Side-effects of protein kinase inhibitors on ion channels.
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Date
2013-12
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Abstract
Protein kinases are one of the largest gene families and have regulatory roles in all aspects of eukaryotic cell function.
Modulation of protein kinase activity is a desirable therapeutic approach for a number of human diseases associated
with aberrant kinase activity, including cancers, arthritis and cardiovascular disorders. Several strategies have been
used to develop specific and selective protein kinase modulators, primarily via inhibition of phosphorylation and
down-regulation of kinase gene expression. These strategies are effective at regulating intracellular signalling
pathways, but are unfortunately associated with several undesirable effects, particularly those that modulate ion
channel function. In fact, the side-effects have precluded these inhibitors from being both useful experimental tools
and therapeutically viable. This review focuses on the ion channel side-effects of several protein kinase inhibitors and
specifically on those modulating K+, Na+ and Ca2+ ion channels. It is hoped that the information provided with a
detailed summary in this review will assist the future development of novel specific and selective compounds targeting
protein kinases both for experimental tools and for therapeutic approaches.
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Keywords
Bis-indole maleimide, calcium channels, potassium channels, protein kinase C
Citation
Son Youn Kyoung, Park Hongzoo, Firth Amy L, Park Won Sun. Side-effects of protein kinase inhibitors on ion channels. Journal of Biosciences. 2013 Dec; 38(5): 937-949.