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Nat Chem Biol：一种抑制VCP酶的化合物或可用于癌症治疗

2013-08-19 佚名 bio360

癌症VCP酶
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日前，意大利科学家发现，一种抑制VCP酶的化合物可为治疗癌症提供新工具。相关研究论文刊登在了《自然-化学生物学》（Nature Chemical Biology）杂志上。【原文下载】 VCP又名p97或Cdc48，是一种ATP酶（利用ATP裂解产生的能量完成其他反应的酶），在蛋白质的可控降解中起着重要作用。 科学家逐渐发现VCP也与癌症有一定联系：其功能对保持癌细胞健康是必需的。因而，

一种抑制VCP酶的化合物或能用于癌症治疗

日前，意大利科学家发现，一种抑制VCP酶的化合物可为治疗癌症提供新工具。相关研究论文刊登在了《自然-化学生物学》（Nature Chemical Biology）杂志上。【原文下载】

VCP又名p97或Cdc48，是一种ATP酶（利用ATP裂解产生的能量完成其他反应的酶），在蛋白质的可控降解中起着重要作用。

科学家逐渐发现VCP也与癌症有一定联系：其功能对保持癌细胞健康是必需的。因而，抑制VCP功能可防止正常蛋白的降解并导致意外序列的产生，最终促使癌细胞死亡。

在这项研究中，研究人员发现一类合成化合物能通过三种不同的机制抑制 VCP。其中一组化合物跟ATP一样会与相同的位点结合，这组化合物与已知的 VCP抑制剂类似，但对VCP不具有选择性。

另外两组化合物则在新的方式下产生作用：一组会与ATP位点内的蛋白质形成共价键，而另一组则会与远离ATP位点的一个意外的变构位点相结合，可能是为了通过阻止催化所需的构型变化这种方式来关闭VCP的功能。

研究小组表示，这两组名为NMS-859和NMS-873的化合物可以导致癌细胞系中的细胞死亡。

原始出处：
 
Paola Magnaghi, Roberto D'Alessio, Barbara Valsasina, Nilla Avanzi, Simona Rizzi, Daniela Asa, Fabio Gasparri, Liviana Cozzi, Ulisse Cucchi, Christian Orrenius, Paolo Polucci, Dario Ballinari, Claudia Perrera, Antonella Leone, Giovanni Cervi, Elena Casale, Yang Xiao, Chihunt Wong, Daniel J Anderson, Arturo Galvani, Daniele Donati, Tom O'Brien, Peter K Jackson& Antonella Isacchi. Covalent and allosteric inhibitors of the ATPase VCP /p97 induce cancer cell death. Nature Chemical Biology, 28 July 2013; doi:10.1038/nchembio.1313. 【原文下载】

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    2013-09-24 sunylz

    #Bio#

    0

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    2014-07-11 陈吴1234

    #癌症治疗#

    0

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    2014-06-29 12498ebem31暂无昵称

    #Biol#

    0

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    2013-09-03 wangyang7958

    #化合物#

    0

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    2014-07-24 liye789132251

    #Nat#

    0

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澳大利亚科研人员在新一期《癌症研究》杂志上报告说，他们研制出一种能有效杀死癌细胞并且副作用很小的新药，这为治疗癌症带来了新希望。【原文下载】 澳大利亚新南威尔士大学等机构研究人员报告说，这种新药代号为TR100，动物实验显示它可以摧毁两种类型的癌细胞——儿童神经母细胞瘤和黑素瘤。这种新药能迅速锁定癌细胞，并将其内部结构摧毁，同时不会产生较大的毒性副作用。 研究人员正计划用这种新药进行人体临床试

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