The present volume of our series “Methods and Principles in Medicinal Chemistry”
is dedicated to “Voltage-gated Ion Channels” and their impact as targets for
drug design.
Ion channels are ubiquitously distributed throughout cellular life; they represent
integral membrane proteins that both produce and transduce the electrical signals
crucial to the maintenance and function of cells. Ion channels gate or regulate the
ion flow between the cytoplasmic compartment and the extracellular space and
between subcellular compartments. They open and close in response to changes
in membrane potential, changes in ion concentrations on either side of the membrane,
and agonist binding to the channel or closely associated regulatory proteins.
Under pathological conditions ion channels contribute to or drive a variety of
disease processes from achalasia and arrhythmias to xerostomia and vertigo.