PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 22046004-0 2012 Molecular determinants of pentamidine-induced hERG trafficking inhibition. Pentamidine 26-37 ETS transcription factor ERG Homo sapiens 46-50 25366487-1 2014 The effects of terfenadine and pentamidine on the human ether-a-go-go related gene (hERG) channel current and its intracellular trafficking were evaluated. Pentamidine 31-42 ETS transcription factor ERG Homo sapiens 84-88 25366487-5 2014 The two drugs inhibited hERG channel function through different mechanisms: terfenadine through direct channel blockade and pentamidine through inhibition of channel trafficking to the cell membrane. Pentamidine 124-135 ETS transcription factor ERG Homo sapiens 24-28 23586323-4 2013 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 154-165 ETS transcription factor ERG Homo sapiens 23-27 23586323-4 2013 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 174-185 ETS transcription factor ERG Homo sapiens 23-27 23586323-6 2013 KEY RESULTS: Structural modifications of pentamidine differentially affected plasma membrane levels of hERG and K(IR)2.1. Pentamidine 41-52 ETS transcription factor ERG Homo sapiens 103-107 23586323-9 2013 Dofetilide corrected pentamidine-induced hERG, but not K(IR)2.1 trafficking defects. Pentamidine 21-32 ETS transcription factor ERG Homo sapiens 41-45 23093599-8 2013 These data showed for the first time the ERG/DNA complex modulation, both in vitro and in cells, by a heterocyclic diamidine that specifically targets a portion of the ERG DNA recognition site. Pentamidine 115-124 ETS transcription factor ERG Homo sapiens 41-44 23093599-8 2013 These data showed for the first time the ERG/DNA complex modulation, both in vitro and in cells, by a heterocyclic diamidine that specifically targets a portion of the ERG DNA recognition site. Pentamidine 115-124 ETS transcription factor ERG Homo sapiens 168-171 22046004-5 2012 The present study was designed to provide a more complete picture of how hERG surface expression is disrupted by pentamidine at the cellular and molecular levels. Pentamidine 113-124 ETS transcription factor ERG Homo sapiens 73-77 22046004-6 2012 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. Pentamidine 66-77 ETS transcription factor ERG Homo sapiens 99-103 22046004-8 2012 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. Pentamidine 114-125 ETS transcription factor ERG Homo sapiens 222-226 22046004-9 2012 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. Pentamidine 22-33 ETS transcription factor ERG Homo sapiens 71-75 22046004-3 2012 At the same time, pentamidine reduces surface expression of the cardiac potassium channel I(Kr)/human ether a-go-go-related gene (hERG). Pentamidine 18-29 ETS transcription factor ERG Homo sapiens 130-134 19652455-0 2009 Effects of acute intravenous administration of pentamidine, a typical hERG-trafficking inhibitor, on the cardiac repolarization process of halothane-anesthetized dogs. Pentamidine 47-58 ETS transcription factor ERG Homo sapiens 70-74 19652455-2 2009 Recent in vitro studies have indicated that hERG trafficking inhibition may play an important role in the onset of pentamidine-induced long QT syndrome. Pentamidine 115-126 ETS transcription factor ERG Homo sapiens 44-48 15711592-0 2005 Pentamidine reduces hERG expression to prolong the QT interval. Pentamidine 0-11 ETS transcription factor ERG Homo sapiens 20-24 15711592-8 2005 Taken together, our data imply that chronic administration of pentamidine at clinically relevant exposure reduces the membrane expression of the hERG channel, which may most likely be the major mechanism of QT prolongation and torsade de pointes reported in man. Pentamidine 62-73 ETS transcription factor ERG Homo sapiens 145-149 15711592-4 2005 Since the effective concentrations of pentamidine on the hERG channel and APD were much higher than clinically relevant exposures (approximately 1 microM free or lower), we speculated that this drug might not prolong the QT interval through direct inhibition of I(Kr) channel. Pentamidine 38-49 ETS transcription factor ERG Homo sapiens 57-61 30631059-6 2019 The suitability of the model for drug safety evaluation is exemplified by repeated assessment of refractory period that permits sensitive analysis of repolarization impairment induced by the multimodal hERG-inhibitor pentamidine. Pentamidine 217-228 ETS transcription factor ERG Homo sapiens 202-206 15340016-6 2005 After overnight exposure, however, pentamidine reduced hERG currents and inhibited trafficking and maturation of hERG with IC(50) values of 5 to 8 microM similar to therapeutic concentrations. Pentamidine 35-46 ETS transcription factor ERG Homo sapiens 55-59 15340016-6 2005 After overnight exposure, however, pentamidine reduced hERG currents and inhibited trafficking and maturation of hERG with IC(50) values of 5 to 8 microM similar to therapeutic concentrations. Pentamidine 35-46 ETS transcription factor ERG Homo sapiens 113-117 15340016-11 2005 We conclude that pentamidine prolongs the cardiac action potential by block of hERG trafficking and reduction of the number of functional hERG channels at the cell surface. Pentamidine 17-28 ETS transcription factor ERG Homo sapiens 79-83 15340016-11 2005 We conclude that pentamidine prolongs the cardiac action potential by block of hERG trafficking and reduction of the number of functional hERG channels at the cell surface. Pentamidine 17-28 ETS transcription factor ERG Homo sapiens 138-142 15340016-12 2005 We propose that pentamidine, like arsenic trioxide, produces QT prolongation and torsades de pointes in patients by inhibition of hERG trafficking. Pentamidine 16-27 ETS transcription factor ERG Homo sapiens 130-134 27084108-10 2016 A long-term study (over 30h) of pentamidine, a hERG trafficking inhibitor, showed a concentration and time-dependent effect of pentamidine. Pentamidine 32-43 ETS transcription factor ERG Homo sapiens 47-51 30391349-2 2019 Pentamidine, an antiprotozoal drug, causes QT prolongation/Torsades de Pointes (TdP) via hERG trafficking inhibition, but 17-AAG, a geldanamycin derivative heat shock protein 90 (Hsp90) inhibitor, has not shown torsadogenic potential clinically, despite Hsp90 inhibitors generally being hypothesized to cause TdP by hERG trafficking inhibition. Pentamidine 0-11 ETS transcription factor ERG Homo sapiens 89-93 30391349-2 2019 Pentamidine, an antiprotozoal drug, causes QT prolongation/Torsades de Pointes (TdP) via hERG trafficking inhibition, but 17-AAG, a geldanamycin derivative heat shock protein 90 (Hsp90) inhibitor, has not shown torsadogenic potential clinically, despite Hsp90 inhibitors generally being hypothesized to cause TdP by hERG trafficking inhibition. Pentamidine 0-11 ETS transcription factor ERG Homo sapiens 316-320 27282640-12 2016 In addition, pentamidine, a hERG trafficking inhibitor which induced irregular beating activity over a more prolonged duration of time was readily flagged in this assay system. Pentamidine 13-24 ETS transcription factor ERG Homo sapiens 28-32 27084108-10 2016 A long-term study (over 30h) of pentamidine, a hERG trafficking inhibitor, showed a concentration and time-dependent effect of pentamidine. Pentamidine 127-138 ETS transcription factor ERG Homo sapiens 47-51