Sci Transl Med：CK1δ有望成为乳腺癌治疗的新靶点

2015-12-21 MedSci MedSci原创

酪蛋白激酶1δ(CaseinKinase 1δ，CK1δ)是酪蛋白激酶 I (Casein Kinase 1，CK1)的一个亚型，CK1是一类具有独特理化特性的丝氨酸/苏氨酸蛋白激酶，广泛存在于真核生物中，主要分布在细胞质、细胞核、细胞膜及细胞骨架等部位，参与多种细胞功能及发育过程的调节，具有重要功能。Wnt通路对于动物发育是必需的，参与干细胞分化及肿瘤的形成过程，而在Wnt通路中，CK1δ作为β

酪蛋白激酶1δ(CaseinKinase 1δ，CK1δ)是酪蛋白激酶 I (Casein Kinase 1，CK1)的一个亚型，CK1是一类具有独特理化特性的丝氨酸/苏氨酸蛋白激酶，广泛存在于真核生物中，主要分布在细胞质、细胞核、细胞膜及细胞骨架等部位，参与多种细胞功能及发育过程的调节，具有重要功能。Wnt通路对于动物发育是必需的，参与干细胞分化及肿瘤的形成过程，而在Wnt通路中，CK1δ作为β-连环蛋白降解复合物上游的激酶可直接或间接参与对 Dvl-1、APC、Axin和β-连环蛋白磷酸化，并通过β-连环蛋白对Wnt通路中的靶基因发挥重要调节作用。

研究表明在乳腺癌和急性单核细胞白血病中有CK1δ的表达异常，而最新一期的《Science Translational Medicine》上发表的一篇研究则指出CK1δ可作为全新的乳腺癌治疗靶点。研究指出，异常的CK1δ调节通过激活β-连环蛋白促进乳腺癌患者中的肿瘤生长，而使用特异性CK1δ抑制剂SR-3029可从肿瘤细胞中去除β-连环蛋白从而杀死肿瘤组织，治疗CK1δ表达的乳腺癌。
研究者使用一种被称为SR-3029的实验室化合物作为特异性CK1δ抑制剂，研究结果显示SR-3029能够显著阻断动物模型和乳腺癌患者肿瘤组织中的肿瘤生长。

参考文献：

Rosenberg LH, Lafitte M, Quereda V, Grant W, Chen W, Bibian M, Noguchi Y, Fallahi M, Yang C, Chang JC, Roush WR, Cleveland JL, Duckett DR.Therapeutic targeting of casein kinase 1δ in breast cancer. Sci Transl Med. 2015 Dec 16;7(318):318ra202

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#插入话题

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2016-09-26 bsmagic9140

#TRA#

29 0
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2016-05-21 ms3025846204744509

#Transl#

20 0
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2015-12-27 wzf990214

有意思

78 0
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2015-12-27 wzf990214

赞一个

76 0
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2015-12-23 lsndxfj

#新靶点#

16 0
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2015-12-23 ms3994565386320060

#Med#

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