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 …

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 …

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 …

Structures of the σ2 receptor enable docking for bioactive ligand discovery

A Alon, J Lyu, JM Braz, TA Tummino, V Craik… - Nature, 2021 - nature.com
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 …

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 …

Common activation mechanism of class A GPCRs

Q Zhou, D Yang, M Wu, Y Guo, W Guo, L Zhong, X Cai… - Elife, 2019 - elifesciences.org
Class A G-protein-coupled receptors (GPCRs) influence virtually every aspect of human
physiology. Understanding receptor activation mechanism is critical for discovering novel …

GPCR activation mechanisms across classes and macro/microscales

AS Hauser, AJ Kooistra, C Munk… - Nature structural & …, 2021 - nature.com
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 …

Systematic Mendelian randomization using the human plasma proteome to discover potential therapeutic targets for stroke

L Chen, JE Peters, B Prins, E Persyn, M Traylor… - Nature …, 2022 - nature.com
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 …

[HTML][HTML] Illuminating G-protein-coupling selectivity of GPCRs

A Inoue, F Raimondi, FMN Kadji, G Singh, T Kishi… - Cell, 2019 - cell.com
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 …

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 …