Profiling of orthosteric and allosteric group-III metabotropic glutamate receptor ligands on various G protein-coupled receptors with Tag-lite® assays

2018 ◽  
Vol 140 ◽  
pp. 233-245 ◽  
Author(s):  
Abderazak Belhocine ◽  
Pietro Veglianese ◽  
Candide Hounsou ◽  
Elodie Dupuis ◽  
Francine Acher ◽  
...  
Keyword(s):  
G Protein ◽  
Glutamate Receptor ◽  
Metabotropic Glutamate Receptor ◽  
G Protein Coupled Receptors ◽  
Receptor Ligands ◽  
Group Iii ◽  
Metabotropic Glutamate ◽  
G Protein Coupled

scholarly journals Evaluation of FLIPR Calcium 3 Assay Kit—A New No-Wash Fluorescence Calcium Indicator Reagent

2003 ◽  
Vol 8 (5) ◽  
pp. 571-577 ◽  
Author(s):  
Yingxin Zhang ◽  
Dianne Kowal ◽  
Angela Kramer ◽  
John Dunlop
Keyword(s):  
Calcium Signaling ◽  
G Protein ◽  
Glutamate Receptor ◽  
Metabotropic Glutamate Receptor ◽  
G Protein Coupled Receptors ◽  
Metabotropic Glutamate Receptor 5 ◽  
Metabotropic Glutamate ◽  
Calcium Indicator ◽  
Indicator Dye ◽  
G Protein Coupled

We have evaluated the FLIPR Calcium 3 Assay Kit (Calcium 3), a new no-wash fluorescence calcium indicator dye reagent, for the measurement of agonist-stimulated calcium signaling in cells expressing the serotonin 2C (5-HT2C), metabotropic glutamate receptor 5 (mGluR5) and the vasopressin 2 (V2) G-protein-coupled receptors. Calcium 3 yielded equivalent (5-HT2C) or superior (mGluR5 and V2) sensitivity to FLUO-4 as indexed by the change in fluorescence counts following agonist application. Assay variability, indexed by CV, using Calcium 3 or FLUO-4 was equivalent with 5-HT2C receptor responses although CVs were reduced using Calcium 3 in the examples of the mGluR5 and V2 receptors. Receptor pharmacologies based on agonist EC50 values were identical when either Calcium 3 or FLUO-4 were utilized. Our results validate Calcium 3 as a compel-ling alternative to FLUO-4 in the choice of fluorescent dye reagent for studying G-protein-coupled receptors, providing the advantage of a homogenous, no-wash assay format. ( Journal of Biomolecular Screening 2003:571-577)

scholarly journals G Protein-coupled Receptor Kinase-mediated Desensitization of Metabotropic Glutamate Receptor 1A Protects against Cell Death

2000 ◽  
Vol 275 (49) ◽  
pp. 38213-38220 ◽  
Author(s):  
Lianne B. Dale ◽  
Moshmi Bhattacharya ◽  
Pieter H. Anborgh ◽  
Barbara Murdoch ◽  
Mickie Bhatia ◽  
...  
Keyword(s):  
Cell Death ◽  
G Protein ◽  
Glutamate Receptor ◽  
Metabotropic Glutamate Receptor ◽  
Receptor Kinase ◽  
G Protein Coupled Receptor ◽  
Metabotropic Glutamate ◽  
G Protein Coupled

scholarly journals The G protein-Coupled Metabotropic Glutamate Receptor 1 controls neuronal macroautophagy

2020 ◽  
Author(s):  
Maribel Donoso ◽  
Luisa Speranza ◽  
Magdalena Kalinowska ◽  
Catherine Castillo ◽  
Claudia De Sanctis ◽  
...  
Keyword(s):  
G Protein ◽  
Glutamate Receptor ◽  
Metabotropic Glutamate Receptor ◽  
Autophagy Flux ◽  
Metabotropic Glutamate ◽  
Evolutionarily Conserved ◽  
Metabotropic Glutamate Receptor 1 ◽  
Mglu1 Receptor ◽  
G Protein Coupled ◽  
The Brain

AbstractAutophagy is an evolutionarily conserved, highly regulated catabolic process critical to neuronal homeostasis, function and survival throughout organismal lifespan. However, the external factors and signals that control autophagy in neurons are still poorly understood. Here we report that the G protein-coupled metabotropic glutamate receptor 1 (mGlu1) contributes to control basal autophagy in the brain. Autophagy is upregulated in the brain of adult mGlu1 knockout mice and genetic deletion or pharmacological inhibition of native mGlu1 receptors enhances autophagy flux in neurons. The evolutionarily conserved adaptor protein FEZ1, identified by a genome-wide screen as mGlu1 receptor interacting partner, was found to participate in the regulation of neuronal autophagy and to be required for repression of autophagy flux by the mGlu1 receptor. Furthermore, FEZ1 appears to enable association of mGlu1 with Ulk1, a core component of the autophagy pathway. Thus, we propose that the mGlu1 receptor contributes to restrain constitutive autophagy in neurons.

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