Title : The Effect of a Synthetic Estrogen, Ethinylestradiol, on the hERG Block by E-4031.

Pub. Date : 2021 Sep 20

PMID : 34572598






6 Functional Relationships(s)
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1 The Effect of a Synthetic Estrogen, Ethinylestradiol, on the hERG Block by E-4031. E 4031 ETS transcription factor ERG Homo sapiens
2 We previously reported that physiological concentrations of some estrogens partially suppress the hERG channel currents by interacting with the S6 residue F656 and increase the sensitivity of hERG blockade by E-4031. E 4031 ETS transcription factor ERG Homo sapiens
3 We previously reported that physiological concentrations of some estrogens partially suppress the hERG channel currents by interacting with the S6 residue F656 and increase the sensitivity of hERG blockade by E-4031. E 4031 ETS transcription factor ERG Homo sapiens
4 On the other hand, EE2 at therapeutic concentrations reduced the degree of hERG current suppression by E-4031. E 4031 ETS transcription factor ERG Homo sapiens
5 The administration of EE2 followed by E-4031 blockade reversed the current suppression, suggesting that the interaction of EE2 and E-4031 alters hERG at the drug-binding site. E 4031 ETS transcription factor ERG Homo sapiens
6 The administration of EE2 followed by E-4031 blockade reversed the current suppression, suggesting that the interaction of EE2 and E-4031 alters hERG at the drug-binding site. E 4031 ETS transcription factor ERG Homo sapiens