IndraLab

Statements



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"The goals of this study are to investigate the mechanism and site of action whereby a human ether-a-go-go-related gene (HERG)-specific scorpion peptide toxin, ErgTx, suppresses HERG current."

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"Use of HERG blockers including E-4031 and ergtoxin have still not been tested in vivo studies but do show a promising role in potential use with chemotherapeutic agents or in chemoresistant disease."

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"The corollary of this is that conductance of the CnErg1 blocked fraction of the channel population (∼93%) is zero, i.e., CnErg1 causes complete block of individual hERG channels but ∼7% of the populat[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"In this example, 100 nM CnErg1 caused a 58.6% inhibition of hERG current, which is considerably less than the 83.7% inhibition observed at 22°C (see Fig. 7 A )."

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"ErgTx1 inhibit human and rat ERG1 in a similar manner (IC 50 4-7 nM), however, it was unable to affect human ERG2 current while completely blocked the rat ERG2 channel with poor recuperation (~ IC 50 1 nM)."

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"ErgTx1 suppresses the hERG1 current amplitude and this effect is practically fully reversible ( [10] , see also below)."

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"Most important among these is to determine the mechanism by which CnErg1 blocks hERG current and to explain the observation that high concentrations of CnErg1 cause incomplete block of the channel.The[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"In this study we have systematically examined the possible mechanisms for incomplete block of hERG by CnErg1, namely: 1), modification of hERG gating; 2), incomplete block of single channel conductanc[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"However, rapid superfusion of 10 nM ergtoxin onto cells during depolarisation did not lead to blockade (~ 2 +/-1%), suggesting that ergtoxin can not block HERG channels in the open state, except when [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"