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Emerging role of SETDB1 as a therapeutic target

机译:SetdB1作为治疗目标的新兴作用

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Introduction: Epigenetic changes lead to aberrant gene expression in cancer. SETDB1, a histone lysine methyltransferase plays an important role in methylation and gene silencing. Aberrant histone methylation at H3K9 by SETDB1 promotes silencing of tumor suppressor genes and thus contributes to carcinogenesis. Recent studies indicate that SETDB1 is abnormally expressed in various human cancer conditions which contributed to enhanced tumor growth and metastasis. Hence, SETDB1 appears to be a promising epigenetic target for therapeutic intervention.Areas covered: In this article, the structural features, localization and functions of SETDB1 are reviewed. Also, an overview of the role of SETDB1 in cancer and other disease mechanisms, the currently studied inhibitors for SETDB1 are mentioned.Expert opinion: Silencing of tumor suppressor genes due to excessive trimethylation at H3K9 by amplified SETDB1 levels is found in various cancerous conditions. Since epigenetic changes are reversible, SETDB1 holds promise as an important therapeutic target for cancer. Therefore, a better understanding of the role of SETDB1 and its interaction with various proteins in cancer-related mechanisms along with therapeutic interventions specific for SETDB1 may improve targeted cancer therapy.
机译:介绍:表观遗传变化导致癌症中异常基因表达。 SetDB1,组蛋白赖氨酸甲基转移酶在甲基化和基因沉默中起重要作用。 SetDB1的H3K9处的异常组蛋白甲基化促进肿瘤抑制基因的沉默,从而有助于致癌作用。最近的研究表明SetDB1在各种人类癌症条件下异常表达,这有助于增强肿瘤生长和转移。因此,SetDB1似乎是治疗干预的有希望的表观遗传目标。覆盖:在本文中,审查SetDB1的结构特征,本地化和功能。此外,概述了SetDB1在癌症和其他疾病机制中,目前研究的SetDB1的抑制剂.pert意见:在各种癌症条件下发现了由于H3K9的过量三甲基化引起的肿瘤抑制基因的沉默。由于表观遗传变化是可逆的,因此SetdB1将承担承担癌症的重要治疗目标。因此,更好地理解SetdB1的作用及其与癌症相关机制中各种蛋白质的相互作用以及对SetDB1特异的治疗干预措施可以改善靶向癌症治疗。

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