[HTML][HTML] Physicochemical features of the HERG channel drug binding site
D Fernandez, A Ghanta, GW Kauffman… - Journal of Biological …, 2004 - ASBMB
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 previously identified 2 aromatic
residues, Tyr-652 and Phe-656, located in the S6 domain of hERG, as critical sites of …
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 previously identified 2 aromatic
residues, Tyr-652 and Phe-656, located in the S6 domain of hERG, as critical sites of …