CHAPTER 11: The Therapeutic Potential of hERG1 K+ Channels for Treating Cancer and Cardiac Arrhythmias
Published:03 Sep 2014
Special Collection: 2014 ebook collection , 2011-2015 industrial and pharmaceutical chemistry subject collectionSeries: Drug Discovery
hERG potassium channels present pharmacologists and medicinal chemists with a dilemma. On the one hand hERG is a major reason for drugs being withdrawn from the market because of drug induced long QT syndrome and the associated risk of inducing sudden cardiac death, and yet hERG blockers are still widely used in the clinic to treat cardiac arrhythmias. Moreover, in the last decade overwhelming evidence has been provided that hERG channels are aberrantly expressed in cancer cells and that they contribute to tumour cell proliferation, resistance to apoptosis, and neoangiogenesis. Here we provide an overview of the properties of hERG channels and their role in excitable cells of the heart and nervous system as well as in cancer. We consider the therapeutic potential of hERG, not only with regard to the negative impact due to drug induced long QT syndrome, but also its future potential as a treatment in the fight against cancer.