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Combinatorial diffusion assay used to identify topically active melanocyte-stimulating hormone receptor antagonists.

J M Quillan·C K Jayawickreme·M R Lerner
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Abstract

alpha-Melanocyte-stimulating hormone (alpha-MSH) is implicated in pigmentation, central nervous system and immune system functions, growth, mitogenesis, and melanoma. Evaluation of these roles has been hindered by the lack of alpha-MSH antagonists. A combinatorial chemistry-based diffusion assay is used to find random tripeptides that antagonize normal frog and human melanoma MSH receptors and to identify pharmacological groups responsible for receptor interaction. The alpha-MSH antagonist D-Trp-Arg-Leu-NH2 is used to demonstrate directly the contribution of MSH to normal skin tone in frogs following injection or topical application.

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Amino Acid SequenceAnimalsCells, CulturedCyclic AMPDiffusionDrug DesignHumansMelanocyte-Stimulating HormonesMelanomaMelanophoresMolecular Sequence DataOligopeptidesReceptors, Pituitary HormoneSkinSkin Physiological PhenomenaSkin PigmentationStructure-Activity RelationshipTumor Cells, CulturedXenopus laevisJournal Article

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J M Quillan, C K Jayawickreme, M R Lerner. 1995-03-28. Combinatorial diffusion assay used to identify topically active melanocyte-stimulating hormone receptor antagonists.. https://doi.org/10.1073/pnas.92.7.2894

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