Selectivity Profiling and Biological Activity of Novel β-Carbolines as Potent and Selective DYRK1 Kinase Inhibitors

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

(2015) Hannes Falke et al.   JOURNAL OF MEDICINAL CHEMISTRY

A novel DYRK1A (Dual specificity tyrosine phosphorylation-regulated kinase 1A) inhibitor for the treatment of Alzheimer's disease: effect on Tau and amyloid pathologiesin vitro

(2015) Séverine Coutadeur et al.   JOURNAL OF NEUROCHEMISTRY

Chromatin-wide Profiling of DYRK1A Reveals a Role as a Gene-Specific RNA Polymerase II CTD Kinase

(2015) Chiara Di Vona et al.   MOLECULAR CELL

First Selective Dual Inhibitors of Tau Phosphorylation and Beta-Amyloid Aggregation, Two Major Pathogenic Mechanisms in Alzheimer’s Disease

(2014) Marica Mariano et al.   ACS Chemical Neuroscience

Computational & experimental evaluation of the structure/activity relationship of β-carbolines as DYRK1A inhibitors

(2014) Binia Drung et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The Down syndrome-related protein kinase DYRK1A phosphorylates p27Kip1and Cyclin D1 and induces cell cycle exit and neuronal differentiation

(2014) Ulf Soppa et al.   CELL CYCLE

DYRK1A: A Potential Drug Target for Multiple Down Syndrome Neuropathologies

(2014) Walter Becker et al.   CNS & Neurological Disorders-Drug Targets

A Form of the Metabolic Syndrome Associated with Mutations in DYRK1B

(2014) Ali R. Keramati et al.   NEW ENGLAND JOURNAL OF MEDICINE

Design and Synthesis of a Library of Lead-Like 2,4-Bisheterocyclic Substituted Thiophenes as Selective Dyrk/Clk Inhibitors

(2014) Christian Schmitt et al.   PLoS One

Overexpression of Dyrk1A Is Implicated in Several Cognitive, Electrophysiological and Neuromorphological Alterations Found in a Mouse Model of Down Syndrome

(2014) Susana García-Cerro et al.   PLoS One

Hydroxybenzothiophene Ketones Are Efficient Pre-mRNA Splicing Modulators Due to Dual Inhibition of Dyrk1A and Clk1/4

(2014) Christian Schmitt et al.   ACS Medicinal Chemistry Letters

New Perspectives of Dyrk1A Role in Neurogenesis and Neuropathologic Features of Down Syndrome

(2014) Joongkyu Park et al.   Experimental Neurobiology

Kinase Drug Discovery – What’s Next in the Field?

(2013) Philip Cohen et al.   ACS Chemical Biology

A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery

(2013) Yinghong Gao et al.   BIOCHEMICAL JOURNAL

A novel DYRK1B inhibitor AZ191 demonstrates that DYRK1B acts independently of GSK3β to phosphorylate cyclin D1 at Thr286, not Thr288

(2013) Anne L. Ashford et al.   BIOCHEMICAL JOURNAL

Exploiting the repertoire of CK2 inhibitors to target DYRK and PIM kinases

(2013) Giorgio Cozza et al.   BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS

Mechanism of dual specificity kinase activity of DYRK1A

(2013) Agnes Walte et al.   FEBS Journal

Epigallocatechin-3-gallate, a DYRK1A inhibitor, rescues cognitive deficits in Down syndrome mouse models and in humans

(2013) Rafael De la Torre et al.   MOLECULAR NUTRITION & FOOD RESEARCH

NGF Upregulates the Plasminogen Activation Inhibitor-1 in Neurons via the Calcineurin/NFAT Pathway and the Down Syndrome-Related Proteins DYRK1A and RCAN1 Attenuate This Effect

(2013) Georgios C. Stefos et al.   PLoS One

Recent Advances in the Design, Synthesis, and Biological Evaluation of Selective DYRK1A Inhibitors: A New Avenue for a Disease Modifying Treatment of Alzheimer’s?

(2012) Breland Smith et al.   ACS Chemical Neuroscience

Structure–activity relationship study of beta-carboline derivatives as haspin kinase inhibitors

(2012) Gregory D. Cuny et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Emerging role of DYRK family protein kinases as regulators of protein stability in cell cycle control

(2012) Walter Becker   CELL CYCLE

Selectivity, Cocrystal Structures, and Neuroprotective Properties of Leucettines, a Family of Protein Kinase Inhibitors Derived from the Marine Sponge Alkaloid Leucettamine B

(2012) Tania Tahtouh et al.   JOURNAL OF MEDICINAL CHEMISTRY

A public-private partnership to unlock the untargeted kinome

(2012) Stefan Knapp et al.   Nature Chemical Biology

Down syndrome: the brain in trisomic mode

(2012) Mara Dierssen   NATURE REVIEWS NEUROSCIENCE

Normalization of Dyrk1A expression by AAV2/1-shDyrk1A attenuates hippocampal-dependent defects in the Ts65Dn mouse model of Down syndrome

(2012) Xavier Altafaj et al.   NEUROBIOLOGY OF DISEASE

Wnt Signaling Orchestration with a Small Molecule DYRK Inhibitor Provides Long-Term Xeno-Free Human Pluripotent Cell Expansion

(2012) Kouichi Hasegawa et al.   Stem Cells Translational Medicine

Antitumor activity of a small-molecule inhibitor of the histone kinase Haspin

(2011) D Huertas et al.   ONCOGENE

Harmine is an ATP-competitive inhibitor for dual-specificity tyrosine phosphorylation-regulated kinase 1A (Dyrk1A)

(2010) Tatyana Adayev et al.   ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS

Structure–activity relationship study of acridine analogs as haspin and DYRK2 kinase inhibitors

(2010) Gregory D. Cuny et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Probing the Probes: Fitness Factors For Small Molecule Tools

(2010) Paul Workman et al.   CHEMISTRY & BIOLOGY

DYRK family of protein kinases: evolutionary relationships, biochemical properties, and functional roles

(2010) Sergi Aranda et al.   FASEB JOURNAL

MNB/DYRK1A as a multiple regulator of neuronal development

(2010) Francisco J. Tejedor et al.   FEBS Journal

Activation, regulation, and inhibition of DYRK1A

(2010) Walter Becker et al.   FEBS Journal

The role of DYRK1A in neurodegenerative diseases

(2010) Jerzy Wegiel et al.   FEBS Journal

The art of the chemical probe

(2010) Stephen V Frye   Nature Chemical Biology

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

(2010) Yasushi Ogawa et al.   Nature Communications

Guidelines for the effective use of chemical inhibitors of protein function to understand their roles in cell regulation: Table 1

(2009) Philip Cohen   BIOCHEMICAL JOURNAL

Insights into protein kinase regulation and inhibition by large scale structural comparison

(2009) Jeyanthy Eswaran et al.   BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS

Haspin: a newly discovered regulator of mitotic chromosome behavior

(2009) Jonathan M. G. Higgins   CHROMOSOMA

Harmine specifically inhibits protein kinase DYRK1A and interferes with neurite formation

(2009) Nora Göckler et al.   FEBS Journal

Targeting Dyrk1A with AAVshRNA Attenuates Motor Alterations in TgDyrk1A, a Mouse Model of Down Syndrome

(2008) Jon Ortiz-Abalia et al.   AMERICAN JOURNAL OF HUMAN GENETICS

The down syndrome candidate dual-specificity tyrosine phosphorylation-regulated kinase 1A phosphorylates the neurodegeneration-related septin 4

(2008) J.H. Sitz et al.   NEUROSCIENCE