Mechanisms of signalling and biased agonism in G protein-coupled receptors
D Wootten, A Christopoulos, M Marti-Solano… - … reviews Molecular cell …, 2018 - nature.com
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 …
Pharmacogenomics beyond single common genetic variants: the way forward
VM Lauschke, Y Zhou… - Annual Review of …, 2024 - annualreviews.org
Interindividual variability in genes encoding drug-metabolizing enzymes, transporters,
receptors, and human leukocyte antigens has a major impact on a patient's response to …
receptors, and human leukocyte antigens has a major impact on a patient's response to …
GPCRdb in 2023: state-specific structure models using AlphaFold2 and new ligand resources
G Pándy-Szekeres, J Caroli, A Mamyrbekov… - Nucleic acids …, 2023 - academic.oup.com
G protein-coupled receptors (GPCRs) are physiologically abundant signaling hubs routing
hundreds of extracellular signal substances and drugs into intracellular pathways. The …
hundreds of extracellular signal substances and drugs into intracellular pathways. The …
Structures of the σ2 receptor enable docking for bioactive ligand discovery
The σ2 receptor has attracted intense interest in cancer imaging, psychiatric disease,
neuropathic pain,–and other areas of biology,. Here we determined the crystal structure of …
neuropathic pain,–and other areas of biology,. Here we determined the crystal structure of …
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 …
Common activation mechanism of class A GPCRs
Class A G-protein-coupled receptors (GPCRs) influence virtually every aspect of human
physiology. Understanding receptor activation mechanism is critical for discovering novel …
physiology. Understanding receptor activation mechanism is critical for discovering novel …
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 …
Systematic Mendelian randomization using the human plasma proteome to discover potential therapeutic targets for stroke
Stroke is the second leading cause of death with substantial unmet therapeutic needs. To
identify potential stroke therapeutic targets, we estimate the causal effects of 308 plasma …
identify potential stroke therapeutic targets, we estimate the causal effects of 308 plasma …
[HTML][HTML] Illuminating G-protein-coupling selectivity of GPCRs
Heterotrimetic G proteins consist of four subfamilies (G s, G i/o, G q/11, and G 12/13) that
mediate signaling via G-protein-coupled receptors (GPCRs), principally by receptors binding …
mediate signaling via G-protein-coupled receptors (GPCRs), principally by receptors binding …
GPCRdb in 2018: adding GPCR structure models and ligands
G Pándy-Szekeres, C Munk, TM Tsonkov… - Nucleic acids …, 2018 - academic.oup.com
G protein-coupled receptors are the most abundant mediators of both human signalling
processes and therapeutic effects. Herein, we report GPCRome-wide homology models of …
processes and therapeutic effects. Herein, we report GPCRome-wide homology models of …