Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) inhibitors as potential therapeutics

DB Jarhad, KK Mashelkar, HR Kim… - Journal of medicinal …, 2018 - ACS Publications
… Although intense efforts have been made to develop DYRK1A inhibitors, highly potent
and specific inhibitors are still lacking. Many inhibitors of DYRK1A from natural and synthetic …

Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) inhibitors: A survey of recent patent literature

TL Nguyen, C Fruit, Y Hérault, L Meijer… - Expert opinion on …, 2017 - Taylor & Francis
… Like most tyrosine kinase inhibitors developed up to the market, DYRK1A inhibitors are …
inhibiting the catalytic activity of DYRK1A. Expert opinion: Despite the important role of DYRK1A

Mechanism of dual specificity kinase activity of DYRK 1 A

A Walte, K Rüben, R Birner‐Gruenberger… - The FEBS …, 2013 - Wiley Online Library
DYRK1A that may account for its dual specificity kinase activity. For a broad coverage of
chemical scaffolds, we compiled a series of compounds comprising known DYRK1A inhibitors (…

A novel DYRK1A (dual specificity tyrosine phosphorylation‐regulated kinase 1A) inhibitor for the treatment of Alzheimer's disease: effect on Tau and amyloid …

S Coutadeur, H Benyamine, L Delalonde… - Journal of …, 2015 - Wiley Online Library
… tyrosine-phosphorylation-regulated kinase 1A (DYRK1A) is a new high-potential … novel
potent and selective DYRK1A inhibitor. EHT 5372 inhibits DYRK1A-induced Tau phosphorylation…

Novel scaffolds for Dual specificity tyrosine-phosphorylation-regulated kinase (DYRK1A) inhibitors

A Czarna, J Wang, D Zelencova, Y Liu… - Journal of medicinal …, 2018 - ACS Publications
… of DYRK1A in diabetes. Here we report a variety of scaffolds not generally known for DYRK1A
inhibition, … These inhibitors effectively block the tau phosphorylation that is a hallmark of …

Fragment-derived selective inhibitors of dual-specificity kinases DYRK1A and DYRK1B

D Lee Walmsley, JB Murray, P Dokurno… - Journal of medicinal …, 2021 - ACS Publications
… -penetrant DYRK1A inhibitor which showed in vivo activity in a tumor model. The inhibitor
provides a useful tool compound for further exploration of the effect of DYRK1A inhibition in …

Recent research and development of DYRK1A inhibitors

L Zhao, X Xiong, L Liu, Q Liang, R Tong, X Feng… - Chinese Chemical …, 2022 - Elsevier
Dual specificity tyrosine phosphorylation regulated kinase 1A (… inhibitors, and plays an
irreplaceable role in the design of the compounds. This paper mainly reviews DYRK1A inhibitors

Inhibitors of dual-specificity tyrosine phosphorylation-regulated kinases (DYRK) exert a strong anti-herpesviral activity

C Hutterer, J Milbradt, S Hamilton, M Zaja, J Leban… - Antiviral research, 2017 - Elsevier
… Inhibitory effect of DYRK1 inhibitors and transient DYRK1A knockdown, respectively, on
HCMV protein production and viral replication. (A) Inhibitory effect of DYRK inhibitors on …

A dual specificity kinase, DYRK1A, as a potential therapeutic target for head and neck squamous cell carcinoma

A Radhakrishnan, V Nanjappa, R Raja, G Sathe… - Scientific reports, 2016 - nature.com
… We studied the effect of DYRK1A inhibition in HNSCC cell lines. Our study demonstrates that
inhibition of DYRK1A led to cell death via decrease in phosphorylation of FOXO3A which is …

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
… , which inhibits DYRK1A by interfering with its folding process [254], all reported inhibitors
… Several DYRK1A inhibitors have been reported in recent years (reviews: [88,93,95]) which, …