Small molecule inhibitors of DYRK1A identified by computational and experimental approaches

HR Yoon, A Balupuri, KE Choi, NS Kang - International journal of …, 2020 - mdpi.com
Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) is a protein kinase
with diverse functions in cell regulation. Abnormal expression and activity of DYRK1A …

Discovery of a novel chemotype as DYRK1A inhibitors against Alzheimer's disease: Computational modeling and biological evaluation

N Qiu, C Qian, T Guo, Y Wang, H Jin, M Yao… - International Journal of …, 2024 - Elsevier
Dual-specificity tyrosine phosphorylation-regulated kinase 1 A (DYRK1A) plays an essential
role in Tau and Aβ pathology closely related to Alzheimer's disease (AD). Accumulative …

How to design potent and selective DYRK1B inhibitors? Molecular modeling study

A Szamborska-Gbur, E Rutkowska, A Dreas… - Journal of Molecular …, 2019 - Springer
DYRK1B protein kinase is an emerging anticancer target due to its overexpression in a
variety of cancers and its role in cancer chemoresistance through maintaining cancer cells in …

Novel and potential small molecule scaffolds as DYRK1A inhibitors by integrated molecular docking-based virtual screening and dynamics simulation study

MM Shahroz, HK Sharma, ASA Altamimi, MA Alamri… - Molecules, 2022 - mdpi.com
The dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) is a novel,
promising and emerging biological target for therapeutic intervention in neurodegenerative …

Multi-step virtual screening to develop selective DYRK1A inhibitors

T Koyama, N Yamaotsu, I Nakagome, S Ozawa… - Journal of Molecular …, 2017 - Elsevier
Developing selective inhibitors for a particular kinase remains a major challenge in kinase-
targeted drug discovery. Here we performed a multi-step virtual screening for dual-specificity …

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 …

Discovery of potent small molecule inhibitors of DYRK1A by structure-based virtual screening and bioassay

D Wang, F Wang, Y Tan, L Dong, L Chen, W Zhu… - Bioorganic & medicinal …, 2012 - Elsevier
In this study, six novel dual-specificity tyrosine phosphorylation regulated kinase 1A
(DYRK1A) inhibitors with IC50 values ranging from 1.51 to 88.13 μM were successfully …

[HTML][HTML] Identification and analysis of a selective DYRK1A inhibitor

TE Lin, MW Chao, WC HuangFu, HJ Tu… - Biomedicine & …, 2022 - Elsevier
The dysregulation of DYRK1A is implicated in many diseases such as cancer, diabetes, and
neurodegenerative diseases. Alzheimer's disease is one of the most common …

Discovery of a novel DYRK1A inhibitor with neuroprotective activity by virtual screening and in vitro biological evaluation

X Si, C Qian, N Qiu, Y Wang, M Yao, H Wang… - Molecular Diversity, 2024 - Springer
Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) is implicated in
accumulation of amyloid β-protein (Aβ) and phosphorylation of Tau proteins, and thus …

Updating dual-specificity tyrosine-phosphorylation-regulated kinase 2 (DYRK2): molecular basis, functions and role in diseases

A Correa-Sáez, R Jiménez-Izquierdo… - Cellular and Molecular …, 2020 - Springer
Members of the dual-specificity tyrosine-regulated kinase (DYRKs) subfamily possess a
distinctive capacity to phosphorylate tyrosine, serine, and threonine residues. Among the …