BK channel screening allows investigation of the functional and pharmacological impact of β-subunit expression using electrophysiology. Sygnature Discovery provides detailed profiling to support BK channel-focussed drug discovery and lead optimization.
Introduction
BK channels, widely recognized as high-conductance voltage and calcium-activated potassium channels, are transmembrane proteins consisting of four pore-forming α subunits (Figure 1). Each α subunits is comprised of seven transmembrane segments, encompassing a voltage sensor domain and a pore-forming domain.
Figure 1: Schematic representation of the BK channel structure composed of the alpha and beta subunits.
Far from passive entities, BK channels have a unique dual activation mechanism, responding to both membrane depolarization and intracellular calcium concentrations. This distinctive trait enables BK channels to finely modulate cellular excitability and signalling pathways. Activation triggers a cascade where BK channels facilitate the efflux of potassium ions, inducing membrane hyperpolarization and effectively diminishing cellular excitability. Beyond their primary duty in overseeing the smooth muscle tone across vital tissues such as blood vessels, urinary blader, and the gastrointestinal tract, BK channels play a pivotal role in modulating neuronal excitability and synaptic transmission. Sygnature Discovery have developed a suite of comprehensive assays showcasing calcium sensitivity, kinetics, activator and inhibitor profiling, reproducibility benchmarks, and I-V assays. At Sygnature Discovery, we don’t just offer customizable assays; we provide a pathway to novel insights, providing your research with data you can trust.
