Several important new findings have furthered the development of voltage-ga
ted and calcium-activated potassium channel pharmacology. The molecular con
stituents of several members of these large ion channel families were ident
ified. Small-molecule modulators of some of these channels were reported, i
ncluding correolide, the first potent, small-molecule, natural product inhi
bitor of the Shaker family of voltage-gated potassium channels to be disclo
sed. The initial crystal structure of a bacterial potassium channel was det
ermined; this work gives a physical basis for understanding the mechanisms
of ion selectivity and ion conduction. With the recent molecular characteri
zation of a potassium channel structure and the discovery of new templates
for channel modulatory agents, the ability to rationally identify and devel
op potassium channel agonists and antagonists may become a reality in the n
ear future.