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For all the melanocortin receptors, binding of an agonistic ligand activates the receptor, leading to dissociation of the G protein and activation of the enzyme adenyl cyclase. Adenyl cyclase then cleaves ATP to generate the second messenger cyclic AMP (cAMP), which in turn activates multiple downstream pathways.
Melanocortin receptors are members of the rhodopsin family of 7-transmembrane G protein-coupled receptors. There are five known members of the melanocortin receptor system [ 1 ] each with differing specificities for melanocortins : [ 2 ] [ 3 ] [ 4 ]
Melanocortin 4 receptor (MC 4 R) is a melanocortin receptor that in humans is encoded by the MC4R gene highly expressed in paraventricular nucleus of the hypothalamus. [ 5 ] [ 6 ] [ 7 ] It encodes the MC 4 R protein, a G protein-coupled receptor (GPCR) that binds α-melanocyte stimulating hormone (α-MSH).
The melanocortin 1 receptor (MC1R), also known as melanocyte-stimulating hormone receptor (MSHR), melanin-activating peptide receptor, or melanotropin receptor, is a G protein–coupled receptor that binds to a class of pituitary peptide hormones known as the melanocortins, which include adrenocorticotropic hormone (ACTH) and the different forms of melanocyte-stimulating hormone (MSH).
The adrenocorticotropic hormone receptor or ACTH receptor also known as the melanocortin receptor 2 or MC 2 receptor is a type of melanocortin receptor (type 2) which is specific for ACTH. [5] A G protein–coupled receptor located on the external cell plasma membrane, it is coupled to G αs and upregulates levels of cAMP by activating adenylyl ...
The central melanocortin system is defined anatomically as a collection of central nervous system circuits which include: Neurons that express hypothalamic neuropeptide Y and agouti gene-related protein or proopiomelanocortin (POMC) and that originate in the arcuate nucleus .
Melanocortin receptor agonists are hormones, pharmacologic agents or medications that activate, or inversely activate, one or more melanocortin receptors.
Melanocortin 2 receptor accessory protein is a transmembrane accessory protein that in humans is encoded by the MRAP gene [4] located in chromosome 21q22.11. [5] Alternate splicing of the MRAP mRNA generates two functionally isoforms MRAP-α and MRAP-β. [6] MRAP is an accessory protein to a family of five receptors called the melanocortin ...