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IQM-22110, a new selective inhibitor of KChIP3 and its electrophysiological effects on Kv4.3, Kv4.3/KChIP3 and Kv4.3/KChIP2 currents

2023; Elsevier BV; Volume: 122; Issue: 3 Linguagem: Inglês

10.1016/j.bpj.2022.11.1474

1542-0086

Paula G. Socuéllamos, Ángela de Benito-Bueno, Maria Ropero, Sara Diez, Pablo Elizalde, M. Angeles Bonache, Carmen Viedma, Mercedes Martín‐Martínez, Marta Gutiérrez‐Rodríguez, Carmen Valenzuela,

Mass Spectrometry Techniques and Applications

Kv4 channels generate rapidly activating and inactivating outward currents responsible for the repolarization of both cardiac and neuronal action potentials through ITO (transient outward current) and IA (A-type K+ current), respectively. Kv4 dysfunctions have been identified in both cardiac and neuronal diseases (Brugada syndrome, atrial fibrillation, epilepsy or Alzheimer's disease). However, Kv4 channels need to assemble with regulatory subunits to fully reproduce ITO and IA currents. Among them, we will focus on KChIPs (potassium channel interacting proteins), being KChIP3 predominant in the brain and KChIP2 in both brain and heart.