Design of novel melanocortin receptor ligands: Multiple receptors, complex pharmacology, the challenge

Victor J. Hruby, Minying Cai, James Cain, Joel Nyberg, Dev Trivedi

Research output: Contribution to journalReview article

14 Scopus citations

Abstract

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.

Original languageEnglish (US)
Pages (from-to)88-93
Number of pages6
JournalEuropean Journal of Pharmacology
Volume660
Issue number1
DOIs
StatePublished - Jun 11 2011

Keywords

  • 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

  • Pharmacology

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