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The melanocortin peptides that include the ฮฑ-, ฮฒ-, ฮณ-melanocyte stimulating hormones (MSH) and adrenocorticotrophin (ACTH) all possess a His-Phe-Arg-Trp epitope that is known as the 'message' sequence. These peptides are responsible for a range of physiological actions including skin pigmentation, energy homeostasis and adrenocortical steroidogenesis. Five melanocortin receptors have been identified to date, with the MC1R receptor involved in skin pigmentation. As the bioactive conformation of the MSH peptides is based on a peptide ฮฒturn, a recent study has focused on the synthesis of a library of small molecules based upon this structural feature (Compounds That Activate the Mouse Melanocortin-1 Receptor Identified by Screening a Small Molecule Library Based upon the ฮฒ-Turn, C. Haskell-Luevano et al., J. Med. Chem., 42, (1999), 4380-4387).
951 compounds (1) were prepared using solid-phase synthetic methods with side-chains based on structures known to be important for receptor recognition and activation. The compounds were evaluated for their ability to activate the melanocortin-1 receptor subtype when tested at 10 ยตM in a colourimetric bioassay.
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