Targeting Transcription Factors in Cancer.
Targeting Transcription Factors in Cancer.
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DOI：
10.1016/j.trecan.2015.07.001
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发表时间：
2015-09-01
期刊：
影响因子：
18.4
通讯作者：
Vakoc CR
中科院分区：
文献类型：
--
作者：
Bhagwat AS;Vakoc CR
转录因子(转录因子)在人类癌症的发病机制中通常处于失控状态，是一类主要的癌细胞依赖因子。因此，靶向转铁蛋白可以非常有效地治疗特定的恶性肿瘤，如以核激素受体为靶点的药物的临床疗效所强调的那样。在这篇综述中，我们讨论了在肿瘤中作为药物靶点的转录因子的最新进展，重点讨论了新出现的调节转化因子功能的化学方法。作为细胞转化驱动力的转铁蛋白具有显著的多样性和效力，因此有理由继续追求转铁蛋白作为药物发现的治疗靶点。
Transcription factors (TFs) are commonly deregulated in the pathogenesis of human cancer and are a major class of cancer cell dependencies. Consequently, targeting of TFs can be highly effective in treating particular malignancies, as highlighted by the clinical efficacy of agents that target nuclear hormone receptors. In this review we discuss recent advances in our understanding of TFs as drug targets in oncology, with an emphasis on the emerging chemical approaches to modulate TF function. The remarkable diversity and potency of TFs as drivers of cell transformation justifies a continued pursuit of TFs as therapeutic targets for drug discovery.