Article
Physicochemical features of the HERG channel drug binding site.
The Journal of biological chemistry - 12 Mar 2004
Fernandez David, Ghanta Azad, Kauffman Gregory W, Sanguinetti Michael C
Abstract excerpt
Blockade of hERG K(+) channels in the heart is an unintentional side effect of many drugs and can induce cardiac arrhythmia and sudden death. It has become common practice in the past few years to screen compounds for hERG channel activity early during the drug discovery process. Understanding the molecular basis of drug binding to hERG is crucial for the rational design of medications devoid of this activity. We...
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