DYRK1A型
去氢骆驼蓬碱
化学
激酶
蛋白激酶A
计算生物学
生物化学
药理学
生物
作者
Liyun Zhao,Xuan Xiong,Li Liu,Qi Liang,Rongsheng Tong,Xuanlin Feng,Lan Bai,Jianyou Shi
标识
DOI:10.1016/j.cclet.2021.10.003
摘要
Dual specificity tyrosine phosphorylation regulated kinase 1A (DYRK1A) is an evolutionarily conserved protein kinase belonging to the CMGC kinase family, which is closely related to Down syndrome (DS) and Alzheimer's disease (AD). In recent years, not only the treatment of diabetes, but also the treatment of cancer gradually focuses on targeting DYRK1A. Therefore, a series of DYRK1A inhibitors have been developed to treat relevant diseases and clarify their treatment mechanism furtherly. DYRK1A inhibitors are mainly divided into natural products and synthetic compounds. Among them, harmine is an excellent DYRK1A inhibitor. Therefore, the synthetic DYRK1A inhibitors are mainly based on harmine, which greatly enriches the structure and quantity of DYRK1A inhibitors. The interaction between the inhibitors and the DYRK1A protein has a guiding significance in predicting the activity of the inhibitors, and plays an irreplaceable role in the design of the compounds. This paper mainly reviews DYRK1A inhibitors found in recent years and their structure-activity relationship, looking forward to providing a theoretical basis for the development of DYRK1A inhibitors.
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