IndraLab

Statements

Potassium channel toxin gamma-KTx 2.1 inhibits KCNH2. 13 / 13
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"Statistical significance was considered when p < 0.05.The effects of HERG current block by E-4031, BeKm-1, astemizole, terfenadine, and ketoconazole were examined using Protocol-O, Protocol-C, and the[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"The effect of an intermediate concentration of BeKm-1 (5 nM) that does not fully block hERG channels was tested on AP of spontaneously beating hiPS-CMs (XREF_FIG A)."
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"Rapid superfusion of 25 nM BeKm-1 onto cells during depolarisation led to HERG blockade (~ 23 +/-1%, which is of similar magnitude to that seen at the end of depolarisations in Fig. 2F), suggesting th[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"BeKm-1 inhibited hERG1 channels with an IC (50) of 3.3 nm, but had no effect at 100 nm on hEAG, hSK1, rSK2, hIK, hBK, KCNQ1 and KCNE1, KCNQ2 and KCNQ3, KCNQ4 channels, and minimal effect on rELK1."
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"Previous data showed that the maximum degree of hERG current suppression by BeKm-1 was 90 +/- 1% (28)."
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"In addition, the hERG-blocking scorpion toxins, including BeKm-1, have been reported to block from outside the cell [18] ."
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"For WT BeKm-1 binding to the WT hERG channel, we have shown that the maximal degree of BeKm-1 suppression of WT hERG was ~ 90%, and the K d value estimated based on a single toxin concentration (10 nM[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"BeKm-1 does not totally suppress hERG currents : even in the presence of 1000 nM BeKm-1 (100-fold its IC 50) there remained some residual hERG current amounting to ~ 10% of the control amplitude (28)."
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"However, as for BeKm-1, it is feasible that alternative conformational changes independent of inactivation could contribute to the rapid diminution of ergtoxin block upon depolarisation to +80 mV.Coll[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"BeKm-1 blockade of HERG varies inversely with temperature, time, voltage, use and frequency, and this has not been shown before for this or any other HERG blocking compound."
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"The most studied of these are the scorpion toxins, like BeKm-1, which inhibit hERG channel function with nanomolar (nM) potency — a consequence of specific interactions between amino acid residues of [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"As summarized in Fig. 5 C, inhibition of hERG by BeKm-1 was higher at negative voltages and declined at more positive voltages."
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"Examples include charybdotoxin (ChTX), which is targeted toward Kv1.3 and BKCa channels XREF_BIBR, scyllatoxin (ScyTx), which inhibits SKCa channels XREF_BIBR, maurotoxin (MTX), which is targeted toward IKCa channels XREF_BIBR, and BeKm-1, which inhibits Herg channels XREF_BIBR."
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