A review of melanocortin receptor small molecule ligands

Aleksandar Todorovic, Carrie Haskell-Luevano

Research output: Contribution to journalReview articlepeer-review

45 Scopus citations


The melanocortin system (MC) is implicated in the regulation of a variety of physiological pathways including pigmentation, steroid function, energy homeostasis, food intake, obesity, cardiovascular, sexual function, and normal gland regulation. The melanocortin system consists of five receptors identified to date (MC1-5R), melanocortin agonists derived from the pro-opiomelanocortin prohormone (POMC) and two naturally existing antagonists. Melanocortin receptor ligand structure-activity studies have been performed since the 1960s, primarily focused on the pigmentation aspect of physiology. During the 1990s, the melanocortin-4 receptor was identified to play a significant physiological role in the regulation of both food intake and obesity. Subsequently, a concerted drug design effort has focused on the design and discovery of melanocortin receptor small molecules. Herein, we present an overview of melanocortin receptor heterocyclic small molecules.

Original languageEnglish (US)
Pages (from-to)2026-2036
Number of pages11
Issue number10
StatePublished - Oct 2005

Bibliographical note

Funding Information:
We thank the financial support of NIH Grants DK57080, DK64250, and DK63974. Aleksandar Todorovic is the recipient of the American Heart Association Predoctoral Fellowship.


  • Heterocyclic
  • Melanocortin
  • Peptidomimetic
  • Piperazine
  • Piperidine
  • Synthesis


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