Removal of Human Ether-à-go-go Related Gene (hERG) K+ Channel Affinity through Rigidity: A Case of Clofilium Analogues

Cardiotoxicity is a side effect that plagues modern drug design and is very often due to the off-target blockade of the human ether-à-go-go related gene (hERG) potassium channel. To better understand the structural determinants of this blockade, we designed and synthesized a series of 40 derivative...

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Veröffentlicht in:	Journal of medicinal chemistry 2013-12, Vol.56 (23), p.9427-9440
Hauptverfasser:	Louvel, Julien, Carvalho, João F. S, Yu, Zhiyi, Soethoudt, Marjolein, Lenselink, Eelke B, Klaasse, Elisabeth, Brussee, Johannes, IJzerman, Adriaan P
Format:	Artikel
Sprache:	eng
Schlagworte:	Anti-Arrhythmia Agents - chemistry Ether-A-Go-Go Potassium Channels - drug effects Ether-A-Go-Go Potassium Channels - metabolism HEK293 Cells Humans Molecular Docking Simulation Patch-Clamp Techniques Potassium Channel Blockers - chemistry Quaternary Ammonium Compounds - chemical synthesis Quaternary Ammonium Compounds - chemistry Quaternary Ammonium Compounds - metabolism Structure-Activity Relationship
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