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The small neurotoxin apamin blocks not only small conductance Ca(2+) activated K(+) channels (SK type) but also the voltage dependent Kv1.3 channel.

Voos, Patrick and Yazar, Mehtap and Lautenschläger, René and Rauh, Oliver and Moroni, Anna and Thiel, Gerhard (2017):
The small neurotoxin apamin blocks not only small conductance Ca(2+) activated K(+) channels (SK type) but also the voltage dependent Kv1.3 channel.
In: European biophysics journal : EBJ, pp. 517-523, 46, (6), ISSN 1432-1017,
[Article]

Abstract

Apamin is frequently used as a specific blocker of small-conductance Ca(2+)-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.

Item Type: Article
Erschienen: 2017
Creators: Voos, Patrick and Yazar, Mehtap and Lautenschläger, René and Rauh, Oliver and Moroni, Anna and Thiel, Gerhard
Title: The small neurotoxin apamin blocks not only small conductance Ca(2+) activated K(+) channels (SK type) but also the voltage dependent Kv1.3 channel.
Language: English
Abstract:

Apamin is frequently used as a specific blocker of small-conductance Ca(2+)-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.

Journal or Publication Title: European biophysics journal : EBJ
Volume: 46
Number: 6
Divisions: 10 Department of Biology
10 Department of Biology > Plant Membrane Biophysics
Date Deposited: 24 Jan 2017 13:36
Identification Number: pmid:28108814
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