MT1 Human Melatonin GPCR Cell Based Antagonist Arrestin LeadHunter Assay - US

Background Information:

Melatonin receptors belong to the superfamily of G protein-coupled seven transmembrane proteins. G-protein-coupled receptors 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. Melatonin, present primarily in central nervous system, is released following a circadian rhythm with high levels at night.. It is also a highly potent antioxidative substance, reducing the damage caused by free radicals generated by light and beta-amyloid peptide.

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:

Melatonin

Class:

Class A

Coupling:

Gi/Go

Protein Name:

MT1

Uniprot Number:

P48039

Protein Aliases:

Mel1a receptor

Gene Name:

MTNR1A

Gene ID:

4543

Gene Aliases:

MEL-1A-R

Accession Number:

NM_005958

Organism:

Human

Cell Type:

CHO-K1