MC4R Cre-CREB Luciferase Reporter HEK293 Cell Line

The MC4R CRE/CREB Luciferase Reporter HEK293 Cell Line expresses full-length human MC4R (melanocortin 4 receptor) (NM_005912.3) under the control of a CMV promoter, for high constitutive expression, and an inducible firefly luciferase reporter under the control of multimerized cAMP response element (CRE), designed to monitor the activity of the cAMP/PKA signaling pathway. Upon MC4R-ligand binding, the endogenous transcription factor CREB binds to the response elements, inducing transcription of the luciferase reporter. This cell line has been validated by stimulation with alpha-MSH, beta-MSH, and Setmelanotide. Interested in screening and profiling inhibitors, blocking antibodies, or activators of MC4R without the need to purchase and license the cell line? Check out our Metabolic Diseases screening services. The Melanocortin 4 Receptor (MC4R) is a G protein-coupled receptor (GPCR) primarily expressed in the paraventricular nucleus (PVN) of the hypothalamus. It plays a critical role in the leptin-melanocortin signaling pathway, which is the body's primary mechanism for regulating energy intake (appetite) and energy expenditure (metabolism). This receptor binds the POMC (pro-opiomelanocortin)-derived peptides ACTH (adrenocorticotrophic hormone) and alpha-MSH and beta-MSH (melanocyte-stimulating hormones). Defects in this gene are a cause of autosomal dominant obesity. Setmelanotide is an FDA-approved MC4R agonist designed to bypass upstream signaling defects in patients with specific genetic obesity syndromes.