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 …
(GPCRs) have experienced a transformation from random ligand screening to knowledge …
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 …
GPCR activation mechanisms across classes and macro/microscales
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 …
coupled receptors (GPCR) belonging to four classes: A, B1, C and F. Whereas a model of …
MolAICal: a soft tool for 3D drug design of protein targets by artificial intelligence and classical algorithm
Deep learning is an important branch of artificial intelligence that has been successfully
applied into medicine and two-dimensional ligand design. The three-dimensional (3D) …
applied into medicine and two-dimensional ligand design. The three-dimensional (3D) …
Biased signalling: from simple switches to allosteric microprocessors
G protein-coupled receptors (GPCRs) are the largest class of receptors in the human
genome and some of the most common drug targets. It is now well established that GPCRs …
genome and some of the most common drug targets. It is now well established that GPCRs …
How ligands illuminate GPCR molecular pharmacology
G protein-coupled receptors (GPCRs), which are modulated by a variety of endogenous and
synthetic ligands, represent the largest family of druggable targets in the human genome …
synthetic ligands, represent the largest family of druggable targets in the human genome …
GPCR dynamics: structures in motion
The function of G protein-coupled receptors (GPCRs) which represent the largest class of
both human membrane proteins and drug targets depends critically on their ability to …
both human membrane proteins and drug targets depends critically on their ability to …
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 …
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 …
Molecular basis of β-arrestin coupling to formoterol-bound β1-adrenoceptor
Y Lee, T Warne, R Nehmé, S Pandey… - Nature, 2020 - nature.com
Abstract The β1-adrenoceptor (β1AR) is a G-protein-coupled receptor (GPCR) that couples
to the heterotrimeric G protein Gs. G-protein-mediated signalling is terminated by …
to the heterotrimeric G protein Gs. G-protein-mediated signalling is terminated by …