The role of melanocortins in body weight regulation: opportunities for the treatment of obesity

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• 作者：MacNeil ; Douglas J. ; Howard ; Andrew D. ; Guan ; Xiaoming ; Fong ; Tung M. ; Nargund ; Ravi P. ; Bednarek ; Maria A. ; et. al.
• 关键词：Melanocortins ; Melanocortin receptor ; Neuropeptide ; ACTH (adrenocorticotropic hormone) ; AgRP (agouti-related protein) ; POMC (proopiomelanocortin) ; Energy homeostasis ; Obesity ; Sexual function
• 刊名：European Journal of Pharmacology
• 出版年：2002
• 出版时间：April 12, 2002
• 年：2002
• 卷：440
• 期：2-3
• 页码：141-157
• 全文大小：457 K

文摘

Five G-protein-coupled melanocortin receptors (MC₁–MC₅) are expressed in mammalian tissues. The melanocortin receptors support diverse physiological functions, including the regulation of hair color, adrenal function, energy homeostasis, feed efficiency, sebaceous gland lipid production and immune and sexual function. The melanocortins (adrenocorticotropic hormone (ACTH), α-melanocyte-stimulating hormone (α-MSH), β-MSH and γ-MSH) are agonist peptide ligands for the melanocortin receptors and these peptides are processed from the pre-prohormone proopiomelanocortin (POMC). Peptide antagonists for the melanocortin MC₁, MC₃ and MC₄ receptors include agouti-related protein (AgRP) and agouti. Diverse lines of evidence, including genetic and pharmacological data obtained in rodents and humans, support a role for the melanocortin MC₃ and MC₄ receptors in the regulation of energy homeostasis. Recent advances in the development of potent and selective peptide and non-peptide melanocortin receptor ligands are anticipated to help unravel the roles for the melanocortin receptors in humans and to accelerate the clinical use of small molecule melanocortin mimetics.