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 …

Development of therapeutic antibodies for the treatment of diseases

RM Lu, YC Hwang, IJ Liu, CC Lee, HZ Tsai… - Journal of biomedical …, 2020 - Springer
It has been more than three decades since the first monoclonal antibody was approved by
the United States Food and Drug Administration (US FDA) in 1986, and during this time …

Advances in therapeutic peptides targeting G protein-coupled receptors

AP Davenport, CCG Scully, C de Graaf… - Nature Reviews Drug …, 2020 - nature.com
Dysregulation of peptide-activated pathways causes a range of diseases, fostering the
discovery and clinical development of peptide drugs. Many endogenous peptides activate G …

Cryo-EM structure of an activated VIP1 receptor-G protein complex revealed by a NanoBiT tethering strategy

J Duan, D Shen, XE Zhou, P Bi, Q Liu, Y Tan… - Nature …, 2020 - nature.com
Vasoactive intestinal polypeptide receptor (VIP1R) is a widely expressed class BG protein-
coupled receptor and a drug target for the treatment of neuronal, metabolic, and …

Structural insights into differences in G protein activation by family A and family B GPCRs

D Hilger, KK Kumar, H Hu, MF Pedersen, ES O'Brien… - Science, 2020 - science.org
INTRODUCTION Transmembrane signaling of heterotrimeric guanine nucleotide–binding
protein (G protein)–coupled receptors (GPCRs) is mediated by ligand-dependent …

Differential GLP-1R binding and activation by peptide and non-peptide agonists

X Zhang, MJ Belousoff, P Zhao, AJ Kooistra, TT Truong… - Molecular Cell, 2020 - cell.com
Peptide drugs targeting class B1 G-protein-coupled receptors (GPCRs) can treat multiple
diseases; however, there remains substantial interest in the development of orally delivered …

Structure and dynamics of the active human parathyroid hormone receptor-1

LH Zhao, S Ma, I Sutkeviciute, DD Shen, XE Zhou… - Science, 2019 - science.org
The parathyroid hormone receptor-1 (PTH1R) is a class BG protein–coupled receptor
central to calcium homeostasis and a therapeutic target for osteoporosis and …

Activation of the GLP-1 receptor by a non-peptidic agonist

P Zhao, YL Liang, MJ Belousoff, G Deganutti… - Nature, 2020 - nature.com
Class B G-protein-coupled receptors are major targets for the treatment of chronic diseases,
including diabetes and obesity. Structures of active receptors reveal peptide agonists …

Structural basis of Gs and Gi recognition by the human glucagon receptor

A Qiao, S Han, X Li, Z Li, P Zhao, A Dai, R Chang, L Tai… - Science, 2020 - science.org
Class BG protein–coupled receptors, an important class of therapeutic targets, signal mainly
through the Gs class of heterotrimeric G proteins, although they do display some promiscuity …

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 …