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    Please use this identifier to cite or link to this item: http://ir.cnu.edu.tw/handle/310902800/26680


    標題: Evidence for activation of BKCa channels by a known inhibitor of focal adhesion kinase, PF573228
    作者: So, Edmund Cheung
    Wu, King Chuen
    Liang, Chia-Hua
    Chen, Jen-Yin
    Wu, Sheng-Nan
    貢獻者: 化粧品應用與管理系
    關鍵字: Large-conductance Ca2+-activated K+ channel
    Ca2+-activated K+ current
    PF573228
    Focal adhesion kinase
    日期: 2011-11
    上傳時間: 2013-06-03 15:53:02 (UTC+8)
    出版者: Elsevier
    Pergamon-Elsevier Science Ltd
    摘要: Aims
    PF573228 is an inhibitor of focal adhesion kinase (FAK) and recognized to affect cell adhesion and migration in many types of cells. Its effects on ion currents and membrane potential have been investigated in this study.

    Main method
    Electrophysiological studies of PF573228 actions on ion currents were performed in pituitary tumor (GH3) cells, in GH3 cells transfected with KCa1.1 siRNAs and in human embryonic kidney (HEK) cells expressing α-human slowpoke (α-hSlo).

    Key findings
    In whole-cell experiments, PF573228 reversibly increased the amplitude of Ca2+-activated K+ currents (IK(Ca)) in GH3 cells. In inside-out recordings, this compound added to the bath did not modify single-channel conductance but stimulated large-conductance Ca2+-activated K+ (BKCa) channels with an EC50 value of 3.2 μM. As BKCa-channel activity was stimulated by PF573228 (3 μM), subsequent application of BMS191011 (3 μM) did not further increase channel activity. PF573228 shifted the activation curve of BKCa channels to less positive membrane potential. Change in the kinetic behavior of BKCa channels caused by this compound is a result of the increased backward rate constants between closed states. PF573228 depressed the firing of action potentials in GH3 cells. However, in GH3 cells transfected with KCa1.1 siRNAs, PF573228-stimulated IK(Ca) was abolished. In HEK293T cells expressing α-hSlo, PF573228 enhanced BKCa-channel activity.

    Significance
    In addition to an inhibition of FAK phosphorylation, PF573228 is effective in activating BKCa channels. The direct stimulation of these channels by this compound may contribute to the underlying mechanism through which it influences cell behavior.
    關聯: Life Sciences 89(19-20), pp. 691-701
    Appears in Collections:[化妝品應用與管理系(所)] 期刊論文

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