HERG inhibitors with similar potency but different binding kinetics do not pose the same proarrhythmic risk: Implications for drug safety assessment

Journal of Cardiovascular Electrophysiology

Volumn 25, Issue 2, 2014, Pages 197-207

  Di Veroli, Giovanni Y ^a,b,c   Davies, Mark R ^b   Zhang, Henggui ^a   Abi Gerges, Najah ^b   Boyett, Mark R ^a  

^a UNIVERSITY OF MANCHESTER   (United Kingdom)

^b ASTRAZENECA   (United Kingdom)

^c UNIVERSITY OF CAMBRIDGE   (United Kingdom)

Author keywords

computational modeling; drug binding kinetics; hERG ion channel; pro arrhythmia; QT prolongation; Torsades de Pointes; ventricular tachycardia

Indexed keywords

CALCIUM CHANNEL BLOCKING AGENT; ERG1 POTASSIUM CHANNEL; POTASSIUM CHANNEL HERG; PROTEIN BINDING;

ANIMAL; ANTAGONISTS AND INHIBITORS; BINDING SITE; BIOLOGICAL MODEL; CHEMICAL MODEL; CHEMICALLY INDUCED; COMPUTER SIMULATION; DOG; DOSE RESPONSE; DRUG SCREENING; HEART ARRHYTHMIA; HUMAN; KINETICS; METABOLISM; PROCEDURES; THERAPEUTIC EQUIVALENCE;

ANIMALS; ARRHYTHMIAS, CARDIAC; BINDING SITES; CALCIUM CHANNEL BLOCKERS; COMPUTER SIMULATION; DOGS; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG EVALUATION, PRECLINICAL; ETHER-A-GO-GO POTASSIUM CHANNELS; HUMANS; KINETICS; MODELS, CARDIOVASCULAR; MODELS, CHEMICAL; PROTEIN BINDING; THERAPEUTIC EQUIVALENCY;

EID: 84894025279     PISSN: 10453873     EISSN: 15408167     Source Type: Journal    
DOI: 10.1111/jce.12289     Document Type: Article

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