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Open AccessCommunication

Studies of Conorfamide-Sr3 on Human Voltage-Gated Kv1 Potassium Channel Subtypes

1
Laboratorio de Toxinología Marina, Unidad Académica de Ecología y Biodiversidad Acuática, Instituto de Ciencias del Mar y Limnología, Universidad Nacional Autónoma de México, Ciudad de México 04510, Mexico
2
Posgrado en Ciencias Biológicas, Facultad de Ciencias, Universidad Nacional Autónoma de México, Ciudad de México 04510, Mexico
3
Laboratorio de Neurofarmacología Marina, Departamento de Neurobiología Celular y Molecular, Instituto de Neurobiología, Universidad Nacional Autónoma de México, Juriquilla, Qro. 76230, Mexico
4
Programa de Becas Posdoctorales de la Dirección General de Asuntos del Personal Académico (DGAPA-UNAM), Universidad Nacional Autónoma de México, Ciudad de México 04510, Mexico
5
Department of Biology, University of Utah, Salt Lake City, UT 84112, USA
*
Author to whom correspondence should be addressed.
Mar. Drugs 2020, 18(8), 425; https://doi.org/10.3390/md18080425
Received: 27 May 2020 / Revised: 12 July 2020 / Accepted: 13 July 2020 / Published: 13 August 2020
(This article belongs to the Special Issue Cone Snail Venom Peptides, from Treasure Hunt to Drug Leads)
Recently, Conorfamide-Sr3 (CNF-Sr3) was isolated from the venom of Conus spurius and was demonstrated to have an inhibitory concentration-dependent effect on the Shaker K+ channel. The voltage-gated potassium channels play critical functions on cellular signaling, from the regeneration of action potentials in neurons to the regulation of insulin secretion in pancreatic cells, among others. In mammals, there are at least 40 genes encoding voltage-gated K+ channels and the process of expression of some of them may include alternative splicing. Given the enormous variety of these channels and the proven use of conotoxins as tools to distinguish different ligand- and voltage-gated ion channels, in this work, we explored the possible effect of CNF-Sr3 on four human voltage-gated K+ channel subtypes homologous to the Shaker channel. CNF-Sr3 showed a 10 times higher affinity for the Kv1.6 subtype with respect to Kv1.3 (IC50 = 2.7 and 24 μM, respectively) and no significant effect on Kv1.4 and Kv1.5 at 10 µM. Thus, CNF-Sr3 might become a novel molecular probe to study diverse aspects of human Kv1.3 and Kv1.6 channels. View Full-Text
Keywords: Conus spurius; FMRFamide peptides; conorfamides; CNF-Sr3; Shaker K+ channels; Kv1 voltage-gated K+ channels Conus spurius; FMRFamide peptides; conorfamides; CNF-Sr3; Shaker K+ channels; Kv1 voltage-gated K+ channels
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López-Vera, E.; Martínez-Hernández, L.; Aguilar, M.B.; Carrillo, E.; Gajewiak, J. Studies of Conorfamide-Sr3 on Human Voltage-Gated Kv1 Potassium Channel Subtypes. Mar. Drugs 2020, 18, 425.

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