Centre for Nano and Material Sciences, Jain University, Jain Global Campus, Bengaluru, Karnataka, India.
Subcell Biochem. 2022;100:503-521. doi: 10.1007/978-3-031-07634-3_15.
Origin of cancer is strongly related to the unusual epigenetic regulation of gene function as indicated by recent reports. The covalent modifications to DNA or histones without affecting genomes that finally lead to phenotypical changes in cells or organisms are referred as "Epigenetics." The possibility to reprogram the epigenetics in the cancer epigenome is the most important target for cancer treatment and drug resistance. The development of epigenetic drugs holds a great potential for the current cancer therapeutic approaches. Nevertheless, targeting cancer epigenetic pathways is still exciting due to the lack of selective and effective small molecule compounds or drug molecules. Therefore, the current book chapter highlights epigenetic pathways for cancer and potential small molecule inhibitors and epidrugs targeting DNA methyltransferase, histone modification, and more new therapies with nanomaterials and imaging to improve the effectiveness of cancer treatment. The structural aspects on discovery of novel small molecules or drugs targeting epigenetic pathways in cancer exploration as promising strategies will be also discussed.
癌症的起源与基因功能的异常表观遗传调控密切相关，这一点已被最近的研究报告所证实。在不影响基因组的情况下，对 DNA 或组蛋白进行共价修饰，最终导致细胞或生物体表型的变化，这种现象被称为“表观遗传学”。在癌症表观基因组中重新编程表观遗传的可能性是癌症治疗和耐药性的最重要目标。表观遗传药物的发展为当前的癌症治疗方法提供了巨大的潜力。然而，由于缺乏选择性和有效的小分子化合物或药物分子，靶向癌症表观遗传途径仍然令人兴奋。因此，本章重点介绍了癌症的表观遗传途径，以及针对 DNA 甲基转移酶、组蛋白修饰等的潜在小分子抑制剂和表药物，以及利用纳米材料和成像技术来提高癌症治疗效果的新疗法。还将讨论针对癌症探索中表观遗传途径的新型小分子或药物发现的结构方面，这些都是有前途的策略。
