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

D Lee Walmsley, JB Murray, P Dokurno… - Journal of medicinal …, 2021 - ACS Publications
The serine/threonine kinase DYRK1A has been implicated in regulation of a variety of
cellular processes associated with cancer progression, including cell cycle control, DNA …

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

DB Jarhad, KK Mashelkar, HR Kim… - Journal of medicinal …, 2018 - ACS Publications
Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) is a member of an
evolutionarily conserved family of protein kinases that belongs to the CMGC group of …

DYRK1A kinase inhibitors with emphasis on cancer

A Ionescu, F Dufrasne, M Gelbcke… - Mini reviews in …, 2012 - ingentaconnect.com
Various types of cancers (including gliomas, melanomas, and esophageal, pancreas and
non-small-cell lung cancers) display intrinsic resistance to pro-apoptotic stimuli, such as …

DYRK1A in neurodegeneration and cancer: Molecular basis and clinical implications

R Abbassi, TG Johns, M Kassiou, L Munoz - Pharmacology & therapeutics, 2015 - Elsevier
Protein kinases are one of the most studied drug targets in current pharmacological
research, as evidenced by the vast number of kinase-targeting agents enrolled in active …

Structure-guided discovery of potent and selective DYRK1A inhibitors

C Weber, M Sipos, A Paczal, B Balint… - Journal of medicinal …, 2021 - ACS Publications
The kinase DYRK1A is an attractive target for drug discovery programs due to its implication
in multiple diseases. Through a fragment screen, we identified a simple biaryl compound …

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
Introduction: Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) is a
eukaryotic serine-threonine protein kinase belonging to the CMGC group. DYRK1A …

The DYRK family of kinases in cancer: molecular functions and therapeutic opportunities

J Boni, C Rubio-Perez, N López-Bigas, C Fillat… - Cancers, 2020 - mdpi.com
DYRK (dual-specificity tyrosine-regulated kinases) are an evolutionary conserved family of
protein kinases with members from yeast to humans. In humans, DYRKs are pleiotropic …

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 …

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 …

Mechanism of dual specificity kinase activity of DYRK 1 A

A Walte, K Rüben, R Birner‐Gruenberger… - The FEBS …, 2013 - Wiley Online Library
The function of many protein kinases is controlled by the phosphorylation of a critical
tyrosine residue in the activation loop. Dual specificity tyrosine‐phosphorylation‐regulated …