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酪蛋白激酶 2:抗癌药物设计的有吸引力的靶标。

Casein Kinase II: an attractive target for anti-cancer drug design.

机构信息

Experimental Therapeutics Centre, Agency for Science, Technology and Research (A*STAR), Singapore.

出版信息

Int J Biochem Cell Biol. 2010 Oct;42(10):1602-5. doi: 10.1016/j.biocel.2010.06.010. Epub 2010 Jun 15.

DOI:10.1016/j.biocel.2010.06.010
PMID:20558317
Abstract

Casein Kinase II (CK2) is a ubiquitous serine/threonine kinase that is highly conserved in eukaryotic cells. CK2 has been shown to impact cell growth and proliferation, as numerous growth-related proteins are substrates of CK2. More importantly, experimental evidence linking increased expression and activity of CK2 to human cancers underscores the relevance of CK2 biology to cellular transformation and carcinogenesis. Due to the critical regulatory role CK2 plays in cell fate determination in cancer cells, there is a tremendous interest in the development of CK2-specific therapies. Supporting this, recent reports have demonstrated that genetic manipulation of CK2 expression as well as pharmacological inhibition of its enzymatic activity sensitizes cancers to apoptotic stimuli. Here we provide a succinct account of the biology of CK2, its cellular substrates, its pro-survival and pro-proliferation activity, and highlight evidence for its involvement in human cancer.

摘要

酪蛋白激酶 2(CK2)是一种普遍存在的丝氨酸/苏氨酸激酶,在真核细胞中高度保守。CK2 已被证明会影响细胞生长和增殖,因为许多与生长相关的蛋白质是 CK2 的底物。更重要的是,将 CK2 的表达和活性增加与人类癌症联系起来的实验证据强调了 CK2 生物学与细胞转化和癌变的相关性。由于 CK2 在癌细胞中对细胞命运决定起着关键的调节作用,因此人们对开发 CK2 特异性疗法有着巨大的兴趣。支持这一点的是,最近的报告表明,对 CK2 表达的遗传操作以及对其酶活性的药理学抑制使癌症对凋亡刺激敏感。在这里,我们简要介绍了 CK2 的生物学、其细胞底物、其促生存和促增殖活性,并强调了其参与人类癌症的证据。

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Casein Kinase II: an attractive target for anti-cancer drug design.酪蛋白激酶 2:抗癌药物设计的有吸引力的靶标。
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