DYRK1A inhibitors for disease therapy: Current status and perspectives

被引：81
作者：
Liu, Tong [1 ,2 ,3 ]
Wang, Yuxi [1 ,2 ,3 ,6 ,7 ]
Wang, Jiaxing [5 ]
Ren, Changyu [4 ]
Chen, Hao [5 ]
Zhang, Jifa [1 ,2 ,3 ,6 ,7 ]
机构：
[1] Sichuan Univ, Frontiers Sci Ctr Dis Related Mol Network, Targeted Tracer Res & Dev Lab,Inst Resp Hlth,West, Natl Clin Res Ctr Geriatr,Joint Inst Altitude Hlt, Chengdu 610041, Sichuan, Peoples R China
[2] Sichuan Univ, Dept Resp & Crit Care Med, Natl Clin Res Ctr Geriatr, West China Hosp,State Key Lab Biotherapy, Chengdu 610041, Sichuan, Peoples R China
[3] Sichuan Univ, West China Hosp, Natl Clin Res Ctr Geriatr, Canc Ctr,Dept Resp & Crit Care Med, Chengdu 610041, Sichuan, Peoples R China
[4] Chengdu Fifth Peoples Hosp, Dept Pharm, Chengdu 611130, Sichuan, Peoples R China
[5] Univ Tennessee, Ctr Hlth Sci, Coll Pharm, Dept Pharmaceut Sci, Memphis, TN 38163 USA
[6] Sichuan Univ, West China Hosp, Precis Med Key Lab Sichuan Prov, Chengdu 610041, Sichuan, Peoples R China
[7] Sichuan Univ, West China Hosp, Precis Med Res Ctr, Chengdu 610041, Sichuan, Peoples R China
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2022年 / 229卷
关键词：
DS; Cancer; DYRK1A; DYRK1A inhibitor; Drug design; Structure activity relationships; PHOSPHORYLATION-REGULATED KINASE; MET UP-REGULATION; DOWN-SYNDROME; DUAL-SPECIFICITY; BIOLOGICAL EVALUATION; CANCER CELLS; DYRK1A-MEDIATED PHOSPHORYLATION; ALZHEIMERS-DISEASE; HARMINE SUPPRESSES; HIGHLY POTENT;
D O I：
10.1016/j.ejmech.2021.114062
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Dual-specificity tyrosine phosphorylation-regulated kinase 1 A (DYRK1A) is a conserved protein kinase that plays essential roles in various biological processes. It is located in the region q22.2 of chromosome 21, which is involved in the pathogenesis of Down syndrome (DS). Moreover, DYRK1A has been shown to promote the accumulation of amyloid beta (A beta) peptides leading to gradual Tau hyperphosphorylation, which contributes to neurodegeneration. Additionally, alterations in the DRK1A expression are also associated with cancer and diabetes. Recent years have witnessed an explosive increase in the development of DYRK1A inhibitors. A variety of novel DYRK1A inhibitors have been reported as potential treatments for human diseases. In this review, the latest therapeutic potential of DYRK1A for different diseases and the novel DYRK1A inhibitors discoveries are summarized, guiding future inhibitor development and structural optimization.& nbsp;(c) 2021 Elsevier Masson SAS. All rights reserved.
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页数：18
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