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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

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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  2. [GetPortalCommentsPageByObjectIdResponse(id=1869188, encodeId=08f41869188c7, content=<a href='/topic/show?id=fd764459a8' target=_blank style='color:#2F92EE;'>#Cell#</a>, beContent=null, objectType=article, channel=null, level=null, likeNumber=30, replyNumber=0, topicName=null, topicId=null, topicList=[TopicDto(id=4459, encryptionId=fd764459a8, topicName=Cell)], attachment=null, authenticateStatus=null, createdAvatar=, createdBy=524d95, createdName=zhaozhouchifen, createdTime=Sun Dec 13 12:14:00 CST 2015, time=2015-12-13, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=1959443, encodeId=22111959443ae, content=<a href='/topic/show?id=dbe6445416' target=_blank style='color:#2F92EE;'>#CEL#</a>, beContent=null, objectType=article, channel=null, level=null, likeNumber=53, replyNumber=0, topicName=null, topicId=null, topicList=[TopicDto(id=4454, encryptionId=dbe6445416, topicName=CEL)], attachment=null, authenticateStatus=null, createdAvatar=, createdBy=a12645, createdName=智智灵药, createdTime=Tue Jul 05 03:14:00 CST 2016, time=2016-07-05, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=1672761, encodeId=f5f416e276180, content=<a href='/topic/show?id=b79b910345c' target=_blank style='color:#2F92EE;'>#解析#</a>, beContent=null, objectType=article, channel=null, level=null, likeNumber=51, replyNumber=0, topicName=null, topicId=null, topicList=[TopicDto(id=91034, encryptionId=b79b910345c, topicName=解析)], attachment=null, authenticateStatus=null, createdAvatar=null, createdBy=f42d26916490, createdName=hongbochen, createdTime=Mon May 23 22:14:00 CST 2016, time=2016-05-23, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=1288157, encodeId=ea2d128815e6c, content=<a href='/topic/show?id=f10658e342d' target=_blank style='color:#2F92EE;'>#新靶点#</a>, beContent=null, objectType=article, channel=null, level=null, likeNumber=42, replyNumber=0, topicName=null, topicId=null, topicList=[TopicDto(id=58734, encryptionId=f10658e342d, topicName=新靶点)], attachment=null, authenticateStatus=null, createdAvatar=, createdBy=acc3210, createdName=lsndxfj, createdTime=Thu Aug 20 00:14:00 CST 2015, time=2015-08-20, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=1442552, encodeId=6bdd1442552bc, content=<a href='/topic/show?id=7aa28e73211' target=_blank style='color:#2F92EE;'>#药物开发#</a>, beContent=null, objectType=article, channel=null, level=null, likeNumber=39, replyNumber=0, topicName=null, topicId=null, topicList=[TopicDto(id=87732, encryptionId=7aa28e73211, topicName=药物开发)], attachment=null, authenticateStatus=null, createdAvatar=null, createdBy=92874938033, createdName=ms1774076774505970, createdTime=Thu Aug 20 00:14:00 CST 2015, time=2015-08-20, status=1, ipAttribution=)]
    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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