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- Title
Pharmacologic Approach to Defective Protein Trafficking in the E637K-hERG Mutant with PD-118057 and Thapsigargin.
- Authors
Mao, Haiyan; Lu, Xiaoli; Karush, Justin Michael; Huang, Xiaoyan; Yang, Xi; Ba, Yanna; Wang, Ying; Liu, Ningsheng; Zhou, Jianqing; Lian, Jiangfang
- Abstract
Treatment of LQT2 is inadequate. Many drugs which can pharmacologically rescue defective protein trafficking in LQT2 also result in potent blockade of HERG current, negating their therapeutic benefit. It is reported that PD-118057 and thapsigargin can rescue LQT2 without hERG channel blockade, but the precise mechanism of action is unknown. Furthermore, the effect of PD-118057 and thapsigargin on the dominant negative E637K-hERG mutant has not been previously investigated.
- Publication
PloS one, 2013, Vol 8, Issue 6, pe65481
- ISSN
1932-6203
- Publication type
Journal Article
- DOI
10.1371/journal.pone.0065481