Calcium and Sodium Activated Potassium Channel Related Drug Discovery Products

Various tissues' ability to operate depends heavily on calcium signaling cascades. Calcium-activated K⁺ (KCa) channels open in response to increases in cytosolic calcium, modulating calcium-signaling cascades by controlling the membrane potential in both electrically excitable and nonexcitable cells. The three families of KCa channels (BK, SK, and IK) are based on their genetic relationships, single channel conductances, and molecular mechanisms for "sensing" calcium. Creative Biolabs can offer calcium and sodium activated potassium channel related products to contribute to the success of drug discovery.

Overview of Calcium and Sodium Activated Potassium Channel

• BKCa

The BK channel, often referred to as the K_Ca1.1 channel, has most likely been the subject of more experimental study than all the other channels put together. This channel has a very high unitary conductance, 200 pS or more in symmetrical K⁺ concentrations, which has helped to increase its popularity. Ca²⁺ levels that are increased by tens to hundreds of micromolars cause the K_Ca1.1 channels to open. These comparatively high physiologic concentrations are attained near plasma membrane Ca²⁺ channels or at locations where intracellular reserves of Ca²⁺ are released. The fact that K_Ca1.1 contains seven transmembrane domains sets it apart from all other K⁺ channels. There is an extra domain known as S0 that comes before the traditional six transmembrane domains S1–S6 that are shared by all voltage-dependent KV family channels. Because of this, the N-termini of K_Ca1.1 proteins are found outside, not within, of a cell.

• SKCa

Three individuals make up the SKCa (K_Ca2) family: SK1, SK2, and SK3. The six alpha-helical transmembrane segments, S1–S6, and the consensus K⁺-selective pore sequence between S5 and S6 of K_Ca2 channels' transmembrane structure are similar to those of the voltage-dependent KV family of channels. However, unlike voltage-dependent channels, the fourth transmembrane segment S4 only contains a few positively charged residues. The K_Ca2 family of channels show linear current-voltage relationships and are insensitive to changes in transmembrane voltage, which is consistent with the S4 segment's function as a voltage sensor in KV channels.

• IKCa

The K_Ca3.1 family of channels, which were formerly known as SK4 channels, is closely connected to the K_Ca2 family. The name IK (for intermediate conductance for K⁺), which has also been frequently used to refer to these channels, was inspired by the fact that their unitary conductance is higher than that of K_Ca2 channels. Since it is expressed at high levels and affects volume regulation in Ca²⁺-activated K⁺ conductance, K_Ca3.1's characteristics closely resemble that conductance. Additionally, it is a key Ca²⁺-activated K⁺ channel in immune cells like human T lymphocytes. Additional nonexcitable tissues where K_Ca3.1 is important include fibroblasts, dedifferentiated vascular smooth muscle cells, secretory epithelia, and the vascular endothelium. K_Ca3.1 controls membrane potential and Ca²⁺ signaling in each of these organs.