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 …
Biased allosteric modulators: new frontiers in GPCR drug discovery
G protein-coupled receptors (GPCRs) are the largest class of cell surface receptors in the
genome and the most successful family of targets of FDA-approved drugs. New frontiers in …
genome and the most successful family of targets of FDA-approved drugs. New frontiers in …
Signalling bias in new drug discovery: detection, quantification and therapeutic impact
T Kenakin, A Christopoulos - Nature reviews Drug discovery, 2013 - nature.com
Agonists of seven-transmembrane receptors, also known as G protein-coupled receptors
(GPCRs), do not uniformly activate all cellular signalling pathways linked to a given seven …
(GPCRs), do not uniformly activate all cellular signalling pathways linked to a given seven …
Emerging paradigms in GPCR allostery: implications for drug discovery
Allosteric ligands bind to G protein-coupled receptors (GPCRs; also known as seven-
transmembrane receptors) at sites that are distinct from the sites to which endogenous …
transmembrane receptors) at sites that are distinct from the sites to which endogenous …
Biased signaling of G protein coupled receptors (GPCRs): Molecular determinants of GPCR/transducer selectivity and therapeutic potential
M Seyedabadi, MH Ghahremani, PR Albert - Pharmacology & therapeutics, 2019 - Elsevier
G protein coupled receptors (GPCRs) convey signals across membranes via interaction with
G proteins. Originally, an individual GPCR was thought to signal through one G protein …
G proteins. Originally, an individual GPCR was thought to signal through one G protein …
Advances in G protein-coupled receptor allostery: from function to structure
A Christopoulos - Molecular pharmacology, 2014 - ASPET
It is now widely accepted that G protein-coupled receptors (GPCRs) are highly dynamic
proteins that adopt multiple active states linked to distinct functional outcomes. Furthermore …
proteins that adopt multiple active states linked to distinct functional outcomes. Furthermore …
A new inhibitor of the β-arrestin/AP2 endocytic complex reveals interplay between GPCR internalization and signalling
In addition to G protein-coupled receptor (GPCR) desensitization and endocytosis, β-arrestin
recruitment to ligand-stimulated GPCRs promotes non-canonical signalling cascades …
recruitment to ligand-stimulated GPCRs promotes non-canonical signalling cascades …
New advances in targeting the resolution of inflammation: implications for specialized pro-resolving mediator GPCR drug discovery
J Park, CJ Langmead, DM Riddy - ACS pharmacology & …, 2020 - ACS Publications
Chronic inflammation is a component of numerous diseases including autoimmune,
metabolic, neurodegenerative, and cancer. The discovery and characterization of …
metabolic, neurodegenerative, and cancer. The discovery and characterization of …
Pepducin targeting the CXC chemokine receptor type 4 acts as a biased agonist favoring activation of the inhibitory G protein
J Quoyer, JM Janz, J Luo, Y Ren… - Proceedings of the …, 2013 - National Acad Sciences
Short lipidated peptide sequences derived from various intracellular loop regions of G
protein-coupled receptors (GPCRs) are named pepducins and act as allosteric modulators …
protein-coupled receptors (GPCRs) are named pepducins and act as allosteric modulators …
Differential β-arrestin–dependent conformational signaling and cellular responses revealed by angiotensin analogs
B Zimmerman, A Beautrait, B Aguila, R Charles… - Science …, 2012 - science.org
The angiotensin type 1 receptor (AT1R) and its octapeptide ligand, angiotensin II (AngII),
engage multiple downstream signaling pathways, including those mediated by …
engage multiple downstream signaling pathways, including those mediated by …