Faculty Opinions recommendation of Structure-Based Optimization Strategies for G Protein-Coupled Receptor (GPCR) Allosteric Modulators: A Case Study from Analyses of New Metabotropic Glutamate Receptor 5 (mGlu5) X-ray Structures.

2018 ◽  
Author(s):  
Dario Doller
Keyword(s):  
G Protein ◽  
Glutamate Receptor ◽  
Metabotropic Glutamate Receptor ◽  
Allosteric Modulators ◽  
G Protein Coupled Receptor ◽  
Metabotropic Glutamate Receptor 5 ◽  
X Ray ◽  
Metabotropic Glutamate ◽  
G Protein Coupled

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 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)

Regulation of mGlu4 Metabotropic Glutamate Receptor Signaling by Type-2 G-Protein Coupled Receptor Kinase (GRK2)

2004 ◽  
Vol 65 (5) ◽  
pp. 1103-1110 ◽  
Author(s):  
L. Iacovelli ◽  
L. Capobianco ◽  
M. Iula ◽  
V. Di Giorgi Gerevini ◽  
A. Picascia ◽  
...  
Keyword(s):  
G Protein ◽  
Glutamate Receptor ◽  
Metabotropic Glutamate Receptor ◽  
Receptor Signaling ◽  
Receptor Kinase ◽  
G Protein Coupled Receptor ◽  
Metabotropic Glutamate ◽  
G Protein Coupled
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