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Cell reports：科学家解析PKC精细结构为药物开发提供新靶点

2015-08-18 佚名 生物谷

PKC蛋白激酶
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蛋白激酶C(PKC)是通过磷酸化调节其他蛋白活性的一类蛋白激酶。这种简单的生化过程对于决定细胞存亡至关重要。如果PKC活性发生异常，会导致许多疾病的发生。在一项发表在国际学术期刊cell reports上的最新研究中，来自美国加州大学圣地亚哥分校的研究人员对PKC的精细结构进行了进一步解析，为调节PKC的活性提供了新的靶点。研究人员指出，通过理解PKC如何保持结构紧闭，我们可以寻找新的方法使其开放

蛋白激酶C(PKC)是通过磷酸化调节其他蛋白活性的一类蛋白激酶。这种简单的生化过程对于决定细胞存亡至关重要。如果PKC活性发生异常，会导致许多疾病的发生。

在一项发表在国际学术期刊cell reports上的最新研究中，来自美国加州大学圣地亚哥分校的研究人员对PKC的精细结构进行了进一步解析，为调节PKC的活性提供了新的靶点。

研究人员指出，通过理解PKC如何保持结构紧闭，我们可以寻找新的方法使其开放保持活性，如果可以做到这一点就可以促进肿瘤细胞死亡，这对于开发肿瘤治疗策略非常重要。除此之外，如何在神经退行性疾病中保持神经元存活也需要对PKC的结构有深入了解。

在之前的一项研究中，另一个研究小组解析了PKC的大部分结构并对PKC不同结构如何聚集在一起进行了出色的推测，但事实表明这一发现与PKC的工作机制并不能很好匹配。

在这项研究中，研究人员利用X线晶体照相技术进行了结构分析，在此基础上进行进一步推测，对PKC的不同部分如何结合在一起进行了深入分析。最终得出一个与之前不同的PKC结构，并利用一种复杂的细胞成像技术对PKC的不同部分是否能够恰当整合在一起进行了检测。

结果表明PKC的钙离子结合结构域能够与自身尾巴以及催化结构域发生相互作用，锁定酶的活性，使其保持失活状态。当钙离子与PKC结合，钙离子结合结构域与细胞膜搭桥，PKC就会激活发挥酶的催化活性。

综上所述，这项研究利用结构生物学的方法对PKC的结构进行了精细解析，这对于开发小分子药物开启或关闭PKC的活性用于治疗多种疾病具有重要意义。

原文出处：

Corina E. Antal1, Julia A et al.Intramolecular C2 Domain-Mediated Autoinhibition of Protein Kinase C βII.cell reports.2015

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    2015-12-13 zhaozhouchifen

    #Cell#

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    2016-07-05 智智灵药

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    2016-05-23 hongbochen

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    2015-08-20 lsndxfj

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    2015-08-20 ms1774076774505970

    #药物开发#

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