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Constitutive activity of the metabotropic glutamate receptor 2 explored with a whole-cell label-free biosensor

Overview of attention for article published in Biochemical Pharmacology, June 2018
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Title
Constitutive activity of the metabotropic glutamate receptor 2 explored with a whole-cell label-free biosensor
Published in
Biochemical Pharmacology, June 2018
DOI 10.1016/j.bcp.2018.03.026
Pubmed ID
Authors

Maarten L.J. Doornbos, Ilse Van der Linden, Liesbeth Vereyken, Gary Tresadern, Adriaan P. IJzerman, Hilde Lavreysen, Laura H. Heitman

Abstract

Label-free cellular assays using a biosensor provide new opportunities for studying G protein-coupled receptor (GPCR) signaling. As opposed to conventional in vitro assays, integrated receptor-mediated cellular responses are determined in real-time rather than a single downstream signaling pathway. In this study, we examined the potential of a label-free whole cell impedance-based biosensor system (i.e. xCELLigence) to study the pharmacology of one GPCR in particular, the mGlu2receptor. This receptor is a target for the treatment of several psychiatric diseases such as schizophrenia and depression. After optimization of assay conditions to prevent interference of endogenous glutamate in the culture medium, detailed pharmacological assessments were performed. Concentration-response curves showed a concentration-dependent increase in impedance for agonists and positive allosteric modulators, whereas receptor inhibition by an antagonist or negative allosteric modulator resulted in a concentration-dependent decrease in cellular impedance. Interestingly, constitutive receptor activity was observed that was decreased by LY341495, which therefore behaved as an inverse agonist here, a property that was heretofore unappreciated. This was confirmed by concentration-dependent modulation of LY341495 potency and efficacy by a allosteric modulators. In summary, the use of the xCELLigence system to study mGlu2receptor pharmacology was validated. This is the first class C GPCR to be characterized extensively by such method, opening new avenues to study receptor pharmacology including inverse agonism and demonstrating its value for future drug discovery efforts of mGlu receptors as well as other GPCRs.

Twitter Demographics

The data shown below were collected from the profile of 1 tweeter who shared this research output. Click here to find out more about how the information was compiled.

Mendeley readers

The data shown below were compiled from readership statistics for 17 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 17 100%

Demographic breakdown

Readers by professional status Count As %
Unspecified 4 24%
Student > Master 3 18%
Student > Ph. D. Student 3 18%
Researcher 3 18%
Student > Bachelor 2 12%
Other 2 12%
Readers by discipline Count As %
Pharmacology, Toxicology and Pharmaceutical Science 4 24%
Unspecified 4 24%
Biochemistry, Genetics and Molecular Biology 4 24%
Agricultural and Biological Sciences 2 12%
Psychology 1 6%
Other 2 12%

Attention Score in Context

This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 02 April 2018.
All research outputs
#10,180,707
of 12,745,229 outputs
Outputs from Biochemical Pharmacology
#5,108
of 5,612 outputs
Outputs of similar age
#204,976
of 273,184 outputs
Outputs of similar age from Biochemical Pharmacology
#12
of 21 outputs
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We're also able to compare this research output to 21 others from the same source and published within six weeks on either side of this one. This one is in the 14th percentile – i.e., 14% of its contemporaries scored the same or lower than it.