Voos, Patrick ; Yazar, Mehtap ; Lautenschläger, René ; Rauh, Oliver ; Moroni, Anna ; 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, 46 (6)
Artikel, Bibliographie
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 |
| Art des Eintrags: | Bibliographie |
| 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 |
| Publikationsjahr: | September 2017 |
| Titel der Zeitschrift, Zeitung oder Schriftenreihe: | European biophysics journal : EBJ |
| Jahrgang/Volume einer Zeitschrift: | 46 |
| (Heft-)Nummer: | 6 |
| 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. |
| ID-Nummer: | pmid:28108814 |
| Fachbereich(e)/-gebiet(e): | 10 Fachbereich Biologie 10 Fachbereich Biologie > Plant Membrane Biophyscis (am 20.12.23 umbenannt in Biologie der Algen und Protozoen) |
| Hinterlegungsdatum: | 24 Jan 2017 13:36 |
| Letzte Änderung: | 29 Aug 2017 06:27 |
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