spectroscopy
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Melanocyte-Stimulating Hormones / agonists*
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Melanocyte-Stimulating Hormones / chemistry
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Melanocyte-Stimulating Hormones / pharmacology*
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Molecular Conformation
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Receptors, Melanocortin / antagonists & inhibitors*
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Receptors, Melanocortin / chemistry
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Receptors, Melanocortin / physiology
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Structure-Activity Relationship
Substances
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Ligands
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Receptors, Melanocortin
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Melanocyte-Stimulating Hormones