靶向肿瘤表观遗传调节剂 SETDB1 治疗肿瘤

IF 2.3 4区医学 Q3 ONCOLOGY

Current cancer drug targets Pub Date : 2024-08-28 DOI:10.2174/0115680096311909240721160523

Cheng Peng, Nini Zhou, Tengjiang Chen, Jie Lei, Changwen Chen, Shunqin Zhu

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引用次数: 0

摘要

:表观遗传学改变与肿瘤发生的早期阶段有关，被广泛认为是癌症发展过程中无处不在的现象。异常的表观遗传修饰可改变靶基因的表达，诱导异染色质的形成，并使正常细胞逐渐走向永生化肿瘤细胞，从而产生重大影响。SETDB1（SET domain bifurcated histone lysine methyltransferase 1）是一种典型的组蛋白甲-乙基转移酶，通过修饰组蛋白3赖氨酸9的甲基化，促进异染色质的形成并抑制基因的转录。SETDB1通常在肿瘤中高度外显，拷贝数高，预后差，患者生存率低，是表观遗传修饰异常的典型病例。我们讨论了 SETDB1 在多种癌症中的作用机制，并回顾了近年来报道的表观遗传抑制剂及其抗肿瘤效果。此外，我们还总结了 SETDB1 在多种疾病和细胞功能中的作用。

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Targeting the Tumor Epigenetic Regulator SETDB1 for Tumor Therapy

: Epigenetic alterations are implicated in the early stages of tumorigenesis and are widely recognized as a ubiquitous phenomenon in cancer development. Aberrant epigenetic modifications can alter the expression of target genes, induce heterochromatin formation, and gradually drive normal cells towards immortalized tumor cells with significant consequences. SETDB1 (SET domain bifurcated histone lysine methyltransferase 1), a typical histone me-thyltransferase, promotes the formation of heterochromatin and inhibits the transcription of genes by modifying the methylation of lysine 9 of histone 3. SETDB1 is usually highly ex-pressed in tumors with high copy numbers, accompanied by poor prognosis and low patient survival rates, which is a typical case of abnormal epigenetic modification. We discuss the mechanism of SETDB1 in a variety of cancers and review the epigenetic inhibitors that have been reported in recent years, along with their anti-tumor effects. In addition, we summarize the role of SETDB1 in a variety of diseases and cell functions.

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来源期刊

Current cancer drug targets 医学-肿瘤学

CiteScore

5.40

自引率

0.00%

发文量

105

审稿时长

1 months

期刊介绍： Current Cancer Drug Targets aims to cover all the latest and outstanding developments on the medicinal chemistry, pharmacology, molecular biology, genomics and biochemistry of contemporary molecular drug targets involved in cancer, e.g. disease specific proteins, receptors, enzymes and genes. Current Cancer Drug Targets publishes original research articles, letters, reviews / mini-reviews, drug clinical trial studies and guest edited thematic issues written by leaders in the field covering a range of current topics on drug targets involved in cancer. As the discovery, identification, characterization and validation of novel human drug targets for anti-cancer drug discovery continues to grow; this journal has become essential reading for all pharmaceutical scientists involved in drug discovery and development.