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Dysregulation of histone methyltransferases in breast cancer - Opportunities for new targeted therapies?
Molecular Oncology ( IF 6.6 ) Pub Date : 2016-09-23 , DOI: 10.1016/j.molonc.2016.09.003
Ewa M Michalak 1 , Jane E Visvader 1
Affiliation  

Histone methyltransferases (HMTs) catalyze the methylation of lysine and arginine residues on histone tails and non-histone targets. These important post-translational modifications are exquisitely regulated and affect chromatin compaction and transcriptional programs leading to diverse biological outcomes. There is accumulating evidence that genetic alterations of several HMTs impinge on oncogenic or tumor-suppressor functions and influence both cancer initiation and progression. HMTs therefore represent an opportunity for therapeutic targeting in those patients with tumors in which HMTs are dysregulated, to reverse the histone marks and transcriptional programs associated with aggressive tumor behavior. In this review, we describe the known histone methyltransferases and their emerging roles in breast cancer tumorigenesis.



中文翻译:

乳腺癌中组蛋白甲基转移酶的失调-新靶向疗法的机会吗?

组蛋白甲基转移酶(HMT)催化组蛋白尾巴和非组蛋白靶标上赖氨酸和精氨酸残基的甲基化。这些重要的翻译后修饰受到精确调节,并影响染色质紧实度和转录程序,从而导致多种生物学结果。越来越多的证据表明,几种HMT的遗传改变会影响致癌或抑癌功能,并影响癌症的发生和发展。因此,HMT为那些靶向治疗HMT失调的肿瘤患者提供了靶向治疗的机会,以逆转与侵袭性肿瘤行为相关的组蛋白标记和转录程序。在这篇综述中,我们描述了已知的组蛋白甲基转移酶及其在乳腺癌肿瘤发生中的新兴作用。

更新日期:2016-09-23
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