IndraLab

Statements

BeKm-1 inhibits KCNH2. 11 / 11
| 11
reach
"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."
12860380
reach
"As summarized in Fig. 5 C, inhibition of hERG by BeKm-1 was higher at negative voltages and declined at more positive voltages."
19720020
reach
"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]"
12860380
reach
"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]"
12860380
reach
"Our focus here is BeKm-1, a HERG specific peptide toxin that can suppress HERG in the low nM concentration range."
12719233
reach
"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."
11136720
reach
"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."
23573241
reach
"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)."
17293393
reach
"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]"
17293393
reach
"Previous data showed that the maximum degree of hERG current suppression by BeKm-1 was 90 +/- 1% (28)."
17293393
reach
"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)."
32998413