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Ion channels are integral membrane proteins that catalyze the flux of ions across cell membranes, and play fundamental roles in a wide variety of functions throughout the body. In this post-genomic era, when the genes encoding most ion channels have been deciphered with their function remaining elusive yet, a full exploration of the channel proteins has become a new frontier of biological and biomedical research. The present ion channel study is a multidisciplinary research embracing various fields of science. We wish that the Ion Channel special issue would provide new insights into ion channel research and drug discovery.