GLP and G9a histone methyltransferases as potential therapeutic targets for lymphoid neoplasms.

IF 5.3 2区医学 Q1 ONCOLOGY Cancer Cell International Pub Date : 2024-07-12 DOI:10.1186/s12935-024-03441-y

Amandda Évelin Silva-Carvalho, Luma Dayane Carvalho Filiú-Braga, Gabriela Muller Reche Bogéa, Alan Jhones Barbosa de Assis, Fábio Pittella-Silva, Felipe Saldanha-Araujo

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Abstract

Histone methyltransferases (HMTs) are enzymes that regulate histone methylation and play an important role in controlling transcription by altering the chromatin structure. Aberrant activation of HMTs has been widely reported in certain types of neoplastic cells. Among them, G9a/EHMT2 and GLP/EHMT1 are crucial for H3K9 methylation, and their dysregulation has been associated with tumor initiation and progression in different types of cancer. More recently, it has been shown that G9a and GLP appear to play a critical role in several lymphoid hematologic malignancies. Importantly, the key roles played by both enzymes in various diseases made them attractive targets for drug development. In fact, in recent years, several groups have tried to develop small molecule inhibitors targeting their epigenetic activities as potential anticancer therapeutic tools. In this review, we discuss the physiological role of GLP and G9a, their oncogenic functions in hematologic malignancies of the lymphoid lineage, and the therapeutic potential of epigenetic drugs targeting G9a/GLP for cancer treatment.

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作为淋巴肿瘤潜在治疗靶点的 GLP 和 G9a 组蛋白甲基转移酶。

组蛋白甲基转移酶（HMTs）是一种调节组蛋白甲基化的酶，通过改变染色质结构在控制转录方面发挥着重要作用。在某些类型的肿瘤细胞中，HMTs 的异常激活已被广泛报道。其中，G9a/EHMT2 和 GLP/EHMT1 对 H3K9 甲基化至关重要，它们的失调与不同类型癌症的肿瘤发生和发展有关。最近的研究表明，G9a 和 GLP 似乎在几种淋巴血液恶性肿瘤中发挥着关键作用。重要的是，这两种酶在各种疾病中发挥的关键作用使它们成为具有吸引力的药物开发目标。事实上，近年来已有多个研究小组尝试开发针对其表观遗传活性的小分子抑制剂，作为潜在的抗癌治疗工具。在这篇综述中，我们将讨论 GLP 和 G9a 的生理作用、它们在淋巴系血液恶性肿瘤中的致癌功能，以及针对 G9a/GLP 的表观遗传药物在癌症治疗中的潜力。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Cancer Cell International ONCOLOGY-

CiteScore

10.90

自引率

1.70%

发文量

360

审稿时长

1 months

期刊介绍： Cancer Cell International publishes articles on all aspects of cancer cell biology, originating largely from, but not limited to, work using cell culture techniques. The journal focuses on novel cancer studies reporting data from biological experiments performed on cells grown in vitro, in two- or three-dimensional systems, and/or in vivo (animal experiments). These types of experiments have provided crucial data in many fields, from cell proliferation and transformation, to epithelial-mesenchymal interaction, to apoptosis, and host immune response to tumors. Cancer Cell International also considers articles that focus on novel technologies or novel pathways in molecular analysis and on epidemiological studies that may affect patient care, as well as articles reporting translational cancer research studies where in vitro discoveries are bridged to the clinic. As such, the journal is interested in laboratory and animal studies reporting on novel biomarkers of tumor progression and response to therapy and on their applicability to human cancers.