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Small molecule inhibitors of histone acetyltransferases and deacetylases are potential drugs for inflammatory diseases

机译:组蛋白乙酰基转移酶和脱乙酰基酶的小分子抑制剂是治疗炎症性疾病的潜在药物

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摘要

Lysine acetylation is a reversible post-translational modification (PTM) of cellular proteins and represents an important regulatory switch in signal transduction. Lysine acetylation, in combination with other PTMs, directs the outcomes as well as the activation levels of important signal transduction pathways such as the nuclear factor (NF)-κB pathway. Small molecule modulators of the 'writers' (HATs) and 'erasers' (HDACs) can regulate the NF-κB pathway in a specific manner. This review focuses on the effects of frequently used HAT and HDAC inhibitors on the NF-κB signal transduction pathway and inflammatory responses, and their potential as novel therapeutics.
机译:赖氨酸乙酰化是细胞蛋白的可逆翻译后修饰(PTM),代表信号转导中的重要调节开关。赖氨酸乙酰化与其他PTM结合使用可指导结果以及重要信号转导途径(如核因子(NF)-κB途径)的激活水平。 “作者”(HATs)和“橡皮擦”(HDACs)的小分子调节剂可以特定方式调节NF-κB途径。这篇综述集中于常用的HAT和HDAC抑制剂对NF-κB信号转导途径和炎症反应的影响,以及它们作为新型疗法的潜力。

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