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 …
The role of NMR in leveraging dynamics and entropy in drug design
Nuclear magnetic resonance (NMR) spectroscopy has contributed to structure-based drug
development (SBDD) in a unique way compared to the other biophysical methods. The …
development (SBDD) in a unique way compared to the other biophysical methods. The …
Solution NMR spectroscopy of GPCRs: Residue-specific labeling strategies with a focus on 13C-methyl methionine labeling of the atypical chemokine receptor …
The past decade has witnessed remarkable progress in the determination of G protein-
coupled receptor (GPCR) structures, profoundly expanding our understanding of how …
coupled receptor (GPCR) structures, profoundly expanding our understanding of how …
Expression and Purification of a Functional E. coli 13CH3-Methionine-Labeled Thermostable Neurotensin Receptor 1 Variant for Solution NMR Studies
Escherichia coli (E. coli) is the most widely used expression host for recombinant proteins
due to high expression yields and straightforward molecular cloning. Directed evolution of G …
due to high expression yields and straightforward molecular cloning. Directed evolution of G …
Cysteine-ethylation of tissue-extracted membrane proteins as a tool to detect conformational states by solid-state NMR spectroscopy
Solid-state NMR (ssNMR) is an ideal tool to study structure and dynamics of membrane
proteins in their native lipid environment. In principle, ssNMR has no size limitations …
proteins in their native lipid environment. In principle, ssNMR has no size limitations …
Forbidden Coherence Transfer of 19F Nuclei to Quantitatively Measure the Dynamics of a CF3-Containing Ligand in Receptor-Bound States
Y Tokunaga, K Takeuchi, I Shimada - Molecules, 2017 - mdpi.com
The dynamic property of a ligand in the receptor-bound state is an important metric to
characterize the interactions in the ligand–receptor interface, and the development of an …
characterize the interactions in the ligand–receptor interface, and the development of an …
Mechanism of Phospholamban Activation by HAX-1 and their Roles in the Regulation of the SR Calcium-ATPase
EK Larsen - 2021 - search.proquest.com
The Ca 2+ transient of the cardiomyocyte is key to the contractility of the heart. Its
dysregulation has been associated with heart disease, leading to investigation of the …
dysregulation has been associated with heart disease, leading to investigation of the …
[PDF][PDF] Characterising the conformational diversity of the neurotensin receptor
F Bumbak - 2016 - core.ac.uk
Abstract G Protein-Coupled Receptors (GPCRs) deliver approximately 80% of all signals
across the cell membrane and are targets for around 26% of all prescription drugs …
across the cell membrane and are targets for around 26% of all prescription drugs …