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 …

Amylin: pharmacology, physiology, and clinical potential

DL Hay, S Chen, TA Lutz, DG Parkes, JD Roth - Pharmacological reviews, 2015 - ASPET
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 …

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

IB Kotliar, E Lorenzen, JM Schwenk, DL Hay… - Pharmacological …, 2023 - ASPET
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 …

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 …

Receptor activity-modifying proteins (RAMPs): new insights and roles

DL Hay, AA Pioszak - Annual review of pharmacology and …, 2016 - annualreviews.org
It is now recognized that G protein–coupled receptors (GPCRs), once considered largely
independent functional units, have a far more diverse molecular architecture. Receptor …

Rules of engagement: GPCRs and G proteins

A Glukhova, CJ Draper-Joyce… - ACS pharmacology & …, 2018 - ACS Publications
G protein-coupled receptors (GPCRs) are a key drug target class. They account for over one-
third of current pharmaceuticals, and both drugs that inhibit and promote receptor function …

Regulation of signal transduction by calcitonin gene-related peptide receptors

CS Walker, AC Conner, DR Poyner, DL Hay - Trends in pharmacological …, 2010 - cell.com
Calcitonin gene-related peptide (CGRP) plays a pivotal role in migraine, activating its
cognate receptor to initiate intracellular signalling. This atypical receptor comprises a distinct …

Calcitonin gene-related peptide (CGRP) and its role in hypertension

SJ Smillie, SD Brain - Neuropeptides, 2011 - Elsevier
Hypertension is still presently the number one “silent killer” in the Western World, and a
major risk factor for the development of secondary diseases contributing to cardiovascular …

Allostery and biased agonism at class BG protein-coupled receptors

D Wootten, LJ Miller, C Koole, A Christopoulos… - Chemical …, 2017 - ACS Publications
Class BG protein-coupled receptors (GPCRs) respond to paracrine or endocrine peptide
hormones involved in control of bone homeostasis, glucose regulation, satiety, and gastro …

Amylin structure–function relationships and receptor pharmacology: implications for amylin mimetic drug development

RL Bower, DL Hay - British journal of pharmacology, 2016 - Wiley Online Library
Amylin is an important, but poorly understood, 37 amino acid glucoregulatory hormone with
great potential to target metabolic diseases. A working example that the amylin system is …