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 …

Update on the pharmacology of calcitonin/CGRP family of peptides: IUPHAR Review 25

DL Hay, ML Garelja, DR Poyner… - British journal of …, 2018 - Wiley Online Library
The calcitonin/CGRP family of peptides includes calcitonin, α and β CGRP, amylin,
adrenomedullin (AM) and adrenomedullin 2/intermedin (AM2/IMD). Their receptors consist …

Cryo-EM structure of the active, Gs-protein complexed, human CGRP receptor

YL Liang, M Khoshouei, G Deganutti, A Glukhova… - Nature, 2018 - nature.com
Calcitonin gene-related peptide (CGRP) is a widely expressed neuropeptide that has a
major role in sensory neurotransmission. The CGRP receptor is a heterodimer of the …

Amylin: pharmacology, physiology, and clinical potential

DL Hay, S Chen, TA Lutz, DG Parkes, JD Roth… - Pharmacological …, 2015 - Elsevier
Amylin is a pancreatic β-cell hormone that produces effects in several different organ
systems. Here, we review the literature in rodents and in humans on amylin research since …

Complex pharmacology of free fatty acid receptors

G Milligan, B Shimpukade, T Ulven… - Chemical …, 2017 - ACS Publications
G protein-coupled receptors (GPCRs) are historically the most successful family of drug
targets. In recent times it has become clear that the pharmacology of these receptors is far …

New insights into the structure and function of class B1 GPCRs

BP Cary, X Zhang, J Cao, RM Johnson… - Endocrine …, 2023 - academic.oup.com
G protein–coupled receptors (GPCRs) are the largest family of cell surface receptors. Class
B1 GPCRs constitute a subfamily of 15 receptors that characteristically contain large …

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 …

Calcitonin gene‐related peptide modulators–The history and renaissance of a new migraine drug class

R Hargreaves, J Olesen - Headache: The Journal of Head and …, 2019 - Wiley Online Library
Several lines of evidence pointed to an important role for CGRP in migraine. These included
the anatomic colocalization of CGRP and its receptor in sensory fibers innervating pain …

A structural basis for amylin receptor phenotype

J Cao, MJ Belousoff, YL Liang, RM Johnson… - Science, 2022 - science.org
Amylin receptors (AMYRs) are heterodimers of the calcitonin (CT) receptor (CTR) and one of
three receptor activity–modifying proteins (RAMPs), AMY1R, AMY2R, and AMY3R. Selective …

The activity of peptides of the calcitonin family in bone

D Naot, DS Musson, J Cornish - Physiological reviews, 2019 - journals.physiology.org
Calcitonin was discovered over 50 yr ago as a new hormone that rapidly lowers circulating
calcium levels. This effect is caused by the inhibition of calcium efflux from bone, as …