14.08.2020 - A deep-dive into hERG (Kv11.1)
hERG (Kv11.1) - The Voltage-Gated Potassium Channel Beating of Excitement
KV11.1, better known as hERG (human Ether-à-go-go-Related Gene), contributes to the electrical activity of the heart and coordinates the heart's beating (i.e., the hERG channel mediates the repolarizing IKR current in the cardiac action potential). When this channel's ability to conduct electrical current across the cell membrane is inhibited or compromised, either by application of drugs or by rare mutations in some families, it can result in a potentially fatal disorder called long QT syndrome.
A number of clinically successful drugs in the market have had the tendency to inhibit hERG, and create a concomitant risk of sudden death, as a side-effect, which has made hERG inhibition an important antitarget that must be avoided during drug development. Due to the documented potential of QT interval prolonging drugs, the United States Food and Drug Administration issued recommendations for the establishment of a cardiac safety profile during pre-clinical drug development: ICH S7B.
Download the following publication to learn more about Reliable identification of cardiac liability in drug discovery using automated patch clamp.Reliable identification of cardiac liability in drug discovery using automated patch clamp.