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磷酸酶:它们在癌症中的作用及其化学调节剂。

Phosphatases: Their Roles in Cancer and Their Chemical Modulators.

作者信息

Fontanillo Miriam, Köhn Maja

机构信息

Genome Biology Unit, European Molecular Biology Laboratory, Meyerhofstrasse 1, 69117, Heidelberg, Germany.

出版信息

Adv Exp Med Biol. 2016;917:209-40. doi: 10.1007/978-3-319-32805-8_10.

Abstract

Phosphatases are involved in basically all cellular processes by dephosphorylating cellular components such as proteins, phospholipids and second messengers. They counteract kinases of which many are established oncogenes, and therefore kinases are one of the most important drug targets for targeted cancer therapy. Due to this relationship between kinases and phosphatases, phosphatases are traditionally assumed to be tumour suppressors. However, research findings over the last years prove that this simplification is incorrect, as bona-fide and putative phosphatase oncogenes have been identified. We describe here the role of phosphatases in cancer, tumour suppressors and oncogenes, and their chemical modulators, and discuss new approaches and opportunities for phosphatases as drug targets.

摘要

磷酸酶通过使蛋白质、磷脂和第二信使等细胞成分去磷酸化,参与基本上所有的细胞过程。它们与许多已被确认为癌基因的激酶起拮抗作用,因此激酶是靶向癌症治疗最重要的药物靶点之一。由于激酶和磷酸酶之间的这种关系,传统上认为磷酸酶是肿瘤抑制因子。然而,过去几年的研究结果证明这种简化观点是不正确的,因为已经鉴定出了真正的和推定的磷酸酶癌基因。我们在此描述磷酸酶在癌症、肿瘤抑制因子和癌基因中的作用,以及它们的化学调节剂,并讨论将磷酸酶作为药物靶点的新方法和机会。

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