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Updated: Aug 16, 2026

Pharmacologic Induction of Epidermal Melanin and Protection Against Sunburn in a Humanized Mouse Model
Published on: September 7, 2013
A review of melanocortin receptor small molecule ligands
Aleksandar Todorovic1, Carrie Haskell-Luevano
1Department of Medicinal Chemistry, University of Florida, P.O. Box 100485, Gainesville, FL 32610, USA.
Abstract:
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.
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