Melanocortin probes for the melanoma MC1 receptor: Synthesis, receptor binding and biological activity

M. E. Erskine-Grout, G. W.J. Olivier, P. Lucas, U. G. Sahm, S. K. Branch, S. H. Moss, L. J. Notarianni, C. W. Pouton

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Abstract

The fate of α-melanocyte-stimulating hormone (α-MSH) subsequent to binding to the melanoma melanocortin MC1 receptor is of interest with regard to its potential use in targeting cytotoxic drugs or imaging to melanoma. Tools such as iodinated, photoaffinity-labelled, biotinylated and fluorescent melanocortins are required to study the fate of the ligand during its interaction with the receptor. In this study, a series of probes for the receptor based on the potent analogue, [Nle4,Dphe7]α-MSH, have been developed end tasted for their potential usefulness. All probes contain the core melanocortin motif Hls-Phe-Arg-Trp. They bind the receptor readily and appear to have similar intrinsic efficacies to the endogenous peptide, so that biological activity is regulated by their receptor binding affinity. Functional photoaffinity-labelled, biotinylated and fluorescent probes are described. The biotinylated probe binds the receptor when coupled to streptavidin, although with reduced affinity.

Original languageEnglish
Pages (from-to)89-94
Number of pages6
JournalMelanoma Research
Volume6
Issue number2
DOIs
Publication statusPublished - 1 Jan 1996
Externally publishedYes

Keywords

  • binding affinity
  • efficacy
  • fluorescent labels
  • melanocortin probes
  • melanoma cells
  • photoaffinity labels
  • α-MSH

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