DYRK1A inhibitors for disease therapy: Current status and perspectives
DYRK1A inhibitors for disease therapy: Current status and perspectives
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DYRK1A 抑制剂用于疾病治疗：现状和前景
DOI：
10.1016/j.ejmech.2021.114062
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发表时间：
2022-02-05
影响因子：
6.7
通讯作者：
Zhang, Jifa
中科院分区：
文献类型：
--
作者：
Liu, Tong;Wang, Yuxi;Zhang, Jifa
双特异性酪氨酸磷酸化调节激酶1A（DYRK 1A）是一种保守的蛋白激酶，在多种生物学过程中发挥重要作用。它位于21号染色体q22.2区域，参与唐氏综合征（DS）的发病机制。此外，DYRK 1A已显示促进淀粉样蛋白β（A β）肽的积累，导致逐渐的Tau过度磷酸化，这有助于神经变性。此外，DRK 1A表达的改变也与癌症和糖尿病有关。近年来，DYRK 1A抑制剂的开发呈爆炸性增长。已经报道了多种新型DYRK 1A抑制剂作为人类疾病的潜在治疗。本文综述了DYRK 1A对不同疾病的治疗潜力以及新型DYRK 1A抑制剂的发现，为今后DYRK 1A抑制剂的开发和结构优化提供指导。nbsp;（c）2021 Elsevier Masson SAS。All rights reserved.
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.