Citation: Liyun Zhao, Xuan Xiong, Li Liu, Qi Liang, Rongsheng Tong, Xuanlin Feng, Lan Bai, Jianyou Shi. Recent research and development of DYRK1A inhibitors[J]. Chinese Chemical Letters, ;2022, 33(4): 1841-1849. doi: 10.1016/j.cclet.2021.10.003 shu

Recent research and development of DYRK1A inhibitors

Liyun Zhao ^{a, 1} ,
Xuan Xiong ^{a, 1} ,
Li Liu ^{a, 1} ,
Qi Liang ^b ,
Rongsheng Tong ^a ,
Xuanlin Feng ^{c, *,} ,
Lan Bai ^{a, *,} ,
Jianyou Shi ^{a, *,}

a.
Personalized Drug Therapy Key Laboratory of Sichuan Province, Sichuan Academy of Medical Science & Sichuan Provincial People's Hospital, School of Medicine, University of Electronic Science and Technology of China, Chengdu 610072, China
b.
College of Medicine, Southwest Jiaotong University, Chengdu 610031, China
c.
Emergency Intensive Care Unit, Personalized Drug Therapy Key Laboratory of Sichuan Province, Sichuan Academy of Medical Science & Sichuan Provincial People's Hospital, School of Medicine, University of Electronic Science and Technology of China, Chengdu 610072, China

23376592@qq.com

blci@163.com

shijianyoude@126.com

Received Date: 3 August 2021
Revised Date: 4 September 2021
Accepted Date: 4 October 2021
Available Online: 8 October 2021

Figures(9)

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.
- DYRK1A inhibitor,
- Natural product,
- Synthetic compound,
- Alzheimer's disease,
- Down syndrome
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沈阳化工大学材料科学与工程学院沈阳 110142