Binding and cAMP studies of melanotropin peptides with the cloned human peripheral melanocortin receptor, hMC1R.
Binding and stimulation of cAMP by the melanotropin peptides alpha-MSH (alpha-melanocyte-stimulating hormone) and its superpotent analogues [Nle4, DPhe7]alpha-MSH (MT-I) and Ac-[Nle4,[formula: see text]alpha-MSH4-10-NH2 (MT-II) were undertaken to examine their respective properties on the human peripheral melanocyte melanocortin receptor, hMC1R. alpha-MSH was found to possess a binding IC50 value of 6.5 +/- 0.9 x 10(-9) M and cAMP EC50 value of 2.0 +/- 0.6 x 10(-9) M. MT-I possesses a binding IC50 value of 1.2 +/- 0.3 x 10(-9) M and a cAMP EC50 of 0.5 +/- 0.03 x 10(-9) M. MT-II possesses a binding IC50 of 0.57 +/- 0.08 x 10(-9) M and cAMP EC50 value of 0.20 +/- 0.05 x 10(-9) M.
Department of Chemistry, University of Arizona, Tucson 85721.
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Haskell-Luevano
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Miwa
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Dickinson
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Hruby
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Yamada
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Gantz
D000345:Affinity Labels; D000595:Amino Acid Sequence; D000818:Animals; D001667:Binding, Competitive; D001681:Biological Assay; D003001:Cloning, Molecular; D000242:Cyclic AMP / Q000378:metabolism*; D006801:Humans; D007700:Kinetics; D007739:L Cells; D008116:Lizards; D009074:Melanocyte-Stimulating Hormones / Q000494:pharmacology*; D008544:Melanocytes / Q000378:metabolism; D051379:Mice; D008969:Molecular Sequence Data; D010446:Peptide Fragments / Q000138:chemical synthesis / Q000494:pharmacology*; D010456:Peptides, Cyclic / Q000494:pharmacology; D011898:Ranidae; D018043:Receptors, Corticotropin / Q000096:biosynthesis / Q000378:metabolism*; D044101:Receptors, Melanocortin; D011994:Recombinant Proteins / Q000096:biosynthesis / Q000378:metabolism; D012867:Skin / Q000187:drug effects; D012879:Skin Physiological Phenomena; D013329:Structure-Activity Relationship; D014162:Transfection; D000521:alpha-MSH / Q000031:analogs & derivatives / Q000378:metabolism
D000345:Affinity Labels; D010446:Peptide Fragments; D010456:Peptides, Cyclic; D018043:Receptors, Corticotropin; D044101:Receptors, Melanocortin; D011994:Recombinant Proteins; D000521:alpha-MSH; C027756:MSH, 4-Nle-7-Phe-alpha-; D009074:Melanocyte-Stimulating Hormones; D000242:Cyclic AMP