CGRP (CLR/RAMP1) Human Calcitonin GPCR Cell Based Agonist cAMP LeadHunter Assay - US

Background Information:

The calcitonin family of bioactive peptides comprises of calcitonin, amylin, two calcitonin-gene related peptides (CGRP1, and CGRP2) and adrenomedullin. Adrenomedullin is a 52-aa hypotensive peptide. It has structural similarity with CGRP and amylin. ADM is produced in peripheral tissues, adrenal medulla, lung, and kidney. Co-expression of receptor activity modifying protein RAMP2 and RAMP3 with calcitonin receptor-like receptor (CRLR) has been identified respectively as the adrenomedullin receptor 1 (AMR1) designated the CRLR/RAMP2 receptor and the adrenomedullin receptor 2 (AMR2) denoted as the CRLR/RAMP3 receptor. The three known RAMP isoforms (1-3) have been identified as distinct gene products and are required for receptor plasma membrane expression as well as for determination of CRLR receptor phenotype and specificity. Adrenomedullin receptors are coupled to the Gs protein resulting in elevation of intracellular cAMP, Ca2+ mobilization and nitric oxide production. Adrenomedullin receptor agonism may result in hypotension associated with cardiac inotropic activity, angiogenesis and mitogenic activity promoting human malignancies. Adrenomedullin receptor antagonism may find therapeutic use in the treatment of heart disease, cerebral vascular disease, type I diabetes and immune disorder, sepsis and cancer.

cAMP Hunter™ Gs cell lines overexpress naturally Gs coupled, wild type GPCRs and are designed to detect increases in intracellular cAMP levels in response to agonist stimulation of the receptor. These cell lines are designed to be used in conjunction with the HitHunter® cAMP Assay Detection Kit.

Family:

GPCR

Sub Family:

Calcitonin

Class:

Class B

Coupling:

Gs

Protein Name:

CLR

Uniprot Number:

Q16602

Protein Aliases:

Calcitonin receptor-like receptor

Gene Name:

CALCRL

Gene ID:

10203

Gene Aliases:

CGRPR|CRLR

Accession Number:

AY389506

Organism:

Human

Cell Type:

CHO-K1