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The small neurotoxin apamin blocks not only small conductance Ca2+ activated K+ channels (SK type) but also the voltage dependent Kv1.3 channel.
Voos, Patrick; Yazar, Mehtap; Lautenschläger, René; Rauh, Oliver; Moroni, Anna; Thiel, Gerhard.
Afiliação
  • Voos P; Department of Biology, Plant Membrane Biophysics, Technische Universität Darmstadt, Schnittspahnstrasse 3, 64287, Darmstadt, Germany.
  • Yazar M; Department of Biology, Plant Membrane Biophysics, Technische Universität Darmstadt, Schnittspahnstrasse 3, 64287, Darmstadt, Germany.
  • Lautenschläger R; Department of Biology, Plant Membrane Biophysics, Technische Universität Darmstadt, Schnittspahnstrasse 3, 64287, Darmstadt, Germany.
  • Rauh O; Department of Biology, Plant Membrane Biophysics, Technische Universität Darmstadt, Schnittspahnstrasse 3, 64287, Darmstadt, Germany.
  • Moroni A; Department of Biology and CNR IBF-Mi, Università degli Studi di Milano, Milan, Italy.
  • Thiel G; Department of Biology, Plant Membrane Biophysics, Technische Universität Darmstadt, Schnittspahnstrasse 3, 64287, Darmstadt, Germany. thiel@bio.tu-darmstadt.de.
Eur Biophys J ; 46(6): 517-523, 2017 Sep.
Article em En | MEDLINE | ID: mdl-28108814
ABSTRACT
Apamin is frequently used as a specific blocker of small-conductance Ca2+-activated (SK type) K+ channels. Here we show that the small neurotoxin is not as specific as anticipated. It is also a high-affinity inhibitor with an IC50 of 13 nM of the Kv1.3 channel; it blocks the latter with potency similar to the Kv1.3 blocker PAP-1. Since SK type channels and Kv1.3 channels are frequently coexpressed in different tissues such as cells of the immune system, apamin must be used with caution as a pharmacological tool.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Apamina / Canais de Potássio Cálcio-Ativados / Bloqueadores dos Canais de Potássio / Canal de Potássio Kv1.3 / Neurotoxinas Limite: Humans Idioma: En Ano de publicação: 2017 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Apamina / Canais de Potássio Cálcio-Ativados / Bloqueadores dos Canais de Potássio / Canal de Potássio Kv1.3 / Neurotoxinas Limite: Humans Idioma: En Ano de publicação: 2017 Tipo de documento: Article