The major pharmacophore for the melanocortin 1, 3, 4 and 5 receptors is the sequence -His-Phe-Arg-Trp-. There is a need for potent, biologically stable, receptor selective ligands, both agonists and antagonists, for these receptors. In this report we briefly examine the structural and biophysical approaches we have taken to develop selective agonist and antagonist ligands that can cross (or not) the blood brain barrier. Remaining questions and unmet needs are also discussed.
- Agonists and antagonists for MCR
- Melanocortin receptor ligand SAR
- Melanocortin receptor selective ligand
- Orthosteric and allosteric ligand
- Selective ligand for MCR
ASJC Scopus subject areas