2015
DOI: 10.1038/srep18397
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Abstract: The voltage-gated Kv1.3 K+ channel plays a key role in the activation of T lymphocytes. Kv1.3 blockers selectively suppress immune responses mediated by effector memory T cells, which indicates the great potential of selective Kv1.3 inhibitors in the therapy of certain autoimmune diseases. Anuroctoxin (AnTx), a 35-amino-acid scorpion toxin is a high affinity blocker of Kv1.3, but also blocks Kv1.2 with similar potency. We designed and produced three AnTx variants: ([F32T]-AnTx, [N17A]-AnTx, [N17A/F32T]-AnTx) u… Show more

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Cited by 21 publications
(23 citation statements)
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“…75% of the peak current (Fig. 1A), which is comparable to the inhibition of Kv1.3 with the double mutated peptide [N17A/F32T]-AnTx at identical concentration (89% inhibition in the latter case,26Fig. 1C).…”
Section: Resultssupporting
confidence: 59%
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“…75% of the peak current (Fig. 1A), which is comparable to the inhibition of Kv1.3 with the double mutated peptide [N17A/F32T]-AnTx at identical concentration (89% inhibition in the latter case,26Fig. 1C).…”
Section: Resultssupporting
confidence: 59%
“…For the preparation of the anuroctoxin derived peptides, both the Boc and Fmoc chemistry were used previously with success 26. Since the stability of several Boc compatible Se protecting groups is significantly lower than the corresponding sulfur protecting groups ( e.g.…”
Section: Resultsmentioning
confidence: 99%
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“…Other potential Kv1.3 blockers for autoimmune diseases include BmKTX-D33H, an analog of Buthusmartensi's kaliotoxin (BmKTX) [20] and (N17A/F32T)-AnTx, an analog of the scorpion toxin anuroctoxin [21]. The use of these compounds is successful because Kv1.3 is so dominant in T EM lymphocytes that the concentration needed for the inhibition of this channel in these cells has no effect on leukocyte antimicrobial capabilities [5].…”
Section: Drug Progressmentioning
confidence: 99%
“…TOXINS: A number of toxins, e.g. particular toxins from specific snails (151)(152)(153), scorpions (154)(155)(156)(157)(158), and spiders (159)(160)(161), interact with voltage gated ion channels, sometimes with an extracellular loop of the VSD, or else possibly near the membrane interface. Suggestions of how these interactions with channels are relevant to gating have been proposed.…”
Section: The Absence Of Temperature Dependence In These Calculations:mentioning
confidence: 99%