G protein-coupled receptors: structure-and function-based drug discovery

D Yang, Q Zhou, V Labroska, S Qin… - Signal transduction and …, 2021 - nature.com
As one of the most successful therapeutic target families, G protein-coupled receptors
(GPCRs) have experienced a transformation from random ligand screening to knowledge …

Protective role of IGF-1 and GLP-1 signaling activation in neurological dysfunctions

S Bhalla, S Mehan, A Khan, MU Rehman - Neuroscience & Biobehavioral …, 2022 - Elsevier
Abstract Insulin-like growth factor-1 (IGF-1), a pleiotropic polypeptide, plays an essential role
in CNS development and maturation. Glucagon-like peptide-1 (GLP-1) is an endogenous …

GPCR activation mechanisms across classes and macro/microscales

AS Hauser, AJ Kooistra, C Munk… - Nature structural & …, 2021 - nature.com
Two-thirds of human hormones and one-third of clinical drugs activate~ 350 G-protein-
coupled receptors (GPCR) belonging to four classes: A, B1, C and F. Whereas a model of …

Structural insights into multiplexed pharmacological actions of tirzepatide and peptide 20 at the GIP, GLP-1 or glucagon receptors

F Zhao, Q Zhou, Z Cong, K Hang, X Zou… - Nature …, 2022 - nature.com
Glucose homeostasis, regulated by glucose-dependent insulinotropic polypeptide (GIP),
glucagon-like peptide-1 (GLP-1) and glucagon (GCG) is critical to human health. Several …

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 …

Mechanisms of adhesion G protein–coupled receptor activation

A Vizurraga, R Adhikari, J Yeung, M Yu… - Journal of Biological …, 2020 - ASBMB
Adhesion G protein–coupled receptors (AGPCRs) are a thirty-three-member subfamily of
Class B GPCRs that control a wide array of physiological processes and are implicated in …

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 …

Structure and dynamics of the CGRP receptor in apo and peptide-bound forms

TM Josephs, MJ Belousoff, YL Liang, SJ Piper, J Cao… - Science, 2021 - science.org
INTRODUCTION G protein–coupled receptors (GPCRs) are key regulators of information
transmission between cells and organs. Among these, class B1 GPCRs are activated by …

Structural perspective of class B1 GPCR signaling

Z Cong, YL Liang, Q Zhou, S Darbalaei, F Zhao… - Trends in …, 2022 - cell.com
Class B1 G protein-coupled receptors (GPCRs) play important roles in human physiology
and disease pathology. Using cryo-electron microscopy (cryo-EM) and X-ray …