Function and regulation of large conductance Ca2+-activated K+ channel in vascular smooth muscle cells

Large conductance Ca2+-activated K+ (BKCa) channels are abundantly expressed in vascular smooth muscle cells. Activation of BKCa channels leads to hyperpolarization of cell membrane, which in turn counteracts vasoconstriction. Therefore, BKCa channels have an important role in regulation of vascular tone and blood pressure. The activity of BKCa channels is subject to modulation by various factors. Furthermore, the function of BKCa channels are altered in both physiological and pathophysiological conditions, such as pregnancy, hypertension and diabetes, which has dramatic impacts on vascular tone and hemodynamics. Consequently, compounds and genetic manipulation that alter activity and expression of the channel might be of therapeutic interest.

► BKCa channels are abundantly expressed in vascular smooth muscle cells. ► BKCa channels participate in regulation of vascular tone and blood pressure. ► BKCa channels are a key player in both cardiovascular adaption and dysfunctions. ► Developing therapeutics is crucial to treat diseases due to BKCa channel alterations.