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Papers of the Week

Papers: 12 Aug 2023 - 18 Aug 2023

Basic Science

In Vitro Studies, Molecular/Cellular, Neurobiology, Pharmacology/Drug Development


2023 Aug 14

Br J Pharmacol


Pharmacological characterisation of erenumab, Aimovig, at two CGRP responsive receptors.


Garelja ML, Alexander TI, Bennie A, Nimick M, Petersen J, Walker CS, Hay DL


Calcitonin gene-related peptide (CGRP) is involved in migraine pathophysiology. CGRP can signal through two receptors. The canonical CGRP receptor comprises the calcitonin receptor-like receptor (CLR) and receptor activity-modifying protein 1 (RAMP1); the AMY receptor comprises the calcitonin receptor (CTR) with RAMP1. Drugs that reduce CGRP activity, such as receptor antagonists, are approved for the treatment and prevention of migraine. Despite being designed to target the canonical CGRP receptor, emerging evidence suggests that these antagonists, including erenumab (a monoclonal antibody antagonist) can also antagonise the AMY receptor. However, it is difficult to estimate its selectivity between receptors because direct comparisons between receptors under matched conditions have not been made. We therefore characterised erenumab at both CGRP-responsive receptors with multiple ligands, including αCGRP and βCGRP.