| Literature DB >> 28108814 |
Patrick Voos1, Mehtap Yazar1, René Lautenschläger1, Oliver Rauh1, Anna Moroni2, Gerhard Thiel3.
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.Entities:
Keywords: Apamin block; Jurkat; Kv1.3 channel; Lymphocytes; SK channel
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Year: 2017 PMID: 28108814 DOI: 10.1007/s00249-016-1196-0
Source DB: PubMed Journal: Eur Biophys J ISSN: 0175-7571 Impact factor: 1.733