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. 1995 Mar 28;92(7):2894–2898. doi: 10.1073/pnas.92.7.2894

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

J M Quillan 1, C K Jayawickreme 1, M R Lerner 1
PMCID: PMC42325  PMID: 7708744

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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Selected References

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