Melanocortin receptors (MCRs) are members of the rhodopsin-like G protein-coupled receptors family with 7-transmembrane domains. MCRs can be activated by members of the melanocortin derivatives of precursor peptide proopiomelanocortin (POMC), including α-Melanocyte-stimulating hormone (α-MSH), β-MSH, γ-MSH and adrenocorticotrophin (ACTH). These receptors are inhibited by endogenous inverse agonists agouti signaling peptide and agouti-related peptide. There are five known subtypes of MCRs, namely MC1R, MC2R, MC3R, MC4R, MC5R. Different melanocortin receptor presents distinct tissue distributions throughout the nervous system and periphery and distinct selectivity for the various melanocortin peptides. Activation of all five receptors results in adenylate cyclase activity and cAMP production. The multiple physiologic roles of MCRs reveal their irreplaceable status in evolutionary history. MC1R is associated with pigmentation genetics, MC2R in steroidogenesis, and MC5R has an exocrine function especially in sebaceous gland secretion. Abundant in brain, MC3R and MC4R play key roles in energy homeostasis. Mutations in MC4R are the most common cause of autosomal dominant obesity. More recently, fat mass, weight, risk of obesity, and insulin resistance are associated with common variants near the MC4R locus.
Here show five subtypes of MCRs (MC1R to MC5R). The distribution may be a parameter to distinguish different MCRs. MC1R is mainly expressed in melanocytes and preferentially binds α-MSH; MC2R in the adrenal cortex and mainly binds ACTH; MC3R and MC4R in the nervous system, and MC5R in sebaceous glands and other tissues, e.g., the brain, muscles, lung and kidney. Based on MCRs, a lot of synthetic agonists are under clinical development because of the significance in diagnostic test.
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