PNAS:新的激酶检测方法有助于确定开发癌症药物的目标

2017-09-21 佚名 medicalxpress

新的激酶检测方法有助于确定开发癌症药物的目标

新的激酶检测方法有助于确定开发癌症药物的目标

激酶是催化磷酸基团转移到另一种蛋白质的蛋白质,这一过程称为磷酸化,这是蛋白质功能的关键。许多磷酸化蛋白是致癌基因,可以引发癌细胞的形成。

市面上有几十种用于治疗癌症的激酶抑制剂。但癌细胞适应后,使一些药物效果较差。新的激酶靶点将导致新药物的产生,可以使治疗难治性癌症患者的治疗方案多样化,这是一个漫长而乏味的过程。

普渡大学生物化学教授W.AndyTao和ACSCentralScience杂志发表的研究成果的资深作者W.AndyTao说:“这些是癌症生长和增殖的关键分子。可以使癌基因磷酸化的所有替代激酶很重要,所以如果我们看到阻力,就应该重新定位。”

以前没有现有的方法可用于系统地鉴定负责磷酸化癌基因的激酶。来自Purdue的药物化学和分子药理学系(MCMP),化学系和普渡大学癌症研究中心的陶和合作者开发了一种可以快速筛选激酶-蛋白质相互作用的强大方法。

该方法采用称为双分子荧光互补(BiFC)的已知成像测定法,其中将荧光蛋白分成两部分,标记为末端N和C.将一个末端加入到一组激酶中,另一个终端放置靶基因。

“如果两种蛋白质相互作用,它们会将N和C端子拉在一起,并且可以重建完整的荧光蛋白以发出荧光。”胡说。

由于荧光,连接的蛋白质是可见的,但是科学家们可以使用快速质谱鉴定激酶。研究人员在559个人类激酶库中测试了他们的方法,并且能够鉴定出新激酶,并通过其他生物化学检测方式进行确认。

原始出处:

I-Hsuan Chena, Liang Xuea, Chuan-Chih Hsua, et.al. Phosphoproteins in extracellular vesicles as candidate markers for breast cancer. PNAS

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    2018-07-08 drwjr
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    2017-09-23 redcrab
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