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논문 기본 정보
- 자료유형
- 학술저널
- 저자정보
- 저널정보
- 대한약리학회 The Korean Journal of Physiology & Pharmacology The Korean Journal of Physiology & Pharmacology 제15권 제5호
- 발행연도
- 2011.1
- 수록면
- 291 - 297 (7page)
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The effect of cyclosporin A (CsA), an immunosuppressant, on human ether-a-go-go-related gene (HERG) channel as it is expressed in human embryonic kidney cells was studied using a whole-cell, patch-clamp technique. CsA inhibited the HERG channel in a concentration-dependent manner, with an IC50 value and a Hill coefficient of 3.17μM and 0.89, respectively. Pretreatment with cypermethrine, a calcineurin inhibitor, had no effect on the CsA-induced inhibition of the HERG channel. The CsA-induced inhibition of HERG channels was voltage-dependent, with a steep increase over the voltage range of the channel opening. However, the inhibition exhibited voltage independence over the voltage range of fully activated channels. CsA blocked the HERG channels predominantly in the open and inactivated states rather than in the closed state. Results of the present study suggest that CsA acts directly on the HERG channel as an open-channel blocker, and it acts independently of its effect on calcineurin activity.
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참고문헌 (23)
참고문헌 신청
Cayabyab FS / 2002 / Regulation of an ERG K＋ current by Src tyrosine kinase / J Biol Chem 277 : 13673 ~ 13681
Cockerill SL / 2007 / Modulation of hERG potassium currents in HEK-293 cells by protein kinase C. Evidence for direct phosphorylation of pore forming subunits / J Physiol 58
Curran ME / 1995 / A molecular basis for cardiac arrhythmia: HERG mutations cause long QT syndrome / Cell 80 : 795 ~ 803
Damjanovich S / 1987 / Cyclosporin depolarizes human lymphocytes: earliest observed effect on cell metabolism / Eur J Immunol 17 : 763 ~ 768
Hamill OP / 1981 / Improved patch-clamp techniques for high-resolution current recording from cells and cell-free membrane patches / Pflugers Arch 391 : 85 ~ 100
Cockerill SL / 2007 / Modulation of hERG potassium currents in HEK-293 cells by protein kinase C. Evidence for direct phosphorylation of pore forming subunits / J Physiol 58
Curran ME / 1995 / A molecular basis for cardiac arrhythmia: HERG mutations cause long QT syndrome / Cell 80 : 795 ~ 803
Damjanovich S / 1987 / Cyclosporin depolarizes human lymphocytes: earliest observed effect on cell metabolism / Eur J Immunol 17 : 763 ~ 768
Hamill OP / 1981 / Improved patch-clamp techniques for high-resolution current recording from cells and cell-free membrane patches / Pflugers Arch 391 : 85 ~ 100
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