临床试验的当前趋势以及作为癌症治疗药物的小分子表观遗传抑制剂的开发。
Current trends in clinical trials and the development of small molecule epigenetic inhibitors as cancer therapeutics.
作者信息
Zohourian Nazanin, Brown James Al
机构信息
Department of Biological Science, University of Limerick, Limerick, V94 T9PX, Ireland.
Limerick Digital Cancer Research Centre (LDCRC), University of Limerick, Limerick, Ireland.
出版信息
Epigenomics. 2024 Apr 19;16(9):671-80. doi: 10.2217/epi-2023-0443.
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.
表观遗传机制控制和调节正常的染色质结构及基因表达模式，在许多不同类型的癌症中都观察到了表观遗传失调。重要的是，表观遗传修饰是可逆的，这为沉默癌基因和重新激活肿瘤抑制因子提供了可能。操纵这些表观遗传机制的小分子药物处于癌症治疗新疗法的前沿。组蛋白去乙酰化酶抑制剂（HDACi）的临床应用证明了靶向表观遗传机制进行癌症治疗的有效性。值得注意的是，包括赖氨酸乙酰转移酶抑制剂（KATi）在内的新型抑制剂的开发是基于表观遗传学治疗的未来方向。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学治疗的潜在市场增长。
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