Products/Services Used | Details | Operation |
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PCR Cloning and Subcloning> | Briefly, the rat KCa2.2a, human KCa2.1, human KCa2.3, or human KCa3.1 channel cDNA constructs were either generated in-house or through molecular cloning services (Genscript, Piscataway, NJ, USA). | Get A Quote |
Small-conductance Ca2+-activated potassium (KCa2.x) channels are gated exclusively by intracellular Ca2+. The activation of KCa2.3 channels induces hyperpolarization, which augments Ca2+ signaling in endothelial cells. Cilia are specialized Ca2+ signaling compartments. Here, we identified compound 4 that potentiates human KCa2.3 channels selectively. The subtype selectivity of compound 4 for human KCa2.3 over rat KCa2.2a channels relies on an isoleucine residue in the HA/HB helices. Positive modulation of KCa2.3 channels by compound 4 increased flow-induced Ca2+ signaling and cilia length, while negative modulation by AP14145 reduced flow-induced Ca2+ signaling and cilia length. These findings were corroborated... More