Frontiers in Medicinal Chemistry

Volume: 9

The Potential Application of Melanotropin Ligands for the Treatment of Obesity and Related Disorders: Potential and Problems

Author(s): Victor J. Hruby and Minying Cai

Pp: 161-181 (21)

DOI: 10.2174/9781681082493116090007

* (Excluding Mailing and Handling)


Considerable scientific evidence has been obtained that suggests that the melanocortin 3 and melanocortin 4 receptors are critically involved in energy balance and feeding behavior in animals, including humans. The natural ligands for these receptors are processed products of the gene pro-opiomelanocortin (POMC) and include α-, β- and γ- melanocyte stimulating hormones and possibly other POMC products. Hence, it has been postulated that selective agonists and antagonists might serve as drugs for the treatment of feeding disorders. At the same time, it was found that melanotropin peptides can have other biological activities related to the MC3R and MC4R, and that some of these activities, such as blood pressure changes, need to be modulated in order to be useful drugs without unwarranted side effects. Current progress in these efforts will be discussed along with possible new directions that might be useful in these important areas of biology and medicine.

Keywords: AGRP, anorexia, melanocortin genes, melanotropin peptides, MC3R. MC4R, obesity.

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