CGRPR/CRE Luciferase Reporter HEK293 Cell Line
Recombinant HEK293 cell line stably expressing full-length human calcitonin receptor-like receptor (CALCRL/CRLR/CLR; accession number: NM_005795) and firefly luciferase under the control of a multimerized cAMP response element (CRE). This cell line can be used to measure the EC50 and IC50 of CGRP receptor agonists and antagonists using luciferase reporter activity as read-out.
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Materials Required for Cell Culture
Name | Ordering Information |
Thaw Medium 1 | BPS Bioscience #60187 |
Growth Medium 1G | BPS Bioscience #79544 |
Materials Required for Cellular Assay
Name | Ordering Information |
Thaw Medium 1 | BPS Bioscience #60187 |
Growth Medium 1G | BPS Bioscience #79544 |
MEM medium for preparing assay medium | Hyclone #SH30024.01 |
Bovine Serum Albumin (BSA, protease free) | Sigma #A4919 |
Human α-CGRP | Sigma #C0167 |
Human β- CGRP | Cayman Chemical #24725 |
Rimegepant | Cayman Chemical #26338 |
Zavegepant (Vazegepant) Hydrochloride | |
Eptinezumab | Invitrogen #MA5-42119 |
Galcanezumab | Invitrogen #MA5-42106 |
Anti-CALCRL antibody | Aviva #APR42260 |
PE Donkey Anti-Rabbit Antibody | Biolegend #406421 |
ONE-Step™ Luciferase Assay System | BPS Bioscience #60690 |
Luminometer |
The cell line has been screened to confirm the absence of Mycoplasma species.
Calcitonin gene-related peptide (CGRP) receptor is a G-protein coupled receptor with three components: calcitonin receptor-like receptor (CALCRL), receptor activity-modifying protein (RAMP1) and CGRP-receptor component protein (CRCP). RAMP1 is required for both the trafficking of the calcitonin-like receptor to the plasma membrane and the coupling of the receptor with CGRP agonist. CRCP is involved in the association between the CGRP receptor and the G protein. Upon ligand binding, the complex interacts with the G protein, the Gαs subunit dissociates from the complex and activates adenylyl cyclase, which produces cAMP. Elevation of the intracellular concentration of cAMP stimulates cAMP-dependent signaling pathways, ultimately resulting in transcription factor cAMP response element binding protein (CREB) to bind to the CRE promoter and induce gene expression.
Figure 1: Mechanism of action of CGRP.
Preclinical evidence suggests that during a migraine, activated sensory neurons in the trigeminal ganglion release CGRP from their projecting nerve endings located within the meninges. The released CGRP then binds and activates CGRP receptors causing vasodilation and plasma extravasation. Further evidence comes from the observation that intravenous administration of α-CGRP induces a headache in susceptible individuals. Recent breakthroughs in understanding the role of CGRP in migraine has led to the development of a novel class of CGRP antagonist biologics that promise significant improvement over conventional pharmacotherapy