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PI3Kα in cardioprotection: Cytoskeleton, late Na+ current, and mechanism of arrhythmias.
Channels ( IF 3.3 ) Pub Date : 2019-12-02 , DOI: 10.1080/19336950.2019.1697127
Pavel Zhabyeyev 1, 2 , Xueyi Chen 1, 2 , Bart Vanhaesebroeck 3 , Gavin Y Oudit 1, 2
Affiliation  

PI 3-kinase α (PI3Kα) is a lipid kinase that converts phosphatidylinositol-4,5-bisphosphate (PIP2) to phosphatidylinositol-3,4,5-triphosphate (PIP3). PI3Kα regulates a variety of cellular processes such as nutrient sensing, cell cycle, migration, and others. Heightened activity of PI3Kα in many types of cancer made it a prime oncology drug target, but also raises concerns of possible adverse effects on the heart. Indeed, recent advances in preclinical models demonstrate an important role of PI3Kα in the control of cytoskeletal integrity, Na+ channel activity, cardioprotection, and prevention of arrhythmias.



中文翻译:

PI3Kα 在心脏保护中的作用:细胞骨架、晚期 Na+ 电流和心律失常的机制。

PI 3-激酶 α (PI3Kα) 是一种脂质激酶,可将 4,5-二磷酸磷脂酰肌醇 (PIP2) 转化为 3,4,5-三磷酸磷脂酰肌醇 (PIP3)。PI3Kα 调节多种细胞过程,例如营养感应、细胞周期、迁移等。PI3Kα 在多种癌症中的活性增强使其成为主要的肿瘤药物靶点,但也引发了对可能对心脏产生不利影响的担忧。事实上,临床前模型的最新进展证明了 PI3Kα 在控制细胞骨架完整性、Na +通道活性、心脏保护和预防心律失常方面的重要作用。

更新日期:2019-12-02
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