MC1 Human Melanocortin GPCR Cell Based Agonist Arrestin LeadHunter Assay - US

Background Information:

Melanocortin receptors (MCRs) belong to the superfamily of seven transmembrane G-protein-coupled receptors, which constitute one of the major signal transduction systems in eukaryotic cells. Coding sequences for these receptors, in those regions believed to contribute to the agonist-antagonist binding site, are strongly conserved across mammalian species. The melanocortin system and their receptors are involved in a wide range of physiological functions, including pigmentation, energy homeostasis, inflammation, immunomodulation, steroidogenesis, sexual function and temperature control. The melanocortin MC1 receptor is made primarily in melanocytes, MC2 in adrenal cortex, MC3 and MC4 almost exclusively neuronal, and MC5 in exocrine gland cells. Melanocortin MC1 receptor agonism may increase the risk of developing melanoma and nonmelanoma skin cancer beyond their effects on pigmentation phenotype.

PathHunter β-Arrestin GPCR cell lines are engineered to co-express the ProLink™ (PK) tagged GPCR and the Enzyme Acceptor (EA) tagged β-Arrestin. Activation of the GPCR-PK induces β-Arrestin-EA recruitment, forcing complementation of the two β-galactosidase enzyme fragments (EA and PK). The resulting functional enzyme hydrolyzes substrate to generate a chemiluminescent signal.

Family:

GPCR

Sub Family:

Melanocortin

Class:

Class A

Coupling:

Gs

Protein Name:

MC1

Uniprot Number:

Q01726

Protein Aliases:

alpha melanocyte stimulating hormone receptor

Gene Name:

MC1R

Gene ID:

4157

Gene Aliases:

MSH-R|MSHR

Accession Number:

NM_002386

Organism:

Human

Cell Type:

U2OS