High Throughput Techniques for Discovering New Glycine Receptor Modulators and their Binding Sites.

Frontiers in Molecular Neuroscience
Daniel F GilbertTimothy I Webb

Abstract

The inhibitory glycine receptor (GlyR) is a member of the Cys-loop receptor family that mediates inhibitory neurotransmission in the central nervous system. These receptors are emerging as potential drug targets for inflammatory pain, immunomodulation, spasticity and epilepsy. Antagonists that specifically inhibit particular GlyR isoforms are also required as pharmacological probes for elucidating the roles of particular GlyR isoforms in health and disease. Although a substantial number of both positive and negative GlyR modulators have been identified, very few of these are specific for the GlyR over other receptor types. Thus, the potential of known compounds as either therapeutic leads or pharmacological probes is limited. It is therefore surprising that there have been few published studies describing attempts to discover novel GlyR isoform-specific modulators. The first aim of this review is to consider various methods for efficiently screening compounds against these receptors. We conclude that an anion sensitive yellow fluorescent protein is optimal for primary screening and that automated electrophysiology of cells stably expressing GlyRs is useful for confirming hits and quantitating the actions of identified compounds...Continue Reading

Citations

Dec 3, 2014·Fitoterapia·Jing-Yang Zhang, Yong-Xiang Wang
Oct 29, 2011·The Journal of Biological Chemistry·Timothy LynaghJoseph W Lynch
Nov 1, 2011·British Journal of Pharmacology·Robiul Islam, Joseph W Lynch
May 27, 2010·The Journal of Biological Chemistry·Megan E TippsS John Mihic
May 17, 2018·Brain and Neuroscience Advances·Luca A Annecchino, Simon R Schultz
Dec 6, 2018·Cytotechnology·Daniel F GilbertJoachim Wiest
Jul 27, 2012·Neuroscience Bulletin·Wei-Guang Li, Tian-Le Xu
Sep 7, 2017·Journal of Medicinal Chemistry·Christopher L Cioffi

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BETA
fluorescence resonance
FRET
transfection
chip
chips
PCR

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