Mechanisms of signalling and biased agonism in G protein-coupled receptors
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 …
humans that signal in response to diverse inputs and regulate a plethora of cellular …
Structural insights into G-protein-coupled receptor allostery
G-protein-coupled receptors (GPCRs) are key cell-surface proteins that transduce external
environmental cues into biochemical signals across the membrane. GPCRs are intrinsically …
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 …
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 …
of receptors that often undergo autoproteolysis to produce α and β subunits,–. A tethered …
The tethered peptide activation mechanism of adhesion GPCRs
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 …
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 …
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 …
processes such as immune responses, organ development, cellular communication …
Cryo-EM structure of the activated GLP-1 receptor in complex with a G protein
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 …
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
Glucose homeostasis, regulated by glucose-dependent insulinotropic polypeptide (GIP),
glucagon-like peptide-1 (GLP-1) and glucagon (GCG) is critical to human health. Several …
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
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 …
such as osteoporosis, diabetes and obesity. Here we report the structure of a full-length …