About: Image-Based Marker-Free Screening of GABA(A) Agonists, Antagonists, and Modulators

Facets (new session)
Description
Metadata
Settings
- owl:sameAs
- Inference Rule:

About: Image-Based Marker-Free Screening of GABA(A) Agonists, Antagonists, and Modulators Goto Sponge NotDistinct Permalink

An Entity of Type : schema:ScholarlyArticle, within Data Space : covidontheweb.inria.fr associated with source document(s)

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
title	Image-Based Marker-Free Screening of GABA(A) Agonists, Antagonists, and Modulators
Creator	Kuttler, Fabien Turcatti, Gerardo Banfi, Damiano Jourdain, Pascal Marquet, Pierre Rappaz, Benjamin Biomolecular, Screening Facility,
source	PMC
abstract	The ionotropic GABA(A) receptors represent the main target for different groups of widely used drugs having hypnotic and anxiolytic effects. So far, most approaches used to assess GABA activity involve invasive low -throughput electrophysiological techniques or rely on fluorescent dyes, preventing the ability to conduct noninvasive and thus nonperturbing screens. To address this limitation, we have developed an automated marker-free cell imaging method, based on digital holographic microscopy (DHM). This technology allows the automatically screening of compounds in multiple plates without having to label the cells or use special plates. This methodological approach was first validated by screening the GABA(A) receptor expressed in HEK cells using a selection of active compounds in agonist, antagonist, and modulator modes. Then, in a second blind screen of a library of 3041 compounds (mostly composed of natural products), 5 compounds having a specific agonist action on the GABA(A) receptor were identified. The hits validated from this unbiased screen were the natural products muscimol, neurosteroid alphaxalone, and three compounds belonging to the avermectin family, all known for having an agonistic effect on the GABA(A) receptor. The results obtained were exempt from false negatives (structurally similar unassigned hits), and false-positive hits were detected and discarded without the need for performing electrophysiological measurements. The outcome of the screen demonstrates the applicability of our screening by imaging method for the discovery of new chemical structures, particularly regarding chemicals interacting with the ionotropic GABA(A) receptor and more generally with any ligand-gated ion channels and transporters.
has issue date	2019-11-28(xsd:dateTime)
bibo:doi	10.1177/2472555219887142
bibo:pmid	31779505
has license	cc-by-nc
sha1sum (hex)	9b5f79cbbd8256f0e383c91f036bc480940bf803
schema:url	https://doi.org/10.1177/2472555219887142
resource representing a document's title	Image-Based Marker-Free Screening of GABA(A) Agonists, Antagonists, and Modulators
has PubMed Central identifier	PMC7243081
has PubMed identifier	31779505
schema:publication	SLAS Discov
resource representing a document's body	covid:9b5f79cbbd8256f0e383c91f036bc480940bf803#body_text
is schema:about of	named entity 'This' named entity 'DHM' named entity 'involve' named entity 'USED' named entity 'APPROACHES' named entity 'NONINVASIVE' named entity 'BASED' named entity 'throughput' named entity 'rely' named entity 'plates' named entity 'screening' named entity 'cell imaging' named entity 'fluorescent dyes' named entity 'GABA A receptors' named entity 'anxiolytic' named entity 'screens' named entity 'drug discovery' named entity 'SAR' named entity 'membrane potential' named entity 'vindesine' named entity 'GABA' named entity 'gigaohm seal' named entity 'Illkirch' named entity 'Leica' named entity 'microtubule' named entity 'chloride' named entity 'transmembrane' named entity 'DMSO' named entity 'cytoskeleton' named entity 'GABA' named entity 'agonist' named entity 'oxaline' named entity 'colchicine' named entity 'culture medium' named entity 'GABA' named entity 'fluorophores' named entity 'GABA A receptors' named entity 'Clontech' named entity 'OPD' named entity 'light source' named entity 'meleagrin' named entity 'chloride' named entity 'room temperature' named entity 'ion' named entity 'agonist' named entity 'physical properties' named entity 'high-content screening' named entity 'HEK' named entity 'laser' named entity 'potency' named entity 'HEPES' named entity 'room temperature' named entity 'anxiolytics' named entity 'binding sites' named entity 'DHM' named entity 'Switzerland' named entity 'refractive index' named entity 'agonists' named entity 'SAR' named entity 'psychiatric diseases' named entity 'QPI' named entity 'hypnotics' named entity 'microscopy' named entity 'DHM' named entity 'time frame' named entity 'substituent' named entity 'fluorescent dyes' named entity 'GABA' named entity 'fetal calf serum' named entity 'DHM' named entity 'mOsm' named entity 'serial dilution' named entity 'agonist' named entity 'standard error'

Faceted Search & Find service v1.13.91 as of Mar 24 2020

Alternative Linked Data Documents: Sponger | ODE Content Formats:

RDF

ODATA

Microdata

About

OpenLink Virtuoso version 07.20.3229 as of Jul 10 2020, on Linux (x86_64-pc-linux-gnu), Single-Server Edition (94 GB total memory)
Data on this page belongs to its respective rights holders.
Virtuoso Faceted Browser Copyright © 2009-2025 OpenLink Software