Pharmacological characterisation of erenumab, Aimovig, at two calcitonin gene-related peptide responsive receptors.

ABSTRACT:

Background and purpose

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 and receptor activity-modifying protein 1 (RAMP1); the AMY₁ receptor comprises the calcitonin receptor 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 AMY₁ receptor. However, it is difficult to estimate its selectivity because direct comparisons between receptors under match

SUBMITTER: Garelja ML 

PROVIDER: S-EPMC10840612 | biostudies-literature | 2024 Jan

REPOSITORIES: biostudies-literature