Title : Structure-activity relationships of pentamidine-affected ion channel trafficking and dofetilide mediated rescue.

Pub. Date : 2013 Jul

PMID : 23586323






4 Functional Relationships(s)
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1 EXPERIMENTAL APPROACH: hERG and K(IR)2.1 trafficking in HEK293 cells was evaluated by Western blot and immunofluorescence microscopy after treatment with pentamidine and six pentamidine analogues, and correction with dofetilide and four dofetilide analogues that displayed different abilities to inhibit IKr . Pentamidine ETS transcription factor ERG Homo sapiens
2 EXPERIMENTAL APPROACH: hERG and K(IR)2.1 trafficking in HEK293 cells was evaluated by Western blot and immunofluorescence microscopy after treatment with pentamidine and six pentamidine analogues, and correction with dofetilide and four dofetilide analogues that displayed different abilities to inhibit IKr . Pentamidine ETS transcription factor ERG Homo sapiens
3 KEY RESULTS: Structural modifications of pentamidine differentially affected plasma membrane levels of hERG and K(IR)2.1. Pentamidine ETS transcription factor ERG Homo sapiens
4 Dofetilide corrected pentamidine-induced hERG, but not K(IR)2.1 trafficking defects. Pentamidine ETS transcription factor ERG Homo sapiens