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 …

Structural insights into G-protein-coupled receptor allostery

DM Thal, A Glukhova, PM Sexton, A Christopoulos - Nature, 2018 - nature.com
G-protein-coupled receptors (GPCRs) are key cell-surface proteins that transduce external
environmental cues into biochemical signals across the membrane. GPCRs are intrinsically …

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 …

[HTML][HTML] 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 …

[HTML][HTML] 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 …

[HTML][HTML] ProLIF: a library to encode molecular interactions as fingerprints

C Bouysset, S Fiorucci - Journal of cheminformatics, 2021 - Springer
Interaction fingerprints are vector representations that summarize the three-dimensional
nature of interactions in molecular complexes, typically formed between a protein and a …

[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 …

[HTML][HTML] Pharmacogenomics of GPCR drug targets

AS Hauser, S Chavali, I Masuho, LJ Jahn… - Cell, 2018 - cell.com
Natural genetic variation in the human genome is a cause of individual differences in
responses to medications and is an underappreciated burden on public health. Although …

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 …

[HTML][HTML] GPCRs steer Gi and Gs selectivity via TM5-TM6 switches as revealed by structures of serotonin receptors

S Huang, P Xu, DD Shen, IA Simon, C Mao, Y Tan… - Molecular cell, 2022 - cell.com
Summary Serotonin (or 5-hydroxytryptamine, 5-HT) is an important neurotransmitter that
activates 12 different G protein-coupled receptors (GPCRs) through selective coupling of G …