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 …
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 …
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
G-protein-coupled receptors (GPCRs) represent a ubiquitous membrane protein family and
are important drug targets. Their diverse signaling pathways are driven by complex …
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 …
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 …
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 …
are either essential for signal transduction and solute transport or function as scaffold …
A2A adenosine receptor functional states characterized by 19F-NMR
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 …
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 …
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 …
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
Over the past decade, the vast amount of information generated through structural and
biophysical studies of GPCRs has provided unprecedented mechanistic insight into the …
biophysical studies of GPCRs has provided unprecedented mechanistic insight into the …