表观遗传学药物：癌症治疗中的靶向表观遗传标记。
Epidrugs: targeting epigenetic marks in cancer treatment.
机构信息
Department of Surgery, Drug Research and Development Center, Federal University of Ceara , Fortaleza , Brazil.
Department of Physiology and Pharmacology, Drug Research and Development Center, Federal University of Ceara , Fortaleza , Brazil.
出版信息
Epigenetics. 2019 Dec;14(12):1164-1176. doi: 10.1080/15592294.2019.1640546. Epub 2019 Jul 13.
Abstract
Growing evidence suggests that aberrant epigenetic regulation of gene function is strongly related to the genesis of cancer. Unlike genetic mutations, the ability to reprogram the epigenetic landscape in the cancer epigenome is one of the most promising target therapies in both treatment and reversibility of drug resistance. Epigenetic alterations in cancer development and progression may be the basis for the individual variation in drug response. Thus, this review focuses on the emerging area of pharmaco(epi)genomics, specifically highlighting epigenetic reprogramming during tumorigenesis and how epigenetic markers are targeted as a therapy (epidrugs) and the clinical implications of this for cancer treatment.
摘要
越来越多的证据表明，基因功能的表观遗传调控失常与癌症的发生密切相关。与基因突变不同，在癌症表观基因组中重新编程表观遗传景观的能力是治疗和逆转耐药性最有前途的靶向治疗之一。癌症发生和发展中的表观遗传改变可能是药物反应个体差异的基础。因此，本综述侧重于药物基因组学（epi）的新兴领域，特别是强调肿瘤发生过程中的表观遗传重编程，以及如何将表观遗传标记作为一种治疗方法（epidrugs）进行靶向治疗，以及这对癌症治疗的临床意义。
相似文献
1
Epidrugs: targeting epigenetic marks in cancer treatment.表观遗传学药物：癌症治疗中的靶向表观遗传标记。
Epigenetics. 2019 Dec;14(12):1164-1176. doi: 10.1080/15592294.2019.1640546. Epub 2019 Jul 13.
2
Cancer epigenetics: Moving forward.癌症表观遗传学：展望未来。
PLoS Genet. 2018 Jun 7;14(6):e1007362. doi: 10.1371/journal.pgen.1007362. eCollection 2018 Jun.
3
Towards a more precise therapy in cancer: Exploring epigenetic complexity.朝着癌症更精准的治疗迈进：探索表观遗传学的复杂性。
Curr Opin Chem Biol. 2020 Aug;57:41-49. doi: 10.1016/j.cbpa.2020.04.008. Epub 2020 May 29.
4
Targeting the epigenetic regulation of antitumour immunity.靶向抗肿瘤免疫的表观遗传调控。
Nat Rev Drug Discov. 2020 Nov;19(11):776-800. doi: 10.1038/s41573-020-0077-5. Epub 2020 Sep 14.
5
Targeting Epigenetics in Cancer.靶向治疗癌症的表观遗传学。
Annu Rev Pharmacol Toxicol. 2018 Jan 6;58:187-207. doi: 10.1146/annurev-pharmtox-010716-105106. Epub 2017 Oct 6.
6
Pharmacological targeting of the cancer epigenome.癌症表观基因组的药物靶向治疗。
Nat Cancer. 2024 Jun;5(6):844-865. doi: 10.1038/s43018-024-00777-2. Epub 2024 Jun 27.
7
Epigenetic protein complexes: the adequate candidates for the use of a new generation of epidrugs in personalized and precision medicine in cancer.表观遗传蛋白复合物：新一代表观遗传药物在癌症个性化和精准医学中应用的合适候选物。
Epigenomics. 2020 Jan;12(2):171-177. doi: 10.2217/epi-2019-0169. Epub 2019 Dec 18.
8
Pharmacoepigenetics: an element of personalized therapy?药物表观遗传学：个性化治疗的一个要素？
Expert Opin Drug Metab Toxicol. 2017 Apr;13(4):387-398. doi: 10.1080/17425255.2017.1260546. Epub 2016 Nov 28.
9
New Promises to Cure Cancer and Other Genetic Diseases/Disorders: Epi-drugs Through Epigenetics.新型癌症和其他遗传疾病/障碍治疗方法：通过表观遗传学的 epi-drugs。
Curr Top Med Chem. 2019;19(12):972-994. doi: 10.2174/1568026619666190603094439.
10
Paediatric Strategy Forum for medicinal product development of epigenetic modifiers for children: ACCELERATE in collaboration with the European Medicines Agency with participation of the Food and Drug Administration.儿童表观遗传修饰剂药品开发儿科战略论坛：加速计划，与欧洲药品管理局合作，美国食品药品监督管理局参与
Eur J Cancer. 2020 Nov;139:135-148. doi: 10.1016/j.ejca.2020.08.014. Epub 2020 Sep 26.
引用本文的文献
1
Research progress on the diagnostic value of fecal calprotectin in colorectal tumors.粪便钙卫蛋白在结直肠肿瘤诊断价值中的研究进展
Front Med (Lausanne). 2025 Jul 9;12:1626197. doi: 10.3389/fmed.2025.1626197. eCollection 2025.
2
Novel quinazoline-triazole-based -hydroxybenzamides/-hydroxypropenamides as HDAC inhibitors: design, synthesis, biological evaluation, and docking studies.基于喹唑啉-三唑的新型羟基苯甲酰胺/羟基丙烯酰胺作为组蛋白去乙酰化酶（HDAC）抑制剂：设计、合成、生物学评价及对接研究
RSC Adv. 2025 Jul 22;15(32):26201-26215. doi: 10.1039/d5ra04193g. eCollection 2025 Jul 21.
3
Cancer-Associated Genetic Aberrations and Precision Medicine.癌症相关的基因畸变与精准医学
Int J Med Sci. 2025 Jun 12;22(12):2932-2943. doi: 10.7150/ijms.109506. eCollection 2025.
4
CEBPD regulates CD47 and MAP4K4 via chromatin accessibility in canine mammary tumor monocytes.CEBPD通过染色质可及性调节犬乳腺肿瘤单核细胞中的CD47和MAP4K4。
Sci Rep. 2025 Jul 2;15(1):23404. doi: 10.1038/s41598-025-06296-z.
5
Tranylcypromine-Based LSD1 Inhibitors as Useful Agents to Reduce Viability of .基于反苯环丙胺的赖氨酸特异性去甲基化酶1（LSD1）抑制剂作为降低……活力的有效药物
ACS Infect Dis. 2025 Aug 8;11(8):2178-2189. doi: 10.1021/acsinfecdis.5c00224. Epub 2025 Jul 2.
6
Structural characteristics and SARs of EZH2 inhibitors.EZH2抑制剂的结构特征与构效关系
Mol Divers. 2025 Jul 1. doi: 10.1007/s11030-025-11272-w.
7
Systematic analysis of the aberrances and functional implications of epigenetic genes in hepatocellular carcinoma.肝细胞癌中表观遗传基因异常及其功能影响的系统分析
Discov Oncol. 2025 May 27;16(1):936. doi: 10.1007/s12672-025-02765-z.
8
Intimate partner violence and stress-related disorders: from epigenomics to resilience.亲密伴侣暴力与应激相关障碍：从表观基因组学到复原力
Front Glob Womens Health. 2025 May 12;6:1536169. doi: 10.3389/fgwh.2025.1536169. eCollection 2025.
9
Drug Discovery for Histone Deacetylase Inhibition: Past, Present and Future of Zinc-Binding Groups.组蛋白去乙酰化酶抑制作用的药物发现：锌结合基团的过去、现在与未来
Pharmaceuticals (Basel). 2025 Apr 16;18(4):577. doi: 10.3390/ph18040577.
10
Epigenetic implications in the pathogenesis of corticotroph tumors.表观遗传学在促肾上腺皮质激素细胞肿瘤发病机制中的意义
Pituitary. 2025 Apr 21;28(3):51. doi: 10.1007/s11102-025-01522-3.
本文引用的文献
1
Targeting epigenetics for cancer therapy.针对癌症治疗的表观遗传学靶点。
Arch Pharm Res. 2019 Feb;42(2):159-170. doi: 10.1007/s12272-019-01126-z. Epub 2019 Feb 26.
2
Strategies for first-line immunotherapy in squamous cell lung cancer: are combinations a game changer?鳞状细胞肺癌一线免疫治疗策略：联合治疗会改变局面吗？
Transl Lung Cancer Res. 2018 Sep;7(Suppl 3):S198-S201. doi: 10.21037/tlcr.2018.07.02.
3
N-methyladenine DNA Modification in Glioblastoma.神经胶质母细胞瘤中的 N-甲基腺嘌呤 DNA 修饰。
Cell. 2018 Nov 15;175(5):1228-1243.e20. doi: 10.1016/j.cell.2018.10.006. Epub 2018 Nov 1.
4
Monoclonal antibodies in cancer immunotherapy.癌症免疫疗法中的单克隆抗体。
Mol Biol Rep. 2018 Dec;45(6):2935-2940. doi: 10.1007/s11033-018-4427-x. Epub 2018 Oct 11.
5
Epigenetics and Epi-miRNAs: Potential markers/therapeutics in leukemia.表观遗传学和 epi-miRNAs：白血病的潜在标志物/治疗靶点。
Biomed Pharmacother. 2018 Oct;106:1668-1677. doi: 10.1016/j.biopha.2018.07.133. Epub 2018 Jul 29.
6
Downregulated microRNAs in the colorectal cancer: diagnostic and therapeutic perspectives.结直肠癌中下调的 microRNAs：诊断和治疗视角。
BMB Rep. 2018 Nov;51(11):563-571. doi: 10.5483/BMBRep.2018.51.11.116.
7
Unveiling epigenetic regulation in cancer, aging, and rejuvenation with in vivo reprogramming technology.利用体内重编程技术揭示癌症、衰老和 rejuvenation 中的表观遗传调控。
Cancer Sci. 2018 Sep;109(9):2641-2650. doi: 10.1111/cas.13731. Epub 2018 Aug 15.
8
The causal relationship between epigenetic abnormality and cancer development: in vivo reprogramming and its future application.表观遗传异常与癌症发展之间的因果关系：体内重编程及其未来的应用。
Proc Jpn Acad Ser B Phys Biol Sci. 2018;94(6):235-247. doi: 10.2183/pjab.94.016.
9
Pharmacological Targeting of Cell Cycle, Apoptotic and Cell Adhesion Signaling Pathways Implicated in Chemoresistance of Cancer Cells.药物靶向作用于细胞周期、凋亡和细胞黏附信号通路可逆转肿瘤细胞的耐药性。
Int J Mol Sci. 2018 Jun 6;19(6):1690. doi: 10.3390/ijms19061690.
10
Association between H3K4 methylation and cancer prognosis: A meta-analysis.H3K4 甲基化与癌症预后的关联：一项荟萃分析。
Thorac Cancer. 2018 Jul;9(7):794-799. doi: 10.1111/1759-7714.12647. Epub 2018 May 8.
Zotero 插件