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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 ; Yazar, Mehtap ; Lautenschläger, René ; Rauh, Oliver ; Moroni, Anna ; Thiel, Gerhard :
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, 46 (6) pp. 517-523. ISSN 1432-1017
[Artikel], (2017)

Kurzbeschreibung (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.

Typ des Eintrags: Artikel
Erschienen: 2017
Autor(en): Voos, Patrick ; Yazar, Mehtap ; Lautenschläger, René ; Rauh, Oliver ; Moroni, Anna ; Thiel, Gerhard
Titel: The small neurotoxin apamin blocks not only small conductance Ca(2+) activated K(+) channels (SK type) but also the voltage dependent Kv1.3 channel.
Sprache: Englisch
Kurzbeschreibung (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.

Titel der Zeitschrift, Zeitung oder Schriftenreihe: European biophysics journal : EBJ
Band: 46
(Heft-)Nummer: 6
Fachbereich(e)/-gebiet(e): 10 Fachbereich Biologie
10 Fachbereich Biologie > Plant Membrane Biophysics
Hinterlegungsdatum: 24 Jan 2017 13:36
ID-Nummer: pmid:28108814
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