Literature DB >> 28108814

The small neurotoxin apamin blocks not only small conductance Ca2+ activated K+ channels (SK type) but also the voltage dependent Kv1.3 channel.

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

Mesh:

Substances:

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


  24 in total

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Authors:  Amy K Weaver; Valerie C Bomben; Harald Sontheimer
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4.  Design of PAP-1, a selective small molecule Kv1.3 blocker, for the suppression of effector memory T cells in autoimmune diseases.

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5.  Kv1.3 channels are a therapeutic target for T cell-mediated autoimmune diseases.

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Review 7.  The functional network of ion channels in T lymphocytes.

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8.  Margatoxin is a non-selective inhibitor of human Kv1.3 K+ channels.

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  8 in total

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Journal:  Am J Physiol Renal Physiol       Date:  2017-03-08

2.  KCa2 channel localization and regulation in the axon initial segment.

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4.  Prefrontal Cortex KCa2 Channels Regulate mGlu5-Dependent Plasticity and Extinction of Alcohol-Seeking Behavior.

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Review 5.  Small-conductance Ca2+-activated K+ channels: insights into their roles in cardiovascular disease.

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6.  Apamin structure and pharmacology revisited.

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7.  Evaluation of apamin effects on myelination process in C57BL/6 mice model of multiple sclerosis.

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8.  Bioinformatics identification and pharmacological validation of Kcnn3/KCa2 channels as a mediator of negative affective behaviors and excessive alcohol drinking in mice.

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  8 in total

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