Modulation of hERG potassium channels by a novel small molecule activator
journal contributionposted on 09.05.2018, 12:04 by John S. Mitcheson, Jules C. Hancox
(Opening paragraph) KCNH2-encoded hERG1 channels conduct the rapid delayed rectifier potassium current (IKr), which plays a vital role in controlling the duration of cardiac action potentials. Ever since the importance of hERG1 currents in regulating cardiac repolarisation was first demonstrated there has been considerable interest in pharmacologically manipulating these channels. In this issue, Sale et al. (2017), have characterised the properties of a structurally and functionally novel hERG activator, ITP-2, which dramatically increases hERG1 current amplitudes.