ArticleFrontiers in molecular neuroscience2009
High Throughput Techniques for Discovering New Glycine Receptor Modulators and their Binding Sites.
Article in Frontiers in molecular neuroscience, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 36 citations in OpenAlex.
- Assaying Proliferation Characteristics of Cells Cultured Under Static Versus Periodic Conditions.Methods in molecular biology (Clifton, N.J.) · 2023Article
- Advancing Ion Channel Research with Automated Patch Clamp (APC) Electrophysiology Platforms.Advances in experimental medicine and biology · 2021Article
- 3D Printed Lab-on-a-Chip Platform for Chemical Stimulation and Parallel Analysis of Ion Channel Function.Micromachines · 2019Article
- Proliferation characteristics of cells cultured under periodic versus static conditions.Cytotechnology · 2019Article
- Using automated patch clamp electrophysiology platforms in pain-related ion channel research: insights from industry and academia.British journal of pharmacology · 2018Review
- Structure/Function Studies of the α4 Subunit Reveal Evolutionary Loss of a GlyR Subtype Involved in Startle and Escape Responses.Frontiers in molecular neuroscience · 2018Article
- A Recombinant Human Pluripotent Stem Cell Line Stably Expressing Halide-Sensitive YFP-I152L for GABAAR and GlyR-Targeted High-Throughput Drug Screening and Toxicity Testing.Frontiers in molecular neuroscience · 2016Article
- 4-bromopropofol decreases action potential generation in spinal neurons by inducing a glycine receptor-mediated tonic conductance.British journal of pharmacology · 2014Article
- Fluorescence-based high-throughput functional profiling of ligand-gated ion channels at the level of single cells.PloS one · 2013Article
- Emerging approaches to probing ion channel structure and function.Neuroscience bulletin · 2012Review
- Mechanism of action of the insecticides, lindane and fipronil, on glycine receptor chloride channels.British journal of pharmacology · 2012Article
- Molecular determinants of ivermectin sensitivity at the glycine receptor chloride channel.The Journal of biological chemistry · 2011Article
- Frontiers in molecular neuroscience - résumé and perspective.Frontiers in molecular neuroscience · 2011Article
- Recent progress in understanding the interaction between avermectins and ligand-gated ion channels: putting the pests to sleep.Invertebrate neuroscience : IN · 2010Review
- Identification of novel specific allosteric modulators of the glycine receptor using phage display.The Journal of biological chemistry · 2010Article
- An improved ivermectin-activated chloride channel receptor for inhibiting electrical activity in defined neuronal populations.The Journal of biological chemistry · 2010Article
- Glycinergic transmission: physiological, developmental and pathological implications.Frontiers in molecular neuroscience · 2010Article
- Progress in automating patch clamp cellular physiology.Brain and neuroscience advancesReview
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
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. The second aim of this review is to demonstrate how these techniques are used in our laboratory for the purpose of both discovering novel GlyR-active compounds and characterizing their binding sites. We also describe a reliable, cost effective method for transfecting HEK293 cells in single wells of a 384-well plate using nanogram quantities of plasmid DNA.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.