GPCR drug discovery: integrating solution NMR data with crystal and cryo-EM structures

I Shimada, T Ueda, Y Kofuku, MT Eddy… - Nature Reviews Drug …, 2019 - nature.com
The 826 G protein-coupled receptors (GPCRs) in the human proteome regulate key
physiological processes and thus have long been attractive drug targets. With the crystal …

[HTML][HTML] Methyl TROSY spectroscopy: a versatile NMR approach to study challenging biological systems

S Schütz, R Sprangers - Progress in nuclear magnetic resonance …, 2020 - Elsevier
A major goal in structural biology is to unravel how molecular machines function in detail. To
that end, solution-state NMR spectroscopy is ideally suited as it is able to study biological …

Delineating the conformational landscape of the adenosine A2A receptor during G protein coupling

SK Huang, A Pandey, DP Tran, NL Villanueva, A Kitao… - Cell, 2021 - cell.com
G-protein-coupled receptors (GPCRs) represent a ubiquitous membrane protein family and
are important drug targets. Their diverse signaling pathways are driven by complex …

The role of structural dynamics in GPCR‐mediated signaling

D Hilger - The FEBS journal, 2021 - Wiley Online Library
G protein‐coupled receptors (GPCRs) play critical roles in the regulation of human
physiology in response to a wide array of different extracellular stimuli and thus represent …

Molecular insights into the biased signaling mechanism of the μ-opioid receptor

X Cong, D Maurel, H Déméné, I Vasiliauskaité-Brooks… - Molecular Cell, 2021 - cell.com
GPCR functional selectivity opens new opportunities for the design of safer drugs. Ligands
orchestrate GPCR signaling cascades by modulating the receptor conformational …

Solution NMR: A powerful tool for structural and functional studies of membrane proteins in reconstituted environments

R Puthenveetil, O Vinogradova - Journal of Biological Chemistry, 2019 - ASBMB
A third of the genes in prokaryotic and eukaryotic genomes encode membrane proteins that
are either essential for signal transduction and solute transport or function as scaffold …

A2A adenosine receptor functional states characterized by 19F-NMR

L Sušac, MT Eddy, T Didenko… - Proceedings of the …, 2018 - National Acad Sciences
The human proteome contains 826 G protein-coupled receptors (GPCR), which control a
wide array of key physiological functions, making them important drug targets. GPCR …

Advances in the study of GPCRs by 19F NMR

LP Picard, RS Prosser - Current Opinion in Structural Biology, 2021 - Elsevier
Crystallography and cryo-electron microscopy have advanced atomic resolution
perspectives of inactive and active states of G protein-coupled receptors (GPCRs), alone …

Adenosine A2A receptor antagonists: from caffeine to selective non‐xanthines

KA Jacobson, ZG Gao, P Matricon… - British journal of …, 2022 - Wiley Online Library
A long evolution of knowledge of the psychostimulant caffeine led in the 1960s to another
purine natural product, adenosine and its A2A receptor. Adenosine is a short‐lived …

Structure and dynamics of GPCRs in lipid membranes: physical principles and experimental approaches

AJY Jones, F Gabriel, A Tandale, D Nietlispach - Molecules, 2020 - mdpi.com
Over the past decade, the vast amount of information generated through structural and
biophysical studies of GPCRs has provided unprecedented mechanistic insight into the …