Enabling a Comeback in Ion Channel Drug Discovery

Ion channels—tiny protein pores in the membranes of each living cell—are the gateways for millions of positively or negatively charged ions that flow in and out of a cell every second, affecting its electrochemical balance and controlling many biological processes. As ion channel functions are intrinsic to basic physiological processes like nerve and muscle activity, pharmaceutically modulating the extent to which ions enter or leave cells has proven very useful and lucrative to drug firms. Ion channel proteins are the second-most targeted class of proteins, behind G-protein coupled receptors (GPCRs), and drugs that modulate ion channels address a set of diseases such as epilepsy, arrhythmia, cystic fibrosis and Type II diabetes, collectively described as channelopathies.

Ion channels aren't just important as drug targets, however. Since certain ion channels may be responsible for unwanted and dangerous side effects associated with a wider range of drug therapies...