Advancing Kv2.2 Drug Discovery
Sygnature Discovery’s ion channel screening platform provides reliable, high-quality data to support the search of novel starting points for Kv2.2 drug discovery. By integrating well-characterized cellular models with high-throughput fluorescence-based screening and automated electrophysiology, we offer a robust and scalable workflow designed to efficiently progress hit compounds through early-stage characterization.
With extensive expertise in ion channel pharmacology, we tailor each screening cascade to meet the specific needs to the project, ensuring both primary screening and follow-up electrophysiology profiling generate data that supports informed decision-making.
Introduction
Voltage-gated potassium (Kv) channels are transmembrane proteins that mediate the selective passage of K+ ions across cellular membranes, playing critical roles in the regulation of neuronal excitability, cardiac excitability, muscle contraction and hormone secretion. The Kv channel family is categorized into twelve subfamilies – Kv1 to Kv12 – each consisting of multiple α-subunits that assemble into functional tetrameric channels. These channels exhibit distinct biophysical and pharmacological properties and play a critical role in modulating cellular excitability.
Kv2.2 Therapeutic Potential
A recent study has identified a tumour-specific Kv2.2-associated ion channel complex uniquely expressed in GMB cells while absent in healthy brain tissue (Dong et al. 2023). Therapeutic strategies employing synthetic peptides targeting this complex have demonstrated selective cytotoxicity against GMB cells and have significantly extended survival rate in preclinical models. These findings suggest that Kv2.2 may represent a promising molecular target for the development of novel, tumour selective therapies aimed at improving GMB treatment outcomes.
Dong et al., Nature Cancer, 2023, PMID: 37697045
