Abstract
The melanocortin receptors 3 and 4 control energy homeostasis, food-intake behavior, and correlated pathophysiological conditions. The melanocortin-4 receptor (MC4R) has been broadly investigated. In contrast, the knowledge related to physiological roles of the melanocortin-3 receptor (MC3R) is lacking because of the limited number of known MC3R selective ligands. Here, we report the design, synthesis, biological activity, conformational analysis, and docking with receptors of two potent and selective agonists at the human MC3 receptor.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Cyclic AMP / biosynthesis
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HEK293 Cells
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Humans
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Melanocyte-Stimulating Hormones / chemical synthesis
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Melanocyte-Stimulating Hormones / chemistry
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Melanocyte-Stimulating Hormones / pharmacology
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Models, Molecular
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Molecular Conformation
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Molecular Docking Simulation
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Oligopeptides / chemical synthesis
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Oligopeptides / chemistry*
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Oligopeptides / pharmacology
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Receptor, Melanocortin, Type 1 / metabolism
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Receptor, Melanocortin, Type 3 / agonists*
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Receptor, Melanocortin, Type 4 / metabolism
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Receptors, Melanocortin / metabolism
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Structure-Activity Relationship
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alpha-MSH / analogs & derivatives
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alpha-MSH / chemical synthesis
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alpha-MSH / chemistry
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alpha-MSH / pharmacology
Substances
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MC3R protein, human
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MC4R protein, human
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Oligopeptides
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Receptor, Melanocortin, Type 1
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Receptor, Melanocortin, Type 3
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Receptor, Melanocortin, Type 4
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Receptors, Melanocortin
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acetyl-norleucyl(4)-(aspartyl(5)-histidyl(6)-phenylalanyl(7)-arginyl(8)-tryptophyl(9)-lysyl(10))cyclo-alpha-MSH(4-10)amide
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melanocortin 5 receptor
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SHU 9119
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alpha-MSH
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Melanocyte-Stimulating Hormones
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Cyclic AMP