Melanocortin GPCR Family Subtypes and Products

What Are Melanocortin Receptors?

Melanocortin receptors are a family of G protein-coupled receptors (GPCRs) comprised of five receptor subtypes: MC1, MC2, MC3, MC4, and MC5. Melanocortin receptors are involved in a variety of functions, such as addiction, energy regulation, erectile function, memory, mood, and nociception. Research is being done into the therapeutic application of MC4 antagonists in treating post-traumatic stress disorders, and its concurrent symptoms, while MC4 agonists have potential application as a weight-loss therapy. Research is also being done on MC1 and MC5 receptors, specifically their role in inflammation, emotional regulation, and neurodegenerative diseases.

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Melanocortin Receptor Information

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MC1

MC4

The melanocortin 1 receptor (MC1R), also known as melanocyte-stimulating hormone receptor (MSHR) or melanotropin receptor, is a seven transmembrane G-protein coupled receptors expressed on the surface of melanocytes MC1 receptors binds to a class of pituitary peptide hormones known as the melanocortins. Binding of melanocortins to five subtypes of melanocortin receptors exert a large array of central and peripheral effects. MC1R is one of the key proteins expressed in skin and hair and involved in regulating skin and hair color. Activation of MC1R by agonist stimulates the synthesis of eumelanin by a process melanogenesis, primarlily activating adenylate cyclase. MC1R has a potential role in anti-inflammatory and melanoma treatment. Further studies of the MC1 receptor are essential in gaining a better understanding of the mechanism and in vivo regulation of pigmentation and anti-inflammatory functions.

The melanocortin receptor MC4 is expressed in the central nervous system, gastrointestinal tract and placenta. The melanocortin family is essential in the control of body weight homeostasis, sexual behavior, and autonomic functions; MC4 receptors are primarily involved in the regulation of food uptake. MC4 agonists have great potential in the treatment of weight disorders and sexual dysfunction, whereas MC4 antagonists may be useful in the treatment of anorectic and cachectic conditions.

Melanocortin Cell Lines

Receptor FamilyReceptorSpeciesParentalStable Cell Lines Division-Arrested Cells Membranes
MelanocortinMC1humanHEK293TC1340DC1340MC1340
MC4humanHEK293TH1343H1343H1343

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