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Targeting epigenetic regulators for cancer therapy: mechanisms and advances in clinical trials.
Signal Transduction and Targeted Therapy ( IF 40.8 ) Pub Date : 2019-12-17 , DOI: 10.1038/s41392-019-0095-0 Yuan Cheng 1 , Cai He 1 , Manni Wang 1 , Xuelei Ma 1 , Fei Mo 1 , Shengyong Yang 1 , Junhong Han 1 , Xiawei Wei 1
Signal Transduction and Targeted Therapy ( IF 40.8 ) Pub Date : 2019-12-17 , DOI: 10.1038/s41392-019-0095-0 Yuan Cheng 1 , Cai He 1 , Manni Wang 1 , Xuelei Ma 1 , Fei Mo 1 , Shengyong Yang 1 , Junhong Han 1 , Xiawei Wei 1
Affiliation
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Epigenetic alternations concern heritable yet reversible changes in histone or DNA modifications that regulate gene activity beyond the underlying sequence. Epigenetic dysregulation is often linked to human disease, notably cancer. With the development of various drugs targeting epigenetic regulators, epigenetic-targeted therapy has been applied in the treatment of hematological malignancies and has exhibited viable therapeutic potential for solid tumors in preclinical and clinical trials. In this review, we summarize the aberrant functions of enzymes in DNA methylation, histone acetylation and histone methylation during tumor progression and highlight the development of inhibitors of or drugs targeted at epigenetic enzymes.
中文翻译：
针对癌症治疗的表观遗传调节因子：临床试验的机制和进展。
表观遗传改变涉及组蛋白或 DNA 修饰的可遗传但可逆的变化，这些变化调节基本序列之外的基因活性。表观遗传失调通常与人类疾病，特别是癌症有关。随着各种针对表观遗传调节因子的药物的开发，表观遗传靶向治疗已应用于血液系统恶性肿瘤的治疗，并在临床前和临床试验中显示出对实体瘤的可行治疗潜力。在这篇综述中，我们总结了肿瘤进展过程中DNA甲基化、组蛋白乙酰化和组蛋白甲基化酶的异常功能，并重点介绍了针对表观遗传酶的抑制剂或药物的开发。
更新日期：2019-12-17
中文翻译：
针对癌症治疗的表观遗传调节因子：临床试验的机制和进展。
表观遗传改变涉及组蛋白或 DNA 修饰的可遗传但可逆的变化，这些变化调节基本序列之外的基因活性。表观遗传失调通常与人类疾病，特别是癌症有关。随着各种针对表观遗传调节因子的药物的开发，表观遗传靶向治疗已应用于血液系统恶性肿瘤的治疗，并在临床前和临床试验中显示出对实体瘤的可行治疗潜力。在这篇综述中，我们总结了肿瘤进展过程中DNA甲基化、组蛋白乙酰化和组蛋白甲基化酶的异常功能，并重点介绍了针对表观遗传酶的抑制剂或药物的开发。
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