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 …
AlphaFold2 versus experimental structures: evaluation on G protein-coupled receptors
As important drug targets, G protein-coupled receptors (GPCRs) play pivotal roles in a wide
range of physiological processes. Extensive efforts of structural biology have been made on …
range of physiological processes. Extensive efforts of structural biology have been made on …
Structural perspective of class B1 GPCR signaling
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 …
and disease pathology. Using cryo-electron microscopy (cryo-EM) and X-ray …
[HTML][HTML] Delineating the activation mechanism and conformational landscape of a class BG protein-coupled receptor glucagon receptor
Y Wang, M Li, W Liang, X Shi, J Fan, R Kong… - Computational and …, 2022 - Elsevier
Class BG protein-coupled receptors (GPCRs) are important targets in the treatment of
metabolic syndrome and diabetes. Although multiple structures of class B GPCRs–G protein …
metabolic syndrome and diabetes. Although multiple structures of class B GPCRs–G protein …
Pharmacological characterisation of erenumab, Aimovig, at two calcitonin gene‐related peptide responsive receptors
ML Garelja, TI Alexander, A Bennie… - British journal of …, 2024 - Wiley Online Library
Abstract Background and Purpose Calcitonin gene‐related peptide (CGRP) is involved in
migraine pathophysiology. CGRP can signal through two receptors. The canonical CGRP …
migraine pathophysiology. CGRP can signal through two receptors. The canonical CGRP …
G-Protein coupled receptors: structure and function in drug discovery
The G-protein coupled receptors (GPCRs) superfamily comprise similar proteins arranged
into families or classes thus making it one of the largest in the mammalian genome. GPCRs …
into families or classes thus making it one of the largest in the mammalian genome. GPCRs …
Allosteric interactions in the parathyroid hormone GPCR–arrestin complex formation
Peptide ligands of class B G-protein-coupled receptors act via a two-step binding process,
but the essential mechanisms that link their extracellular binding to intracellular receptor …
but the essential mechanisms that link their extracellular binding to intracellular receptor …
The G protein-first mechanism for activation of the class B glucagon-like peptide 1 receptor coupled to N-terminal domain-mediated conformational progression
Recently, there has been a great deal of excitement about new glucagon-like peptide 1
receptor (GLP-1R) agonists (eg, semaglutide and tirzepatide) that have received FDA …
receptor (GLP-1R) agonists (eg, semaglutide and tirzepatide) that have received FDA …
Capturing peptide–GPCR interactions and their dynamics
A Kaiser, I Coin - Molecules, 2020 - mdpi.com
Many biological functions of peptides are mediated through G protein-coupled receptors
(GPCRs). Upon ligand binding, GPCRs undergo conformational changes that facilitate the …
(GPCRs). Upon ligand binding, GPCRs undergo conformational changes that facilitate the …
In silico ligand docking approaches to characterise the binding of known allosteric modulators to the glucagon-like peptide 1 receptor and prediction of ADME/Tox …
The glucagon-like peptide 1 receptor (GLP-1R) is a member of the family (or class) B G-
protein-coupled receptor (GPCR). The receptor is a regulator of insulin and a key target in …
protein-coupled receptor (GPCR). The receptor is a regulator of insulin and a key target in …