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Electrophysiological characterization of new selective KChIP3 modulators

AuthorsPeraza, Diego A.; Cercós, Pilar CSIC; Prieto, Ángela CSIC; Cruz, Alicia de la CSIC; Naranjo, José Ramón; Gutiérrez-Rodríguez, Marta CSIC ORCID ; Valenzuela, Carmen CSIC ORCID CVN; González, Teresa
Issue Date2015
CitationRECI V (2015)
AbstractDREAM, also named calsenilin or KChIP3, is a neuronal calcium sensor that regulates multiple genes after binding to DRE sites in the nucleus. Outside nucleus, DREAM regulates diverse cellular functions by binding to several proteins, one of them the Kv4.3 channel. Kv4.3 channels, after assembling with different modulatory subunits, generate a fast and transient outward potassium current. In the heart, Kv4.3 binds with KChIP2 subunits, generating the Ito1, one of the main repolarizing cardiac currents. In neurons, they associate to KChIP1 or KChIP3 and generate the IA, which is implicated in very specialized functions as learning, memory and behavior. Here, we describe the electrophysiological effects of new compounds designed to bind with high affinity to KChIP3, in Kv4.3 and Kv4.3+KChIP3 channels expressed in CHO cells. PC342 inhibited Kv4.3 and Kv4.3+KChIP3 to a similar extent, whereas PC332 and PC358 inhibited Kv4.3+KChIP3 to a greater extent. Block induced by PC332 was time- and voltage-dependent, consistent with binding to a closed-active state. Therefore, PC332 and PC358 may represent good compounds to develop new drugs that selectively modulate the neuronal electric activity in distinct neuronal populations.
DescriptionResumen del póster presentado a la 5ª Reunión de la Red Española de Canales Iónicos: "Present and future in ion channel research", celebrada en Barcelona (España) del 4 al 6 de octubre de 2015.
Appears in Collections:(IIBM) Comunicaciones congresos
(IQM) Comunicaciones congresos
(CNB) Comunicaciones congresos

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