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Tamoxifen inhibits KCNH2. 16 / 20
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"The major findings of the present study were as follows: 1) endoxifen, the active metabolite of tamoxifen, inhibited hERG tail currents in a concentration-dependent manner; 2) endoxifen preferentially[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"In particular, tamoxifen inhibits the activity of the human ether-a-go-go-related gene (hERG) channels expressed in Xenopus oocytes at supratherapeutic concentrations ( Thomas et al., 2003 )."
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"Long ago, it was demonstrated that Kv11.1 current was inhibited by tamoxifen ( xref ) and more recently it was shown that such inhibition is actually due to the active metabolite of tamoxifen, named endoxifen ( xref )."
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"Endoxifen reduced the hERG currents by 16.7±0.8% at the end of the depolarizing pulse to +60 mV, which increased to 21.9±1.4% ( n =7, P <0.05) after repolarization to −50 mV, suggesting that endoxifen[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"The major findings of the present study were as follows: 1) endoxifen, the active metabolite of tamoxifen, inhibited hERG tail currents in a concentration-dependent manner; 2) endoxifen preferentially[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"For example, the hERG inhibitory activity of dactinomycin from cytotoxic antibiotics and tamoxifen from endocrine therapy had been validated by in vitro assays. xref , xref Tamoxifen inhibited hERG at −50mV in a concentration-dependent manner with IC 50 value of 1.2 μM. xref Dactinomycin markedly reduced the hERG mRNA levels as well. xref Moreover, amsacrine, an antineoplastic agent used in acute lymphoblastic leukemia, had been confirmed to block hERG in HEK 293 cells with IC 50 values of 209.4 nM. xref Finally, we computationally identified multiple novel hERG blockers by deephERG, such as picamycin and bleommycin."
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"Since tamoxifen and endoxifen inhibited hERG currents in a concentration-dependent manner in the present study, QT-prolongation and TdP during tamoxifen administration seem to be, at least in part, as[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"In our study, tamoxifen and endoxifen inhibited hERG currents in a concentration-dependent manner with IC 50 values of 1.2 and 1.6 μM, respectively."
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"Although we did not measure the blocking time constants from the illustrated hERG currents of Fig. 1 , it appears that these drugs had different blocking kinetics: tamoxifen induced a faster block of [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Thus, during tamoxifen treatment, tamoxifen and endoxifen inhibit the hERG currents both by direct channel blockage and by the disruption of channel trafficking."
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"In conclusion, tamoxifen and endoxifen inhibited both hERG currents and the trafficking of the hERG channel protein to the plasma membrane in a concentration-dependent manner."
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"Long ago , it was demonstrated that Kv11.1 current was inhibited by tamoxifen ( Thomas et al ., 2003 ) and more recently it was shown that such inhibition is actually due to the active metabolite of tamoxifen , named endoxifen ( Chae et al ., 2015 ) ."
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"Tamoxifen blocked HERG potassium channels with an IC (50) value of 45.3 microM."
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"This study demonstrates that HERG potassium channels are blocked by the antiestrogenic drug tamoxifen."
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"It is worth recalling here that Tamoxifen (one of the most used drugs for BC treatment) was shown to block hERG1 currents [XREF_BIBR], a fact that could explain the QT interval elongation observed in Tamoxifen treated patients."
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"Using immunoblot, we studied whether tamoxifen and endoxifen inhibited hERG channel protein trafficking."
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