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- W3150682710 abstract "Using biochemical and electrophysiological methods we found that pentamidine exclusively inhibits hERG export from the endoplasmic reticulum to the cell surface in a heterologous expression system as well as in cardiomyocytes. hERG trafficking inhibition could be rescued in the presence of the pharmacological chaperone astemizole. We used rescue experiments in combination with an extensive mutational analysis to locate an interaction site for pentamidine at phenylalanine 656, a crucial residue in the canonical drug binding site of terminally folded hERG. Our data suggest that pentamidine binding to a folding intermediate of hERG arrests channel maturation in a conformational state that cannot be exported from the endoplasmic reticulum. We propose that pentamidine is the founding member of a novel pharmacological entity whose members act as small molecule ‘antichaperones’." @default.
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- W3150682710 date "2012-01-01" @default.
- W3150682710 modified "2023-09-27" @default.
- W3150682710 title "Direct Inhibitory Effect of Fluoxetine on TREK-2 Channel" @default.
- W3150682710 hasPublicationYear "2012" @default.
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