2004Drugs of the FutureRequires access

The MC4 receptor as a therapeutic target

Shigeyuki Chaki, A. Nakazato

Open publisher page 11 citations

Abstract

Melanocortins, which are derived from pro-opiomelanocortin (POMC) by enzymatic processing, are involved in a wide range of physiological events. The melanocortins exert their effects by binding to melanocortin receptors. To date, five receptor subtypes, MC 1 -MC 5 , all of which are G-protein-coupled receptors, have been cloned. Of these, the MC 4 receptor, the expression of which is restricted to the central nervous system (CNS), is of interest in terms of the central regulation of feeding behavior and energy homeostasis. Recent findings on the distribution of the receptor in the brain and studies with selective agonists/antagonists have underscored its role in stress responses, the development of addiction, nociception and sexual function. The MC 4 receptor may therefore be an attractive target for the treatment of many CNS-related disorders, such as obesity, cachexia, depression/anxiety, drug addiction, pain and sexual dysfunction.

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What this paper is about

Melanocortins, which are derived from pro-opiomelanocortin (POMC) by enzymatic processing, are involved in a wide range of physiological events. The melanocortins exert their effects by binding to melanocortin receptors. To date, five receptor subtypes, MC 1 -MC 5 , all of which are G-protein-coupled receptors, have been cloned. Of these, the MC 4 receptor, the expression of which is restricted to the central nervous system (CNS), is of interest in terms of the central regulation of feeding behavior and energy homeostasis. Recent findings on the distribution of the receptor in the brain and studies with selective agonists/antagonists have underscored its role in stress responses, the development of addiction, nociception and sexual function. The MC 4 receptor may therefore be an attractive target for the treatment of many CNS-related disorders, such as obesity, cachexia, depression/anxiety, drug addiction, pain and sexual dysfunction.

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Available abstract

Melanocortins, which are derived from pro-opiomelanocortin (POMC) by enzymatic processing, are involved in a wide range of physiological events. The melanocortins exert their effects by binding to melanocortin receptors. To date, five receptor subtypes, MC 1 -MC 5 , all of which are G-protein-coupled receptors, have been cloned. Of these, the MC 4 receptor, the expression of which is restricted to the central nervous system (CNS), is of interest in terms of the central regulation of feeding behavior and energy homeostasis. Recent findings on the distribution of the receptor in the brain and studies with selective agonists/antagonists have underscored its role in stress responses, the development of addiction, nociception and sexual function. The MC 4 receptor may therefore be an attractive target for the treatment of many CNS-related disorders, such as obesity, cachexia, depression/anxiety, drug addiction, pain and sexual dysfunction.

Key concepts: Melanocortins, Melanocortin, Melanocortin 4 receptor, Receptor, Energy homeostasis, Endocrinology, Internal medicine, Addiction

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