Recent advances in the determination of G protein-coupled receptor structures

2018 ◽  
Vol 51 ◽  
pp. 28-34 ◽  
Author(s):  
David M Thal ◽  
Ziva Vuckovic ◽  
Christopher J Draper-Joyce ◽  
Yi-Lynn Liang ◽  
Alisa Glukhova ◽  
...  
Keyword(s):  
G Protein ◽  
G Protein Coupled Receptor ◽  
Recent Advances ◽  
G Protein Coupled

Recent Advances in Predicting G-Protein Coupled Receptor Classification

2012 ◽  
Vol 7 (2) ◽  
pp. 132-142 ◽  
Author(s):  
Xuan Xiao ◽  
Wei-Zhong Lin ◽  
Kuo-Chen Chou
Keyword(s):  
G Protein ◽  
G Protein Coupled Receptor ◽  
Recent Advances ◽  
G Protein Coupled

scholarly journals Probe dependency in the determination of ligand binding kinetics at a prototypical G protein-coupled receptor

2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Reggie Bosma ◽  
Leigh A. Stoddart ◽  
Victoria Georgi ◽  
Monica Bouzo-Lorenzo ◽  
Nick Bushby ◽  
...  
Keyword(s):  
Ligand Binding ◽  
G Protein ◽  
Binding Kinetics ◽  
G Protein Coupled Receptor ◽  
G Protein Coupled

scholarly journals Structural determination of the mechanism of domain separation of G‐protein‐coupled receptor kinase 4g

2019 ◽  
Vol 33 (S1) ◽  
Author(s):  
Jae Kyung Yeon ◽  
Garima Sharma ◽  
Wesley M. Botello‐Smith ◽  
Yun Lyna Luo ◽  
Bradley T. Andresen
Keyword(s):  
G Protein ◽  
Structural Determination ◽  
Receptor Kinase ◽  
G Protein Coupled Receptor ◽  
G Protein Coupled ◽  
Domain Separation

scholarly journals ThermoFRET: A novel nanoscale G protein coupled receptor thermostability assay functional in crude solubilised membrane preparations

2020 ◽  
Author(s):  
David N Tippett ◽  
Brad Hoare ◽  
Tamara Miljus ◽  
David A Sykes ◽  
Dmitry B. Veprintsev
Keyword(s):  
Drug Discovery ◽  
Protein Purification ◽  
G Protein ◽  
High Throughput ◽  
Thermal Denaturation ◽  
Protein Unfolding ◽  
Orphan Receptor ◽  
G Protein Coupled Receptor ◽  
G Protein Coupled

AbstractSensitive protein stability assays for membrane proteins are crucial for developing purification protocols, for structural and biophysical characterisation and drug discovery. Here, we describe a novel high-throughput 384-well FRET-based thermostability methodology, ThermoFRET, allowing for the ultrasensitive determination of G protein coupled receptor (GPCR) stability. This method measures FRET between a terbium-cryptate labelled GPCR and BODIPY-FL-Cystine, a thiolreactive dye that reacts with cysteine residues exposed upon protein unfolding in response to thermal denaturation. ThermoFRET is functional in crude solubilised membrane preparations, without protein purification and can detect receptor stabilising ligands, making it ideally suited for orphan receptor screening.

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