Targeting the acetylation signaling pathway in cancer therapy.
Targeting the acetylation signaling pathway in cancer therapy.
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DOI：
10.1016/j.semcancer.2021.03.001
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发表时间：
2022-10
影响因子：
14.5
通讯作者：
Wei W
中科院分区：
文献类型：
--
作者：
Dang F;Wei W
乙酰化是蛋白质翻译后的主要修饰之一，它将乙酰基官能团引入赖氨酸残基等氨基酸中，产生醋酸酯键，中和其正电荷。乙酰化对蛋白质功能的调节有多种方式，如影响蛋白质的稳定性、活性、定位以及与其他蛋白质或DNA的相互作用。已有研究表明，组蛋白乙酰转移酶（HATs）和组蛋白去乙酰化酶（hdac）加入转录机制可以调节组蛋白乙酰化状态，直接参与控制细胞增殖和分裂的基因的动态调控。基因表达失调与肿瘤发生有关，而组蛋白去乙酰化酶的异常激活已在几种类型的癌症中得到报道。此外，越来越多的证据表明，乙酰化广泛参与非组蛋白，影响其在包括肿瘤发生在内的各种细胞过程中的作用。因此，抑制HAT或HDAC酶活性的小分子化合物已被开发和研究用于治疗目的。本文综述了蛋白质乙酰化的最新进展，并讨论了靶向乙酰化信号通路在癌症中的治疗潜力。
Acetylation represents one of the major post-translational protein modifications, which introduces an acetyl functional group into amino acids such as the lysine residue to yield an acetate ester bond, neutralizing its positive charge. Regulation of protein functions by acetylation occurs in multiple ways, such as affecting protein stability, activity, localization, and interaction with other proteins or DNA. It has been well documented that the recruitment of histone acetyltransferases (HATs) and histone deacetylases (HDACs) to the transcriptional machinery can modulate histone acetylation status, which is directly involved in the dynamic regulation of genes controlling cell proliferation and division. Dysregulation of gene expression is involved in tumorigenesis and aberrant activation of histone deacetylases has been reported in several types of cancer. Moreover, there is growing body of evidence showing that acetylation is widely involved in non-histone proteins to impact their roles in various cellular processes including tumorigenesis. As such, small molecular compounds inhibiting HAT or HDAC enzymatic activities have been developed and investigated for therapeutic purpose. Here we review the recent progress in our understanding of protein acetylation and discuss the therapeutic potential of targeting the acetylation signaling pathway in cancer.
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