Functional dynamics of G protein-coupled receptors reveal new routes for drug discovery

P Conflitti, E Lyman, MSP Sansom… - Nature Reviews Drug …, 2025 - nature.com
G protein-coupled receptors (GPCRs) are the largest human membrane protein family that
transduce extracellular signals into cellular responses. They are major pharmacological …

Nanodiscs for the study of membrane proteins

IG Denisov, SG Sligar - Current Opinion in Structural Biology, 2024 - Elsevier
Nanodiscs represent a versatile tool for studies of membrane proteins and protein-
membrane interactions under native-like conditions. Multiple variations of the Nanodisc …

[HTML][HTML] Biased activation of the vasopressin V2 receptor probed by molecular dynamics simulations, NMR and pharmacological studies

A Fouillen, P Couvineau, G Gaibelet, S Riché… - Computational and …, 2024 - Elsevier
G protein-coupled receptors (GPCRs) control critical cell signaling. Their response to
extracellular stimuli involves conformational changes to convey signals to intracellular …

The critical importance of conditions: Reconciling GPCR functionality and biophysical findings

MA Reith, JK Rainey - Structure, 2024 - Elsevier
G-protein-coupled receptor (GPCR) activation relies on conformational sampling, a nuanced
but functionally key behavior well suited to elucidation by nuclear magnetic resonance …

[HTML][HTML] The conformational equilibria of a human GPCR compared between lipid vesicles and aqueous solutions by integrative 19F-NMR

AP Ray, B **, MT Eddy - bioRxiv, 2024 - pmc.ncbi.nlm.nih.gov
Endogenous phospholipids influence the conformational equilibria of G protein-coupled
receptors, regulating their ability to bind drugs and form signaling complexes. However …