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

R Varkevisser; M J C Houtman; T Linder; K C G de Git; H D M Beekman; R R Tidwell; A P Ijzerman; Anna Stary-Weinzinger; M A Vos; M A G van der Heyden

doi:10.1111/bph.12208

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

R Varkevisser
, M J C Houtman
, T Linder
, K C G de Git
, H D M Beekman
, R R Tidwell
, A P Ijzerman
, Anna Stary-Weinzinger
, M A Vos
, M A G van der Heyden (Corresponding author)

Publications: Contribution to journal › Article › Peer Reviewed

Abstract

Drug interference with normal hERG protein trafficking substantially reduces the channel density in the plasma membrane and thereby poses an arrhythmic threat. The chemical substructures important for hERG trafficking inhibition were investigated using pentamidine as a model drug. Furthermore, the relationship between acute ion channel block and correction of trafficking by dofetilide was studied.

Original language	English
Pages (from-to)	1322-1334
Number of pages	13
Journal	British Journal of Pharmacology
Volume	169
Issue number	6
DOIs	https://doi.org/10.1111/bph.12208
Publication status	Published - Jul 2013

Austrian Fields of Science 2012

301206 Pharmacology
106006 Biophysics

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Varkevisser, R., Houtman, M. J. C., Linder, T., de Git, K. C. G., Beekman, H. D. M., Tidwell, R. R., Ijzerman, A. P., Stary-Weinzinger, A., Vos, M. A., & van der Heyden, M. A. G. (2013). Structure-activity relationships of pentamidine-affected ion channel trafficking and dofetilide mediated rescue. British Journal of Pharmacology, 169(6), 1322-1334. https://doi.org/10.1111/bph.12208

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abstract = "Drug interference with normal hERG protein trafficking substantially reduces the channel density in the plasma membrane and thereby poses an arrhythmic threat. The chemical substructures important for hERG trafficking inhibition were investigated using pentamidine as a model drug. Furthermore, the relationship between acute ion channel block and correction of trafficking by dofetilide was studied.",

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AU - Varkevisser, R

AU - Houtman, M J C

AU - Linder, T

AU - de Git, K C G

AU - Beekman, H D M

AU - Tidwell, R R

AU - Ijzerman, A P

AU - Stary-Weinzinger, Anna

AU - Vos, M A

AU - van der Heyden, M A G

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Y1 - 2013/7

N2 - Drug interference with normal hERG protein trafficking substantially reduces the channel density in the plasma membrane and thereby poses an arrhythmic threat. The chemical substructures important for hERG trafficking inhibition were investigated using pentamidine as a model drug. Furthermore, the relationship between acute ion channel block and correction of trafficking by dofetilide was studied.

AB - Drug interference with normal hERG protein trafficking substantially reduces the channel density in the plasma membrane and thereby poses an arrhythmic threat. The chemical substructures important for hERG trafficking inhibition were investigated using pentamidine as a model drug. Furthermore, the relationship between acute ion channel block and correction of trafficking by dofetilide was studied.

U2 - 10.1111/bph.12208

DO - 10.1111/bph.12208

M3 - Article

C2 - 23586323

SN - 0007-1188

VL - 169

SP - 1322

EP - 1334

JO - British Journal of Pharmacology

JF - British Journal of Pharmacology

IS - 6

ER -

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

Abstract

Austrian Fields of Science 2012

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