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 …
Structural insights into G-protein-coupled receptor allostery
G-protein-coupled receptors (GPCRs) are key cell-surface proteins that transduce external
environmental cues into biochemical signals across the membrane. GPCRs are intrinsically …
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 …
drug targets, mediating the action of one-third of medicines. The GPCR database, GPCRdb …
[HTML][HTML] 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 …
[HTML][HTML] 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 …
[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 …
nature of interactions in molecular complexes, typically formed between a protein and a …
[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 …
[HTML][HTML] Pharmacogenomics of GPCR drug targets
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 …
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 …
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
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 …
activates 12 different G protein-coupled receptors (GPCRs) through selective coupling of G …