Development of a novel selective inhibitor of the Down syndrome-related kinase Dyrk1A

Y Ogawa, Y Nonaka, T Goto, E Ohnishi… - Nature …, 2010 - nature.com
Dyrk1A (dual-specificity tyrosine-(Y)-phosphorylation-regulated kinase 1A) is a
serine/threonine kinase essential for brain development and function, and its excessive …

Selectivity profiling and biological activity of novel β-carbolines as potent and selective DYRK1 kinase inhibitors

K Rüben, A Wurzlbauer, A Walte, W Sippl, F Bracher… - PloS one, 2015 - journals.plos.org
DYRK1A is a pleiotropic protein kinase with diverse functions in cellular regulation,
including cell cycle control, neuronal differentiation, and synaptic transmission. Enhanced …

Function and regulation of Dyrk1A: towards understanding Down syndrome

J Park, WJ Song, KC Chung - Cellular and molecular life sciences, 2009 - Springer
Down syndrome (DS) is associated with a variety of symptoms, such as incapacitating
mental retardation and neurodegeneration (ie, Alzheimer's disease), that prevent patients …

10-Iodo-11H-indolo[3,2-c]quinoline-6-carboxylic Acids Are Selective Inhibitors of DYRK1A

H Falke, A Chaikuad, A Becker, N Loaëc… - Journal of medicinal …, 2015 - ACS Publications
The protein kinase DYRK1A has been suggested to act as one of the intracellular regulators
contributing to neurological alterations found in individuals with Down syndrome. For an …

Design and synthesis of a library of lead-like 2, 4-bisheterocyclic substituted thiophenes as selective Dyrk/Clk inhibitors

C Schmitt, D Kail, M Mariano, M Empting, N Weber… - Plos one, 2014 - journals.plos.org
The Dyrk family of protein kinases is implicated in the pathogenesis of several diseases,
including cancer and neurodegeneration. Pharmacological inhibitors were mainly described …

The omnipresence of DYRK1A in human diseases

E Deboever, A Fistrovich, C Hulme… - International journal of …, 2022 - mdpi.com
The increasing population will challenge healthcare, particularly because the worldwide
population has never been older. Therapeutic solutions to age-related disease will be …

Activation, regulation, and inhibition of DYRK1A

W Becker, W Sippl - The FEBS journal, 2011 - Wiley Online Library
Dual‐specificity tyrosine phosphorylation‐regulated kinase 1A (DYRK1A) is a protein kinase
with diverse functions in neuronal development and adult brain physiology. Higher than …

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 …

A chemical with proven clinical safety rescues Down-syndrome-related phenotypes in through DYRK1A inhibition

H Kim, KS Lee, AK Kim, M Choi… - Disease models & …, 2016 - journals.biologists.com
ABSTRACT DYRK1A is important in neuronal development and function, and its excessive
activity is considered a significant pathogenic factor in Down syndrome and Alzheimer's …

Development of kinase-selective, harmine-based DYRK1A inhibitors that induce pancreatic human β-cell proliferation

K Kumar, P Wang, R Sanchez, EA Swartz… - Journal of medicinal …, 2018 - ACS Publications
DYRK1A has been implicated as an important drug target in various therapeutic areas,
including neurological disorders and oncology. DYRK1A has more recently been shown to …