DYRK1A inhibitors for disease therapy: Current status and perspectives

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.

Automated summary

DYRK1A, a conserved protein kinase, plays essential roles in various biological processes and is associated with Down syndrome, neurodegenerative diseases, cancer, and diabetes. The development of DYRK1A inhibitors has seen a rapid increase in recent years, providing new directions for future therapeutic research.