G-Protein-Coupled Receptors and Ischemic Stroke: a Focus on Molecular Function and Therapeutic Potential

2021 ◽  
Author(s):  
Zeinab Vahidinia ◽  
Mohammad Taghi Joghataei ◽  
Cordian Beyer ◽  
Mohammad Karimian ◽  
Abolfazl Azami Tameh
Keyword(s):  
Ischemic Stroke ◽  
G Protein ◽  
Therapeutic Potential ◽  
G Protein Coupled Receptors ◽  
Molecular Function ◽  
G Protein Coupled

scholarly journals Seeing cells smell: Dynamic optical measurements of Ca2+ and cAMP signaling from Olfactory Receptors transiently expressed in HEK293TN cells

2019 ◽  
Author(s):  
A Pietraszewska-Bogiel ◽  
L van Weeren ◽  
J Goedhart
Keyword(s):  
G Protein ◽  
Therapeutic Potential ◽  
Olfactory Receptors ◽  
Functional Expression ◽  
G Protein Coupled Receptors ◽  
Optical Measurements ◽  
Camp Signaling ◽  
Kinetic Measurements ◽  
Fluorescent Biosensors ◽  
G Protein Coupled

ABSTRACTOlfactory receptors (ORs) constitute the largest family of G-protein coupled receptors. They are responsible for the perception of odor (olfaction) and also play important roles in other biological processes, including regulation of cell proliferation. Their increasing diagnostic and therapeutic potential, especially for cancer research, requests the ongoing development of methodologies that would allow their robust functional expression in non-olfactory cells, and dynamic analysis of their signaling pathways. To enable realtime detection of OR activity, we use single cell imaging with genetically encoded fluorescent biosensors, Yellow Cameleon or EPAC, which are routinely used for kinetic measurements of Ca2+ or cAMP signaling downstream of various G-protein coupled receptors. We demonstrate that the co-expression of Lucy-Rho tagged variants of ORs together with an accessory protein, RTP1s, in HEK293TN cells is sufficient to detect the activity of a panel of ORs. Using this methodology, we were able to detect both Ca2+ and cAMP signaling downstream of twelve ORs within 2 minutes from the application of odorant.

scholarly journals patGPCR: A Multitemplate Approach for Improving 3D Structure Prediction of Transmembrane Helices of G-Protein-Coupled Receptors

2013 ◽  
Vol 2013 ◽  
pp. 1-12 ◽  
Author(s):  
Hongjie Wu ◽  
Qiang Lü ◽  
Lijun Quan ◽  
Peide Qian ◽  
Xiaoyan Xia
Keyword(s):  
G Protein ◽  
Structure Prediction ◽  
Transmembrane Helix ◽  
3D Structure ◽  
G Protein Coupled Receptors ◽  
Ligand Docking ◽  
Molecular Function ◽  
Transmembrane Helices ◽  
G Protein Coupled ◽  
Multiple Template

The structures of the seven transmembrane helices of G-protein-coupled receptors are critically involved in many aspects of these receptors, such as receptor stability, ligand docking, and molecular function. Most of the previous multitemplate approaches have built a “super” template with very little merging of aligned fragments from different templates. Here, we present a parallelized multitemplate approach, patGPCR, to predict the 3D structures of transmembrane helices of G-protein-coupled receptors. patGPCR, which employs a bundle-packing related energy function that extends on the RosettaMem energy, parallelizes eight pipelines for transmembrane helix refinement and exchanges the optimized helix structures from multiple templates. We have investigated the performance of patGPCR on a test set containing eight determined G-protein-coupled receptors. The results indicate that patGPCR improves the TM RMSD of the predicted models by 33.64% on average against a single-template method. Compared with other homology approaches, the best models for five of the eight targets built by patGPCR had a lower TM RMSD than that obtained from SWISS-MODEL; patGPCR also showed lower average TM RMSD than single-template and multiple-template MODELLER.

Therapeutic Potential of G Protein‐Coupled Receptors against Nonalcoholic Steatohepatitis

Hepatology ◽  
2021 ◽  
Author(s):  
Dating Sun ◽  
Xia Yang ◽  
Bin Wu ◽  
Xiao‐Jing Zhang ◽  
Hongliang Li ◽  
...  
Keyword(s):  
G Protein ◽  
Nonalcoholic Steatohepatitis ◽  
Therapeutic Potential ◽  
G Protein Coupled Receptors ◽  
G Protein Coupled

scholarly journals Update on GPCR-based targets for the development of novel antidepressants

2021 ◽  
Author(s):  
Ioannis Mantas ◽  
Marcus Saarinen ◽  
Zhi-Qing David Xu ◽  
Per Svenningsson
Keyword(s):  
Major Depressive Disorder ◽  
Depressive Disorder ◽  
G Protein ◽  
Therapeutic Potential ◽  
G Protein Coupled Receptors ◽  
Major Depressive ◽  
Ligand Selectivity ◽  
Direct Targeting ◽  
Atypical Antidepressants ◽  
G Protein Coupled

AbstractTraditional antidepressants largely interfere with monoaminergic transport or degradation systems, taking several weeks to have their therapeutic actions. Moreover, a large proportion of depressed patients are resistant to these therapies. Several atypical antidepressants have been developed which interact with G protein coupled receptors (GPCRs) instead, as direct targeting of receptors may achieve more efficacious and faster antidepressant actions. The focus of this review is to provide an update on how distinct GPCRs mediate antidepressant actions and discuss recent insights into how GPCRs regulate the pathophysiology of Major Depressive Disorder (MDD). We also discuss the therapeutic potential of novel GPCR targets, which are appealing due to their ligand selectivity, expression pattern, or pharmacological profiles. Finally, we highlight recent advances in understanding GPCR pharmacology and structure, and how they may provide new avenues for drug development.

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