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Cell:发现非小细胞肺癌治疗新方法

2017-09-30 佚名 medicalxpress

斯克里普斯研究所的科学家们开发了一种抗癌疗法的新战略,他们使用新发现的小分子抑制剂,有效抑制非小细胞肺癌的增长,非小细胞肺癌占据了肺癌总数的85%,而且目前的治疗方法都不太乐观。

斯克里普斯研究所的科学家们开发了一种抗癌疗法的新战略,他们使用新发现的小分子抑制剂,有效抑制非小细胞肺癌的增长,非小细胞肺癌占据了肺癌总数的85%,而且目前的治疗方法都不太乐观。

研究报告发表于本周的《细胞》杂志中,这种新方法是基于一组复杂的蛋白质组学,核心是承认某些蛋白质中的氨基酸有着特殊的化学反应,让他们形成不可逆共价键,科学家可以大量应用这种分子,或者整个集群的蛋白质所含细胞的这些反应,快速识别潜在药物靶点的蛋白质氨基酸。

在这项研究中,研究人员试图运用这种蛋白质组学策略,发现受到转录因子NRF2影响的药物靶点,NRF2是一种强大的抗氧化剂的开关,但是,一些癌细胞强行使用这一功能,保持活跃,使自己免受药物袭击,并且可以不停地失控增长。现有的药物主要关闭大部分的NRF2,但是,值得注意的是,NRF2负责调节整个身体的基因表达,一旦完全阻隔,就会出现过度的副作用。因此,在此次研究中,研究人员希望找到降低NRF2表达的元素,可以更加安全有效的抑制肺癌的发展。

在研究报告中,科学家指出:“通常我们觉得NRF2等转录因子仅仅通过酶的水平来调节酶的功能,在研究过程中,我们确定了NRF2可以利用本身的特性来塑造酶的环境。这一发现使我们确定了非小细胞肺癌药物的新靶点。”

目前,研究人员正在发起临床试验,用以确定新靶点的安全有效性。

原始出处:

Liron Bar-Peled, Esther K. Kemper, Radu M. Suciu, et.al. Chemical Proteomics Identifies Druggable Vulnerabilities in a Genetically Defined Cancer. Cell

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    2018-09-04 维他命
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likeNumber=106, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=http://thirdwx.qlogo.cn/mmopen/vi_32/Q0j4TwGTfTIxvMP6OXzUiaGH5MkDQlW0hczROZxec1gZjfZ52EtN6aG9t0uDZq2A5xmf9FWMa4tZib4qoYnledFg/132, createdBy=9d6c2167401, createdName=hanmeijinxiu, createdTime=Thu Oct 12 19:55:57 CST 2017, time=2017-10-12, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=249903, encodeId=77d8249903b8, content=学习了谢谢分享!!, beContent=null, objectType=article, channel=null, level=null, likeNumber=97, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=https://img.medsci.cn/20200816/e4675a86ea694f12b82202b320dc2654/12f6b900498349e994ce8f516a584d6a.jpg, createdBy=09431951290, createdName=大爰, createdTime=Tue Oct 03 07:28:38 CST 2017, time=2017-10-03, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=249678, encodeId=70ba2496e87e, content=不错的.学习了.谢谢分享., beContent=null, objectType=article, channel=null, level=null, likeNumber=90, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=https://wx.qlogo.cn/mmopen/mONcle9pic3zMoyicyo6ia9f4IuLQAwZoxD6Hx4ibd5CMcOCYhStY6oDibbKK6O2X8iaicldO5ib8j1iapOIobIKCGiczU2A/0, createdBy=56251941490, createdName=虈亣靌, createdTime=Mon Oct 02 13:08:13 CST 2017, time=2017-10-02, status=1, ipAttribution=)]
    2017-10-20 耐看

    厉害

    0

  8. 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likeNumber=106, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=http://thirdwx.qlogo.cn/mmopen/vi_32/Q0j4TwGTfTIxvMP6OXzUiaGH5MkDQlW0hczROZxec1gZjfZ52EtN6aG9t0uDZq2A5xmf9FWMa4tZib4qoYnledFg/132, createdBy=9d6c2167401, createdName=hanmeijinxiu, createdTime=Thu Oct 12 19:55:57 CST 2017, time=2017-10-12, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=249903, encodeId=77d8249903b8, content=学习了谢谢分享!!, beContent=null, objectType=article, channel=null, level=null, likeNumber=97, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=https://img.medsci.cn/20200816/e4675a86ea694f12b82202b320dc2654/12f6b900498349e994ce8f516a584d6a.jpg, createdBy=09431951290, createdName=大爰, createdTime=Tue Oct 03 07:28:38 CST 2017, time=2017-10-03, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=249678, encodeId=70ba2496e87e, content=不错的.学习了.谢谢分享., beContent=null, objectType=article, channel=null, level=null, likeNumber=90, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=https://wx.qlogo.cn/mmopen/mONcle9pic3zMoyicyo6ia9f4IuLQAwZoxD6Hx4ibd5CMcOCYhStY6oDibbKK6O2X8iaicldO5ib8j1iapOIobIKCGiczU2A/0, createdBy=56251941490, createdName=虈亣靌, createdTime=Mon Oct 02 13:08:13 CST 2017, time=2017-10-02, status=1, ipAttribution=)]
    2017-10-12 hanmeijinxiu

    肺癌治疗的新希望

    0

  9. 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content=不错的.学习了.谢谢分享., beContent=null, objectType=article, channel=null, level=null, likeNumber=90, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=https://wx.qlogo.cn/mmopen/mONcle9pic3zMoyicyo6ia9f4IuLQAwZoxD6Hx4ibd5CMcOCYhStY6oDibbKK6O2X8iaicldO5ib8j1iapOIobIKCGiczU2A/0, createdBy=56251941490, createdName=虈亣靌, createdTime=Mon Oct 02 13:08:13 CST 2017, time=2017-10-02, status=1, ipAttribution=)]
    2017-10-03 大爰

    学习了谢谢分享!!

    0

  10. 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content=不错的.学习了.谢谢分享., beContent=null, objectType=article, channel=null, level=null, likeNumber=90, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=https://wx.qlogo.cn/mmopen/mONcle9pic3zMoyicyo6ia9f4IuLQAwZoxD6Hx4ibd5CMcOCYhStY6oDibbKK6O2X8iaicldO5ib8j1iapOIobIKCGiczU2A/0, createdBy=56251941490, createdName=虈亣靌, createdTime=Mon Oct 02 13:08:13 CST 2017, time=2017-10-02, status=1, ipAttribution=)]
    2017-10-02 虈亣靌

    不错的.学习了.谢谢分享.

    0

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ALK融合基因在非小细胞肺癌(NSCLC)的发生率约占3%~7%,ALK阳性晚期NSCLC患者对ALK抑制剂克唑替尼治疗有效,中位有效期约10个月。与其他分子靶向药物类似,克唑替尼治疗后患者不可避免地发生耐药,如何克服克唑替尼耐药性是临床上很棘手的难题。CH5424802是一种药效与特异性都更强的ALK抑制剂,有望克服ALK基因重排阳性晚期NSCLC患者接受克唑替尼治疗后发生的耐药性。

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