scholarly journals Abstract P-4: Cryo-Electron Microscopy of G-Protein Coupled Receptor Complexes for Drug Discovery Approaches

2019 ◽  
Vol 9 (Suppl_1) ◽  
pp. S18-S18
Author(s):  
Anastasiia Gusach ◽  
Aleksandra Luginina ◽  
Valentin Borshchevskiy ◽  
Alexey Mishin
Keyword(s):  
Electron Microscopy ◽  
Drug Discovery ◽  
G Protein ◽  
G Protein Coupled Receptor ◽  
Receptor Complexes ◽  
Cryo Electron Microscopy ◽  
G Protein Coupled

scholarly journals The Significance of G Protein-Coupled Receptor Crystallography for Drug Discovery

2011 ◽  
Vol 63 (4) ◽  
pp. 901-937 ◽  
Author(s):  
John A. Salon ◽  
David T. Lodowski ◽  
Krzysztof Palczewski
Keyword(s):  
Drug Discovery ◽  
G Protein ◽  
G Protein Coupled Receptor ◽  
G Protein Coupled

G Protein-Coupled Receptor Transmembrane Binding Pockets and their Applications in GPCR Research and Drug Discovery: A Survey

2011 ◽  
Vol 11 (15) ◽  
pp. 1902-1924 ◽  
Author(s):  
Nicole A. Kratochwil ◽  
Silvia Gatti-McArthur ◽  
Marius C. Hoener ◽  
Lothar Lindemann ◽  
Andreas D. Christ ◽  
...  
Keyword(s):  
Drug Discovery ◽  
G Protein ◽  
G Protein Coupled Receptor ◽  
Binding Pockets ◽  
G Protein Coupled

scholarly journals Detecting G protein-coupled receptor complexes in postmortem human brain with proximity ligation assay and a Bayesian classifier

BioTechniques ◽  
2020 ◽  
Vol 68 (3) ◽  
pp. 122-129 ◽  
Author(s):  
Ying Zhu ◽  
József Mészáros ◽  
Roman Walle ◽  
Rongxi Fan ◽  
Ziyi Sun ◽  
...  
Keyword(s):  
Human Brain ◽  
G Protein ◽  
Dopamine D2 Receptor ◽  
Bayesian Classifier ◽  
Proximity Ligation Assay ◽  
Systematic Sampling ◽  
G Protein Coupled Receptor ◽  
Proximity Ligation ◽  
Receptor Complexes ◽  
G Protein Coupled

Despite the controversy regarding the existence and physiological relevance of class A G protein-coupled receptor dimerization, there is substantial evidence for functional interactions between the dopamine D2 receptor (D2R) and the adenosine A2A receptor (A2AR). A2AR-D2R complexes have been detected in rodent brains by proximity ligation assay; however, their existence in the human brain has not been demonstrated. In this study, we used Brightfield proximity ligation assay, combined with a systematic sampling and a parameter-free naive Bayesian classifier, and demonstrated proximity between the D2R and the A2AR in the adult human ventral striatum, consistent with their colocalization within complexes and the possible existence of D2R-A2AR heteromers. These methods are applicable to the relative quantification of proximity of two proteins, as well as the expression levels of individual proteins.

Cryo-EM: The Resolution Revolution and Drug Discovery

2020 ◽  
Vol 26 (1) ◽  
pp. 17-31
Author(s):  
Taiana Maia de Oliveira ◽  
Lotte van Beek ◽  
Fiona Shilliday ◽  
Judit É. Debreczeni ◽  
Chris Phillips
Keyword(s):  
Electron Microscopy ◽  
Drug Discovery ◽  
G Protein ◽  
Structural Biology ◽  
Single Particle ◽  
Trp Channels ◽  
G Protein Coupled Receptors ◽  
Imaging Analysis ◽  
Structure Based Drug Design ◽  
G Protein Coupled

Single-particle cryogenic electron microscopy (cryo-EM) has been elevated to the mainstream of structural biology propelled by technological advancements in numerous fronts, including imaging analysis and the development of direct electron detectors. The drug discovery field has watched with (initial) skepticism and wonder at the progression of the technique and how it revolutionized the molecular understanding of previously intractable targets. This article critically assesses how cryo-EM has impacted drug discovery in diverse therapeutic areas. Targets that have been brought into the realm of structure-based drug design by cryo-EM and are thus reviewed here include membrane proteins like the GABAA receptor, several TRP channels, and G protein-coupled receptors, and multiprotein complexes like the ribosomes, the proteasome, and eIF2B. We will describe these studies highlighting the achievements, challenges, and caveats.

Fluorescent probes for G-protein-coupled receptor drug discovery

2018 ◽  
Vol 13 (10) ◽  
pp. 933-947 ◽  
Author(s):  
Christos Iliopoulos-Tsoutsouvas ◽  
Rohit N. Kulkarni ◽  
Alexandros Makriyannis ◽  
Spyros P. Nikas
Keyword(s):  
Drug Discovery ◽  
G Protein ◽  
Fluorescent Probes ◽  
G Protein Coupled Receptor ◽  
G Protein Coupled

G protein-coupled receptor microarrays for drug discovery

2003 ◽  
Vol 8 (16) ◽  
pp. 755-761 ◽  
Author(s):  
Ye Fang ◽  
Joydeep Lahiri ◽  
Laurent Picard
Keyword(s):  
Drug Discovery ◽  
G Protein ◽  
G Protein Coupled Receptor ◽  
G Protein Coupled
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