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Nature Chem Bio:针对BCL-XL的高效小分子抑制剂WEHI-539被发现

2013-05-06 MedSci MedSci原创

Bcl-xL抑制剂WEHI-539
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日前，澳大利亚和美国Genentech公司的科学家合作，成功开发出了一种针对促存活蛋白BCL-XL的高效选择性小分子抑制剂。这项发现使开发针对BCL-XL的特定抗癌药物成为可能。BCL- XL属于一类有利于癌细胞存活的家族蛋白中的一种，其在肿瘤中通常过度表达。因为该蛋白家族很难作为小分子的标靶，所以只有一小部分药物能在临床发展应用 中有所表现。迄今为止，这些药物中没有一种能对特定的蛋白家族成员

研究人员开发出针对BCL-XL的高效小分子抑制剂

日前，澳大利亚和美国Genentech公司的科学家合作，成功开发出了一种针对促存活蛋白BCL-XL的高效选择性小分子抑制剂。这项发现使开发针对BCL-XL的特定抗癌药物成为可能。

BCL- XL属于一类有利于癌细胞存活的家族蛋白中的一种，其在肿瘤中通常过度表达。因为该蛋白家族很难作为小分子的标靶，所以只有一小部分药物能在临床发展应用 中有所表现。迄今为止，这些药物中没有一种能对特定的蛋白家族成员产生选择性，而这个蛋白家族有可能引发一些我们不愿意看到的毒性。

研究人 员设计了一种针对BCL-XL的高效选择性抑制剂。他们确认这种名为WEHI-539的化合物在细胞中具有高效率和选择性的特点，并且能作用于标靶，促进细胞凋亡。科学家可将WEHI-539作为一种重要的工具以更好地了解BCL-XL与癌细胞之间的关系，并为开发针对BCL-XL的特定抗癌药物开启了一 扇大门。

原始出处：

Guillaume Lessene, Peter E Czabotar, Keith G Watson et al. Structure-guided design of a selective BCL-XLinhibitor. Nature Chemical Biology, 21 April 2013; doi:10.1038/nchembio.1246

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    2013-12-02 liye789132251

    #Nat#

    0

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    2013-09-11 lqrandywkz

    #小分子抑制剂#

    0

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    2014-01-28 宋威

    #小分子#

    0

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    2014-02-07 jklm09

    #抑制剂#

    0

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    2013-10-20 sunylz

    #Bio#

    0

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    2013-05-08 yykkxiaodou

    #Bcl-xL#

    0

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