Progress in the development of melanocortin receptor selective ligands

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

Research output: Contribution to journalReview article


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.

Original languageEnglish (US)
Pages (from-to)3443-3479
Number of pages37
JournalCurrent pharmaceutical design
Issue number28
StatePublished - Oct 28 2004

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery

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  • Cite this

    Irani, B. G., Holder, J. R., Todorovic, A., Wilczynski, A. M., Joseph, C. G., Wilson, K. R., & Haskell-Luevano, C. (2004). Progress in the development of melanocortin receptor selective ligands. Current pharmaceutical design, 10(28), 3443-3479.