Development of melanocortin receptor selective ligands

Boman G. Irani, Jerry R. Holder, Aleksandar Todorovic, Andrzej M. Wilezynski, Christine G. Joseph, Krista R. Wilson, Carrie Haskell-Luevano

Research output: Contribution to journalArticlepeer-review


The melanocortin pathway consists of endogenous agonists, antagonists, G-protein coupled receptors (GPCRs), and auxiliary proteins. This pathway has been identified to participate physiologically in numerous biological pathways including energy homeostasis, pigmentation, sexual function, inflammation, cardiovascular function, adrenal function, sebaceous gland lipid production, just to list a few. During this past decade, a clear link between the melanocortin-4 receptor (MC4R) and obesity, in both mice and humans via the regulation of food intake and energy homeostasis, has made this pathway the target of many academic and industrial research endeavors in attempts to develop potent and selective MC4R small molecules as anti-obesity therapeutic agents. Herein, we attempt to summarize the known proteins that constitute the melanocortin system and discuss advances in peptide and non-peptide drug discovery. All rights reserved -

Original languageEnglish (US)
Pages (from-to)285-334
Number of pages50
JournalFrontiers in Medicinal Chemistry
Issue number1
StatePublished - Jan 2006


  • Adrenocorticotropin
  • Agouti-related protein (AGRP)
  • Cortisol
  • Glucocorticoid
  • Homeostasis
  • POMC KO mice
  • Syndecan proteins

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery
  • Organic Chemistry


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