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Statements


CnErg1 inhibits KCNH2. 5 / 5
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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]"

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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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"Collectively, our data provides a plausible kinetic explanation for incomplete blockade of hERG by CnErg1 that is consistent with the proposed highly dynamic conformation of the outer pore domain of hERG."

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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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"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)."