PDF(Pubmed)
Abstract：
Epigenetic mechanisms control and regulate normal chromatin structure and gene expression patterns, with epigenetic dysregulation observed in many different cancer types. Importantly, epigenetic modifications are reversible, offering the potential to silence oncogenes and reactivate tumor suppressors. Small molecule drugs manipulating these epigenetic mechanisms are at the leading edge of new therapeutic options for cancer treatment. The clinical use of histone deacetyltransferases inhibitors (HDACi) demonstrates the effectiveness of targeting epigenetic mechanisms for cancer treatment. Notably, the development of new classes of inhibitors, including lysine acetyltransferase inhibitors (KATi), are the future of epigenetic-based therapeutics. We outline the progress of current classes of small molecule epigenetic drugs for use against cancer (preclinical and clinical) and highlight the potential market growth in epigenetic-based therapeutics.
摘要：
表观遗传机制控制和调节正常染色质结构和基因表达模式，在许多不同的癌症类型中观察到表观遗传失调。重要的是,表观遗传修饰是可逆的，提供沉默癌基因和重新激活肿瘤抑制基因的潜力。操纵这些表观遗传机制的小分子药物处于癌症治疗新治疗选择的前沿。组蛋白去乙酰转移酶抑制剂（HDACi）的临床应用证明了靶向表观遗传机制治疗癌症的有效性。值得注意的是,新型抑制剂的开发，包括赖氨酸乙酰转移酶抑制剂（KATI），是表观遗传疗法的未来。我们概述了目前用于抗癌的小分子表观遗传药物（临床前和临床）的进展，并强调了基于表观遗传的疗法的潜在市场增长。
