Chemistry & Biology ：靶向Exportin-1的新型抗癌药

2015-03-06 佚名生物谷

  一项最新研究发现：基因修饰的癌细胞可以澄清新癌症药物的作用机制。在人类细胞中，细胞核含有我们的DNA，并作为一个“控制中心”，而细胞质充当细胞的“体”。正是在这里，蛋白质得以生成和回收。但是否蛋白质有活性或无活性依赖于它在细胞中的位置。细胞使用运输系统，以确保蛋白质达到需要它的部位。在健康的细胞中，蛋白质不断地在细胞核和细胞质之间被输送。在各转运蛋白的协助下，运输进出细

一项最新研究发现：基因修饰的癌细胞可以澄清新癌症药物的作用机制。在人类细胞中，细胞核含有我们的DNA，并作为一个“控制中心”，而细胞质充当细胞的“体”。正是在这里，蛋白质得以生成和回收。

但是否蛋白质有活性或无活性依赖于它在细胞中的位置。细胞使用运输系统，以确保蛋白质达到需要它的部位。在健康的细胞中，蛋白质不断地在细胞核和细胞质之间被输送。

在各转运蛋白的协助下，运输进出细胞核。当中最知名的是Exportin-1，其运输超过200种不同的蛋白质。Exportin-1的“乘客”之一是肿瘤抑制蛋白。当在细胞核中，这些蛋白质能够检测受损的DNA，并触发细胞死亡。但某些癌细胞通过输送抗癌蛋白出细胞核并进入细胞质，扰乱Exportin-1的正常运转，在那里它们执行癌症抑制的工作被防止。

Rega Institute和Department of Chemistry研究人员先前报告了Exportin-1的抑制剂。 Karyopharm Therapeutics公司专注于发现和开发针对核运输靶标的新型药物，已确定并开发了Exportin-1抑制剂KPT-330用于治疗癌症。在这项新研究中，研究人员证实KPT-330能够靶向并阻断Exportin-1。分子KPT-330能连接到一个特定的氨基酸（Exportin-1蛋白质的结构单元）。

原始出处

Jasper E. Neggers, et al.Identifying Drug-Target Selectivity of Small-Molecule CRM1/XPO1 Inhibitors by CRISPR/Cas9 Genome Editing.Chemistry & Biology.2015

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2015-10-27 kzlchina

#chemistry#

39 0
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2015-08-24 changfy

#export#

38 0
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2016-02-14 sunylz

#Bio#

27 0
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2015-09-28 12498ebem31暂无昵称

#Biol#

30 0
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2015-03-08 sunylz

#抗癌药#

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