Korea Research Institute of Chemical Technology, Daejeon, Republic of Korea.
Seoul National University, Seoul, Republic of Korea.
Adv Exp Med Biol. 2021;1187:103-119. doi: 10.1007/978-981-32-9620-6_5.
Aberrant epigenetic alteration has been associated with development of various cancers, including breast cancer. Since epigenetic modifications such as DNA methylation and histone modification are reversible, epigenetic enzymes, including histone modifying enzymes and DNA methyltransferases, emerge as attractive targets for cancer therapy. Although epi-drugs targeting histone deacetylation or DNA methylation have received FDA approval for cancer therapy, a very modest anti-tumor activity has been observed with monotherapy in clinical studies of breast cancer. To improve efficacy of epi-drugs in breast cancer, combination of epi-drugs with other therapies currently has been investigated. Additionally, basic researches to elucidate molecular causes of cancer should be extensively and intensively conducted in order to find novel epigenetic druggable targets. In this chapter, we summarize how epigenetic regulation affects the development of breast cancer and how to control cancer phenotype by modulating abnormal epigenetic modifications, and then suggest future research directions in epigenetics for breast cancer treatment.
异常的表观遗传改变与各种癌症的发展有关，包括乳腺癌。由于表观遗传修饰（如 DNA 甲基化和组蛋白修饰）是可逆的，因此表观遗传酶（包括组蛋白修饰酶和 DNA 甲基转移酶）成为癌症治疗的有吸引力的靶点。尽管针对组蛋白去乙酰化或 DNA 甲基化的 epi 药物已获得 FDA 批准用于癌症治疗，但在乳腺癌的临床研究中，单药治疗观察到的抗肿瘤活性非常有限。为了提高 epi 药物在乳腺癌中的疗效，目前已经研究了将 epi 药物与其他疗法联合使用。此外，为了寻找新的表观遗传药物靶点，应该广泛而深入地开展阐明癌症分子原因的基础研究。在本章中，我们总结了表观遗传调控如何影响乳腺癌的发展，以及如何通过调节异常的表观遗传修饰来控制癌症表型，然后为乳腺癌治疗的表观遗传学提出了未来的研究方向。
