Di Martile Marta, Del Bufalo Donatella, Trisciuoglio Daniela
Preclinical Models and New Therapeutic Agents Unit, Research, Advanced Diagnostics and Technological Innovation Department, Regina Elena National Cancer Institute, Rome, Italy.
Oncotarget. 2016 Aug 23;7(34):55789-55810. doi: 10.18632/oncotarget.10048.
Lysine acetylation is a post-translational modification that regulates gene transcription by targeting histones as well as a variety of transcription factors in the nucleus. Recently, several reports have demonstrated that numerous cytosolic proteins are also acetylated and that this modification, affecting protein activity, localization and stability has profound consequences on their cellular functions. Interestingly, most non-histone proteins targeted by acetylation are relevant for tumorigenesis. In this review, we will analyze the functional implications of lysine acetylation in different cellular compartments, and will examine our current understanding of lysine acetyltransferases family, highlighting the biological role and prognostic value of these enzymes and their substrates in cancer. The latter part of the article will address challenges and current status of molecules targeting lysine acetyltransferase enzymes in cancer therapy.
赖氨酸乙酰化是一种翻译后修饰，它通过作用于组蛋白以及细胞核中的多种转录因子来调节基因转录。最近，有几份报告表明，许多胞质蛋白也会发生乙酰化，并且这种修饰会影响蛋白质活性、定位和稳定性，对其细胞功能产生深远影响。有趣的是，大多数被乙酰化修饰的非组蛋白与肿瘤发生相关。在这篇综述中，我们将分析赖氨酸乙酰化在不同细胞区室中的功能意义，并审视我们目前对赖氨酸乙酰转移酶家族的理解，着重介绍这些酶及其底物在癌症中的生物学作用和预后价值。文章的后半部分将探讨在癌症治疗中靶向赖氨酸乙酰转移酶的分子所面临的挑战和现状。
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