Abstract：
SET domain bifurcated histone lysine methyltransferase 1 (SETDB1) is an important epigenetic regulator catalyzing histone H3 lysine 9 (H3K9) methylation, specifically di-/tri-methylation. This regulation promotes gene silencing through heterochromatin formation. Aberrant SETDB1 expression, and its oncogenic role is evident in many cancers. Thus, SETDB1 is a valid target with novel therapeutic benefits. In this review, we explore the structural and biochemical features of SETDB1, its regulatory mechanisms, and its role in various cancers. We also discuss recent discoveries in small molecules targeting SETDB1 and provide suggestions for future research.
摘要：
SET结构域分叉组蛋白赖氨酸甲基转移酶1(SETDB1)是催化组蛋白H3赖氨酸9(H3K9)甲基化的重要表观遗传调节因子,特别是二/三甲基化。这种调节通过异染色质形成促进基因沉默。SETDB1表达异常，其致癌作用在许多癌症中都很明显。因此，SETDB1是具有新颖治疗益处的有效靶标。在这次审查中,我们探索SETDB1的结构和生化特征，其调控机制，以及它在各种癌症中的作用。我们还讨论了针对SETDB1的小分子的最新发现，并为未来的研究提供建议。
