G protein-coupled receptors: structure-and function-based drug discovery
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 …
The interplay of glucagon-like peptide-1 receptor trafficking and signalling in pancreatic beta cells
A Marzook, A Tomas, B Jones - Frontiers in endocrinology, 2021 - frontiersin.org
The glucagon-like peptide 1 receptor (GLP-1R) is a class BG protein-coupled receptor
(GPCR) which mediates the effects of GLP-1, an incretin hormone secreted primarily from L …
(GPCR) which mediates the effects of GLP-1, an incretin hormone secreted primarily from L …
Positive allosteric modulation of a GPCR ternary complex
The activation of a G protein–coupled receptor (GPCR) leads to the formation of a ternary
complex between agonist, receptor, and G protein that is characterized by high-affinity …
complex between agonist, receptor, and G protein that is characterized by high-affinity …
Pharmacological selection of cannabinoid receptor effectors: Signalling, allosteric modulation and bias
The type-1 cannabinoid receptor (CB 1) is a promising drug target for a wide range of
diseases. However, many existing and novel candidate ligands for CB 1 have shown only …
diseases. However, many existing and novel candidate ligands for CB 1 have shown only …
Analyzing kinetic signaling data for G-protein-coupled receptors
In classical pharmacology, bioassay data are fit to general equations (eg the dose response
equation) to determine empirical drug parameters (eg EC50 and Emax), which are then …
equation) to determine empirical drug parameters (eg EC50 and Emax), which are then …
Molecular Spies in Action: Genetically Encoded Fluorescent Biosensors Light up Cellular Signals
Cellular function is controlled through intricate networks of signals, which lead to the myriad
pathways governing cell fate. Fluorescent biosensors have enabled the study of these …
pathways governing cell fate. Fluorescent biosensors have enabled the study of these …
Bias translation: The final frontier?
T Kenakin - British Journal of Pharmacology, 2024 - Wiley Online Library
Biased signalling is a natural result of GPCR allosteric function and should be expected from
any and all synthetic and natural agonists. Therefore, it may be encountered in all agonist …
any and all synthetic and natural agonists. Therefore, it may be encountered in all agonist …
Genetically encoded fluorescent biosensors for GPCR research
G protein-coupled receptors (GPCRs) regulate a wide range of physiological and
pathophysiological cellular processes, thus it is important to understand how GPCRs are …
pathophysiological cellular processes, thus it is important to understand how GPCRs are …
Quantifying the kinetics of signaling and arrestin recruitment by nervous system G-protein coupled receptors
Neurons integrate inputs over different time and space scales. Fast excitatory synapses at
boutons (ms and μm), and slow modulation over entire dendritic arbors (seconds and mm) …
boutons (ms and μm), and slow modulation over entire dendritic arbors (seconds and mm) …
[HTML][HTML] Partial agonism improves the anti-hyperglycaemic efficacy of an oxyntomodulin-derived GLP-1R/GCGR co-agonist
Objective Glucagon-like peptide-1 and glucagon receptor (GLP-1R/GCGR) co-agonism can
maximise weight loss and improve glycaemic control in type 2 diabetes and obesity. In this …
maximise weight loss and improve glycaemic control in type 2 diabetes and obesity. In this …