The Ca21-dependent K1-channel KCa3.1 as a therapeutic target in cardiovascular disease

The endothelium is an interesting target tomodify cardiovascular disease. In addition to the well-known autacoids such as nitric oxide and prostaglandins, a third endothelial pathway exists which relaxes vascular smooth muscle through hyperpolarization (endo-thelium-dependent hyperpolarization-type dilation). Herein, calcium-activated potas-sium channels (KCa) are crucial in which two types are expressed in endothelial cells (KCa3.1, KCa2.3). Specifically, KCa3.1 is selectively activated by small molecules that are potentially useful as pharmacological compoundswhich lead to overall vascular dila-tion including the coronary bedandadecrease in arterial pressure. Conversely, blockade of this channel reduces atherosclerosis and neointima formation since under these con-ditions KCa3.1 is up-regulated in phenotypicallymodulated, proliferative smoothmuscle cells and supports migration and proliferation. This review briefly summarizes main ex-perimental findings on this channel