DYRK1A inhibitors for disease therapy: Current status and perspectives

T Liu, Y Wang, J Wang, C Ren, H Chen… - European journal of …, 2022 - Elsevier
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 …

Dual-specificity, tyrosine phosphorylation-regulated kinases (DYRKs) and cdc2-like kinases (CLKs) in human disease, an overview

MF Lindberg, L Meijer - International Journal of Molecular Sciences, 2021 - mdpi.com
Dual-specificity tyrosine phosphorylation-regulated kinases (DYRK1A, 1B, 2-4) and cdc2-
like kinases (CLK1-4) belong to the CMGC group of serine/threonine kinases. These protein …

New β-carboline derivatives as potential α-glucosidase inhibitor: Synthesis and biological activity evaluation

J Lin, D Xiao, L Lu, B Liang, Z Xiong, X Xu - Journal of Molecular Structure, 2023 - Elsevier
Abstract α-Glucosidase is an important therapeutic target of diabetes mellitus. To find potent
α-glucosidase inhibitors, thirty-one β-carboline derivatives containing piperazine moieties …

Azaindole derivatives as potential kinase inhibitors and their SARs elucidation

G Fang, H Chen, Z Cheng, Z Tang, Y Wan - European Journal of Medicinal …, 2023 - Elsevier
Currently, heterocycles have occupied an important position in the fields of drug design.
Among them, azaindole moiety is regarded as one privileged scaffold to develop therapeutic …

Design, synthesis and biological evaluation of harmine derivatives as potent GSK-3β/DYRK1A dual inhibitors for the treatment of Alzheimer's disease

W Liu, X Liu, L Tian, Y Gao, W Liu, H Chen… - European Journal of …, 2021 - Elsevier
Alzheimer's disease (AD) is a chronic and progressive neurodegenerative disease,
characterized by irreversible cognitive impairment, memory loss and behavioral …

Function and inhibition of DYRK1A: emerging roles of treating multiple human diseases

Y Yang, X Fan, Y Liu, D Ye, C Liu, H Yang, Z Su… - Biochemical …, 2023 - Elsevier
Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) is an evolutionarily
conserved protein kinase and the most studied member of the Dual-specificity tyrosine …

novel medicinal chemistry strategies targeting CDK5 for Drug Discovery

W Tang, C Lin, Q Yu, D Zhang, Y Liu… - Journal of Medicinal …, 2023 - ACS Publications
Cyclin-dependent kinase 5 (CDK5) protein plays an important role not only in the central
nervous system but also in the periphery, including immune response, regulation of insulin …

MicroRNA-221-3p inhibits the inflammatory response of keratinocytes by regulating the DYRK1A/STAT3 signaling pathway to promote wound healing in diabetes

K Hu, L Liu, S Tang, X Zhang, H Chang… - Communications …, 2024 - nature.com
Diabetic foot ulcer (DFU), a serious complication of diabetes, remains a clinical challenge.
MicroRNAs affect inflammation and may have therapeutic value in DFU. Here, we find that …

Regeneration of pancreatic β-cells for diabetes therapeutics by natural DYRK1A inhibitors

Y Guo, L Li, Y Yao, H Li - Metabolites, 2022 - mdpi.com
The pathogenesis of diabetes mellitus is characterized by insulin resistance and islet β-cell
dysfunction. Up to now, the focus of diabetes treatment has been to control blood glucose to …

Design, synthesis and evaluation of indole-based bisacylhydrazone derivatives as α-glucosidase inhibitors

CM Hu, YY Zheng, AT Lin, X Zhang, XZ Wu… - Journal of Molecular …, 2023 - Elsevier
A series of indole-based bisacylhydrazone derivatives 4a∼ 4v were synthesized and
assessed for their α-glucosidase activities. The results presented that all synthesized …