摘要
在过去的十年中,从细菌到哺乳动物的乙酰化蛋白的数量呈指数级增长,现在人们普遍认为乙酰化是大多数真核生物信号通路的关键组成部分,与磷酸化一样重要。参与这一过程的酶在哺乳动物中得到了很好的描述;乙酰转移酶和去乙酰化酶存在于核室内外,具有不同的调节功能。在锥虫中,其中一些酶已经被描述,并被假定为合理设计药物的新的抗寄生虫靶点。在这篇综述文章中,我们提出了一个在锥虫中已知的最重要的乙酰化蛋白的更新,分析了可用的乙酰化体。此外,我们还总结了关于锥虫中乙酰转移酶和去乙酰化酶的现有信息及其作为化疗靶点的潜在用途。
关键词: 乙酰化,乙酰转移酶,去乙酰化酶,乙酰化体,锥虫,细胞骨架。
Current Medicinal Chemistry
Title:Update on the Biological Relevance of Lysine Acetylation as a Novel Drug Target in Trypanosomatids
Volume: 29 Issue: 20
关键词: 乙酰化,乙酰转移酶,去乙酰化酶,乙酰化体,锥虫,细胞骨架。
摘要: The number of acetylated proteins identified from bacteria to mammals has grown exponentially in the last ten years, and it is now accepted that acetylation is a key component in most eukaryotic signaling pathways and is as important as phosphorylation. The enzymes involved in this process are well described in mammals; acetyltransferases and deacetylases are found inside and outside the nuclear compartment and have different regulatory functions. In trypanosomatids, several of these enzymes have been described and are postulated to be novel antiparasitic targets for the rational design of drugs. In this review article, we present an update of the most important known acetylated proteins in trypanosomatids, analyzing the acetylomes available. Also, we summarize the information available regarding acetyltransferases and deacetylases in trypanosomes and their potential use as chemotherapeutic targets.
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Cite this article as:
Update on the Biological Relevance of Lysine Acetylation as a Novel Drug Target in Trypanosomatids, Current Medicinal Chemistry 2022; 29 (20) . https://dx.doi.org/10.2174/0929867328666211126145721
DOI https://dx.doi.org/10.2174/0929867328666211126145721 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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