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dc.contributor.authorCercós, Pilar
dc.contributor.authorGonzález Vera, Juan Antonio
dc.identifier.citationCercós, P.; Peraza, D.A.; Benito-Bueno, A.d.; Socuéllamos, P.G.; Aziz-Nignan, A.; Arrechaga-Estévez, D.; Beato, E.; Peña-Acevedo, E.; Albert, A.; González-Vera, J.A.; et al. Pharmacological Approaches for the Modulation of the Potassium Channel KV4.x and KChIPs. Int. J. Mol. Sci. 2021, 22, 1419. 10.3390/ijms22031419es_ES
dc.description.abstractIon channels are macromolecular complexes present in the plasma membrane and intracellular organelles of cells. Dysfunction of ion channels results in a group of disorders named channelopathies, which represent an extraordinary challenge for study and treatment. In this review, we will focus on voltage-gated potassium channels (KV), specifically on the KV4-family. The activation of these channels generates outward currents operating at subthreshold membrane potentials as recorded from myocardial cells (ITO, transient outward current) and from the somata of hippocampal neurons (ISA). In the heart, KV4 dysfunctions are related to Brugada syndrome, atrial fibrillation, hypertrophy, and heart failure. In hippocampus, KV4.x channelopathies are linked to schizophrenia, epilepsy, and Alzheimer’s disease. KV4.x channels need to assemble with other accessory subunits (β) to fully reproduce the ITO and ISA currents. β Subunits affect channel gating and/or the traffic to the plasma membrane, and their dysfunctions may influence channel pharmacology. Among KV4 regulatory subunits, this review aims to analyze the KV4/KChIPs interaction and the effect of small molecule KChIP ligands in the A-type currents generated by the modulation of the KV4/KChIP channel complex. Knowledge gained from structural and functional studies using activators or inhibitors of the potassium current mediated by KV4/KChIPs will better help understand the underlying mechanism involving KV4-mediated-channelopathies, establishing the foundations for drug discovery, and hence their treatments.es_ES
dc.description.sponsorshipMinisterio de Ciencia e Innovacion (MICIU) Spain SAF201675021-R PID2019-104366RB-C21 RTI2018-097189-B-C22 PID2019-104366RBC22es_ES
dc.description.sponsorshipInstituto de Salud Carlos III CIBERCV program CB/11/00222es_ES
dc.description.sponsorshipConsejo Superior de Investigaciones Cientificas (CSIC) PIE 201820E104 2019AEP148 201880E109es_ES
dc.description.sponsorshipEuropean Fund for Economic and Regional Development (FEDER)es_ES
dc.description.sponsorshipSpanish Ministry of Economy, Industry, and Competitivity (MINECO)es_ES
dc.description.sponsorshipConsejo Superior de Investigaciones Cientificas (CSIC) BES-2017-080184 FPU2017/02731es_ES
dc.description.sponsorshipDepartment of Atomic Energy (DAE)es_ES
dc.description.sponsorshipCUNY Research Scholars Programes_ES
dc.description.sponsorshipCollegiate Science Technology Entry Program (CSTEP)es_ES
dc.description.sponsorshipHostos Office of Academic Affairses_ES
dc.description.sponsorshipCSIC Open Access Publication Support Initiative through its Unit of Information Resources for Research (URICI)es_ES
dc.rightsAtribución 3.0 España*
dc.subjectVoltage-gated potassium channels KV4es_ES
dc.subjectTransient outward currentes_ES
dc.subjectA-type currentes_ES
dc.subjectPotassium channel interacting proteins (KChIPs)es_ES
dc.subjectProtein–protein interactionses_ES
dc.titlePharmacological Approaches for the Modulation of the Potassium Channel KV4.x and KChIPses_ES

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Atribución 3.0 España
Except where otherwise noted, this item's license is described as Atribución 3.0 España