Mechanisms of signalling and biased agonism in G protein-coupled receptors

D Wootten, A Christopoulos, M Marti-Solano… - … reviews Molecular cell …, 2018 - nature.com
G protein-coupled receptors (GPCRs) are the largest group of cell surface receptors in
humans that signal in response to diverse inputs and regulate a plethora of cellular …

Structural insights into G-protein-coupled receptor allostery

DM Thal, A Glukhova, PM Sexton, A Christopoulos - Nature, 2018 - nature.com
G-protein-coupled receptors (GPCRs) are key cell-surface proteins that transduce external
environmental cues into biochemical signals across the membrane. GPCRs are intrinsically …

GPCRdb in 2021: integrating GPCR sequence, structure and function

AJ Kooistra, S Mordalski… - Nucleic Acids …, 2021 - academic.oup.com
G protein-coupled receptors (GPCRs) form both the largest family of membrane proteins and
drug targets, mediating the action of one-third of medicines. The GPCR database, GPCRdb …

Tethered peptide activation mechanism of the adhesion GPCRs ADGRG2 and ADGRG4

P **ao, S Guo, X Wen, QT He, H Lin, SM Huang, L Gou… - Nature, 2022 - nature.com
Adhesion G protein-coupled receptors (aGPCRs) constitute an evolutionarily ancient family
of receptors that often undergo autoproteolysis to produce α and β subunits,–. A tethered …

The tethered peptide activation mechanism of adhesion GPCRs

X Barros-Álvarez, RM Nwokonko, A Vizurraga… - Nature, 2022 - nature.com
Adhesion G-protein-coupled receptors (aGPCRs) are characterized by the presence of auto-
proteolysing extracellular regions that are involved in cell–cell and cell–extracellular matrix …

Structural basis for the tethered peptide activation of adhesion GPCRs

YQ **, P **ao, F Yang, RJ Zhao, SC Guo, X Yan… - Nature, 2022 - nature.com
Adhesion G-protein-coupled receptors (aGPCRs) are important for organogenesis,
neurodevelopment, reproduction and other processes,,,,–. Many aGPCRs are activated by a …

Structural basis of tethered agonism of the adhesion GPCRs ADGRD1 and ADGRF1

X Qu, N Qiu, M Wang, B Zhang, J Du, Z Zhong, W Xu… - Nature, 2022 - nature.com
Adhesion G protein-coupled receptors (aGPCRs) are essential for a variety of physiological
processes such as immune responses, organ development, cellular communication …

Cryo-EM structure of the activated GLP-1 receptor in complex with a G protein

Y Zhang, B Sun, D Feng, H Hu, M Chu, Q Qu… - Nature, 2017 - nature.com
Abstract Glucagon-like peptide 1 (GLP-1) is a hormone with essential roles in regulating
insulin secretion, carbohydrate metabolism and appetite. GLP-1 effects are mediated …

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 …

Phase-plate cryo-EM structure of a class B GPCR–G-protein complex

YL Liang, M Khoshouei, M Radjainia, Y Zhang… - Nature, 2017 - nature.com
Class B G-protein-coupled receptors are major targets for the treatment of chronic diseases,
such as osteoporosis, diabetes and obesity. Here we report the structure of a full-length …