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 (Korresp. Autor*in)

Veröffentlichungen: Beitrag in Fachzeitschrift › Artikel › 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.

Originalsprache	Englisch
Seiten (von - bis)	1322-1334
Seitenumfang	13
Fachzeitschrift	British Journal of Pharmacology
Jahrgang	169
Ausgabenummer	6
DOIs	https://doi.org/10.1111/bph.12208
Publikationsstatus	Veröffentlicht - Juli 2013

ÖFOS 2012

301206 Pharmakologie
106006 Biophysik

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10.1111/bph.12208

Zitationsweisen

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.",

author = "R Varkevisser and Houtman, \{M J C\} and T Linder and \{de Git\}, \{K C G\} and Beekman, \{H D M\} and Tidwell, \{R R\} and Ijzerman, \{A P\} and Anna Stary-Weinzinger and Vos, \{M A\} and \{van der Heyden\}, \{M A G\}",

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year = "2013",

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doi = "10.1111/bph.12208",

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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

PY - 2013/7

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

ÖFOS 2012

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