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 …

Small, but powerful and attractive: 19F in biomolecular NMR

AM Gronenborn - Structure, 2022 - cell.com
Nuclear magnetic resonance (NMR) spectroscopy is a versatile tool for probing structure,
dynamics, folding, and interactions at atomic resolution. While naturally occurring …

[HTML][HTML] Structural insights into the dynamic process of β2-adrenergic receptor signaling

A Manglik, TH Kim, M Masureel, C Altenbach, Z Yang… - Cell, 2015 - cell.com
G-protein-coupled receptors (GPCRs) transduce signals from the extracellular environment
to intracellular proteins. To gain structural insight into the regulation of receptor cytoplasmic …

Biased Signaling Pathways in β2-Adrenergic Receptor Characterized by 19F-NMR

JJ Liu, R Horst, V Katritch, RC Stevens, K Wüthrich - Science, 2012 - science.org
Extracellular ligand binding to G protein–coupled receptors (GPCRs) modulates G protein
and β-arrestin signaling by changing the conformational states of the cytoplasmic region of …

Allosteric coupling of drug binding and intracellular signaling in the A2A adenosine receptor

MT Eddy, MY Lee, ZG Gao, KL White, T Didenko… - Cell, 2018 - cell.com
Signaling across cellular membranes, the 826 human G protein-coupled receptors (GPCRs)
govern a wide range of vital physiological processes, making GPCRs prominent drug …

A genetically encoded F-19 NMR probe reveals the allosteric modulation mechanism of cannabinoid receptor 1

X Wang, D Liu, L Shen, F Li, Y Li, L Yang… - Journal of the …, 2021 - ACS Publications
Due to the lack of genetically encoded probes for fluorine-19 nuclear magnetic resonance
spectroscopy (19F NMR), its utility for probing eukaryotic membrane protein dynamics is …

[BUKU][B] Nuclear magnetic resonance studies of interfacial phenomena

VM Gun'ko, VV Turov - 2013 - books.google.com
This book explores important new NMR spectroscopic methods and describes and
compares the application of NMR to a large variety of useful materials with results from other …

Current applications of 19F NMR to studies of protein structure and dynamics

JL Kitevski-LeBlanc, RS Prosser - Progress in nuclear magnetic resonance …, 2012 - Elsevier
While traditional 1H, 13C, and 15N (HCN) solution state NMR protocols provide a wealth of
data on protein structure and dynamics, 19F NMR provides a unique perspective of …

The role of protein dynamics in GPCR function: insights from the β2AR and rhodopsin

A Manglik, B Kobilka - Current opinion in cell biology, 2014 - Elsevier
G protein-coupled receptors (GPCRs) are versatile signaling proteins that mediate complex
cellular responses to hormones and neurotransmitters. Recent advances in GPCR …

Role of the conserved NPxxY(x)5,6F motif in the rhodopsin ground state and during activation

O Fritze, S Filipek, V Kuksa, K Palczewski… - Proceedings of the …, 2003 - pnas.org
In the G protein-coupled receptor rhodopsin, the conserved NPxxY (x) 5, 6F motif connects
the transmembrane helix VII and the cytoplasmic helix 8. The less geometrically constrained …