Department of Anatomical Pathology, Singapore General Hospital, 20 College Road, Academia, Level 10, Diagnostics Tower, Singapore 169856, Singapore.
School of Biological Sciences, Nanyang Technological University, 60 Nanyang Drive, Singapore 637551, Singapore.
Curr Oncol. 2023 Feb 9;30(2):2127-2143. doi: 10.3390/curroncol30020164.
Tumor evolution to evade immune surveillance is a hallmark of carcinogenesis, and the modulation of tumor immunogenicity has been a challenge to present therapeutic responses in immunotherapies alone for numerous cancers. By altering the cell phenotype and reshaping the tumor microenvironment, epigenetic modifications enable tumor cells to overcome immune surveillance as a mechanism of cancer progression and immunotherapy resistance. Demethylase enzymatic activity of lysine-specific demethylase 1 (LSD1), a histone demethylase first identified in 2004, plays a pivotal role in the vast cellular processes of cancer. While FDA-approved indications for epigenetic therapies are limited to hematological malignancies, it is imperative to understand how epigenetic machinery can be targeted to prime immunotherapy responses in breast cancers. In this review, we discuss the potential roles of epigenetics and demethylating agent LSD1 as a potent new cancer management strategy to combat the current challenges of breast cancers, which have presented modest efficacy to immune checkpoint inhibitors till date. Additionally, we describe the combined use of LSD1-specific inhibitors and immune checkpoint inhibitors in existing breast cancer preclinical and clinical trials that elicits a robust immune response and benefit. Overall, the promising results observed in LSD1-targeting therapies signify the central role of epigenetics as a potential novel strategy to overcome resistance commonly seen in immunotherapies.
肿瘤通过逃避免疫监视进行进化是癌症发生的一个标志,而调节肿瘤免疫原性一直是一个挑战,仅靠免疫疗法很难对众多癌症产生治疗反应。通过改变细胞表型和重塑肿瘤微环境,表观遗传修饰使肿瘤细胞能够克服免疫监视,成为癌症进展和免疫治疗耐药的一种机制。赖氨酸特异性脱甲基酶 1(LSD1)的去甲基酶酶活性,作为 2004 年首次发现的组蛋白去甲基酶,在癌症的广泛细胞过程中发挥着关键作用。虽然 FDA 批准的表观遗传疗法的适应证仅限于血液恶性肿瘤,但了解如何靶向表观遗传机制以增强乳腺癌的免疫治疗反应是至关重要的。在这篇综述中,我们讨论了表观遗传学和去甲基化酶 LSD1 的潜在作用,作为一种对抗当前乳腺癌挑战的新的癌症管理策略,到目前为止,这些挑战对免疫检查点抑制剂的疗效有限。此外,我们还描述了 LSD1 特异性抑制剂与免疫检查点抑制剂在现有乳腺癌临床前和临床试验中的联合应用,这引发了强烈的免疫反应和获益。总的来说,在 LSD1 靶向治疗中观察到的有希望的结果表明,表观遗传学作为一种克服免疫治疗中常见耐药性的潜在新策略具有核心作用。