Potential cardiotoxicity of compounds predicted based on the interaction of astemizole with the HERG (human ether-a-go-go-related gene) potassium channel

Assays and kits are provided for the screening of test compounds for their capability to induce cardiotoxicity in a subject. The assays and kits are based on the finding that the interaction of astemizole with the HERG (Human Ether-a-go-go-Related Gene) potassium channel can be exploited to predict...

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Hauptverfasser:	JURZAK, MIREK ROMAN, HEYLEN, GODELIEVE IRMA CHRISTINE MARIA, VAN ZON, MARGOT, JANSSEN, CORNELUS GERARDUS MARIA, VAN ASSOUW, HENRICUS PETRUS MARTINUS MARIA
Format:	Patent
Sprache:	eng
Schlagworte:	BEER BIOCHEMISTRY CHEMISTRY COMPOSITIONS OR TEST PAPERS THEREFOR COMPOSITIONS THEREOF CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL ORENZYMOLOGICAL PROCESSES CULTURE MEDIA ENZYMOLOGY HETEROCYCLIC COMPOUNDS INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIRCHEMICAL OR PHYSICAL PROPERTIES MEASURING MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEICACIDS OR MICROORGANISMS METALLURGY MICROBIOLOGY MICROORGANISMS OR ENZYMES MUTATION OR GENETIC ENGINEERING ORGANIC CHEMISTRY PEPTIDES PHYSICS PROCESSES OF PREPARING SUCH COMPOSITIONS PROPAGATING, PRESERVING OR MAINTAINING MICROORGANISMS SPIRITS TESTING VINEGAR WINE
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Beschreibung
Zusammenfassung:	Assays and kits are provided for the screening of test compounds for their capability to induce cardiotoxicity in a subject. The assays and kits are based on the finding that the interaction of astemizole with the HERG (Human Ether-a-go-go-Related Gene) potassium channel can be exploited to predict cardiotoxicity of compounds during the development of new therapeutics and other agents. Figure 1 A shows the saturation binding of [3H]-astemizole to cell membrane preparations of HEK293 cells stably transfected with the HERG channel cDNA. TB represents Total Binding measured, NSB represents Non Specific Binding measured and SB represents Specific Binding measured.