CGRP physiology, pharmacology, and therapeutic targets: migraine and beyond

AF Russo, DL Hay - Physiological reviews, 2023 - journals.physiology.org
Calcitonin gene-related peptide (CGRP) is a neuropeptide with diverse physiological
functions. Its two isoforms (α and β) are widely expressed throughout the body in sensory …

Shared and independent roles of CGRP and PACAP in migraine pathophysiology

A Kuburas, AF Russo - The Journal of Headache and Pain, 2023 - Springer
The neuropeptides calcitonin gene-related peptide (CGRP) and pituitary adenylate cyclase-
activating polypeptide (PACAP) have emerged as mediators of migraine pathogenesis. Both …

[HTML][HTML] Tirzepatide is an imbalanced and biased dual GIP and GLP-1 receptor agonist

FS Willard, JD Douros, MBN Gabe, AD Showalter… - JCI insight, 2020 - ncbi.nlm.nih.gov
Tirzepatide (LY3298176) is a dual GIP and GLP-1 receptor agonist under development for
the treatment of type 2 diabetes mellitus (T2DM), obesity, and nonalcoholic steatohepatitis …

Mode and site of action of therapies targeting CGRP signaling

A Labastida-Ramírez, E Caronna, C Gollion… - The journal of headache …, 2023 - Springer
Targeting CGRP has proved to be efficacious, tolerable, and safe to treat migraine; however,
many patients with migraine do not benefit from drugs that antagonize the CGRPergic …

Migraine therapeutics differentially modulate the CGRP pathway

M Bhakta, T Vuong, T Taura, DS Wilson… - …, 2021 - journals.sagepub.com
Background The clinical efficacy of migraine therapeutic agents directed towards the
calcitonin-gene related peptide (CGRP) pathway has confirmed the key role of this axis in …

Elucidating the interactome of G protein-coupled receptors and receptor activity-modifying proteins

IB Kotliar, E Lorenzen, JM Schwenk, DL Hay… - Pharmacological …, 2023 - Elsevier
G protein-coupled receptors (GPCRs) are known to interact with several other classes of
integral membrane proteins that modulate their biology and pharmacology. However, the …

Structural insight into selectivity of amylin and calcitonin receptor agonists

J Cao, MJ Belousoff, E Gerrard, R Danev… - Nature Chemical …, 2024 - nature.com
Amylin receptors (AMYRs), heterodimers of the calcitonin receptor (CTR) and one of three
receptor activity-modifying proteins, are promising obesity targets. A hallmark of AMYR …

CGRP receptor antagonists for migraine. Are they also AMY1 receptor antagonists?

ML Garelja, CS Walker, DL Hay - British Journal of …, 2022 - Wiley Online Library
The development of several drugs that target the calcitonin gene‐related peptide (CGRP)
system has been a major breakthrough in the pharmacological management of migraine …

Targeting CGRP for migraine treatment: mechanisms, antibodies, small molecules, perspectives

E De Matteis, M Guglielmetti, R Ornello… - Expert review of …, 2020 - Taylor & Francis
ABSTRACT Introduction Calcitonin Gene-Related Peptide (CGRP) has gradually emerged
as a suitable therapeutic target to treat migraine. Considering the social and economic …

A narrative review of the calcitonin peptide family and associated receptors as migraine targets: Calcitonin gene‐related peptide and beyond

ML Garelja, DL Hay - Headache: The Journal of Head and …, 2022 - Wiley Online Library
Objective To summarize the pharmacology of the calcitonin peptide family of receptors and
explore their relationship to migraine and current migraine therapies. Background …