药学学报, 2019, 54(5): 778-787
引用本文:
杨雨薇, 尚爽, 胡卓伟, 花芳. 赖氨酸乙酰化的研究进展及应用[J]. 药学学报, 2019, 54(5): 778-787.
YANG Yu-wei, SHANG Shuang, HU Zhuo-wei, HUA Fang. Advances and applications of lysine acetylation[J]. Acta Pharmaceutica Sinica, 2019, 54(5): 778-787.

赖氨酸乙酰化的研究进展及应用
杨雨薇, 尚爽, 胡卓伟, 花芳
中国医学科学院、北京协和医学院药物研究所, 天然药物活性物质与功能国家重点实验室, 新药作用机制研究与药效评价北京市重点实验室(BZ0150), 北京 100050
摘要:
蛋白质乙酰化是指在乙酰基转移酶的作用下,蛋白质的赖氨酸残基添加乙酰基的过程。它是连接乙酰辅酶A代谢与细胞信号转导的重要蛋白质翻译后修饰类型。近年来,质谱鉴定的发展提高了研究者对赖氨酸乙酰化的认识,赖氨酸乙酰化参与基因转录、蛋白降解、细胞代谢、应激反应等多个细胞过程,通过调节蛋白质相互作用、活性、稳定性和定位影响其生物学功能,在代谢相关疾病、肿瘤、心血管疾病等多种疾病中发挥重要调控作用。目前,去乙酰化酶抑制剂已经在肿瘤、代谢相关疾病及其他多种疾病中显示出巨大的治疗潜力。本文围绕乙酰化的研究历程、生物学功能及应用进行了归纳和探讨,并对未来研究进行了展望和讨论。
关键词:    乙酰化作用      代谢      蛋白质修饰      转译     
Advances and applications of lysine acetylation
YANG Yu-wei, SHANG Shuang, HU Zhuo-wei, HUA Fang
State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Beijing Key Laboratory of New Drug Mechanisms and Pharmacological Evaluation Study(BZ0150), Institute of Meteria Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
Abstract:
Protein acetylation is a process of adding an acetyl group to a protein lysine residue with the help of acetyltransferase, which is a pivotal protein post-translational modification linking acetyl-CoA metabolism and cell signal transduction. Recently, the development of mass spectrometry has deepened our understanding of lysine acetylation. Lysine acetylation is involved in many processes such as gene transcription, protein degradation, cellular metabolism, and stress response, which affects biological processes by regulating protein interactions, activity, stability and localization. Protein acetylation is widely happened and plays important regulatory roles in a diversity of human diseases such as metabolic diseases, tumors and cardiovascular diseases. Besides, deacetylase inhibitors have displayed a great potential in the treatment of various diseases especially tumors and metabolic associated diseases. In this review, we summarized the advances and application of acetylation, and discussed the remaining problems in this area.
Key words:    acetylation    metabolism    protein modification    translational   
收稿日期: 2019-01-05
DOI: 10.16438/j.0513-4870.2019-0014
基金项目: 国家自然科学基金面上项目(81472717,81673474);北京市自然科学基金面上项目(7162133);中国医学科学院医学与健康科技创新工程(2016-I2M-1-007).
通讯作者: 花芳,Tel:86-10-83165034,E-mail:huafang@imm.ac.cn
Email: huafang@imm.ac.cn
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