Selective inhibition of the kinase DYRK1A by targeting its folding process

A high-throughput chemical screen reveals that harmine-mediated inhibition of DYRK1A increases human pancreatic beta cell replication

(2015) Peng Wang et al.   NATURE MEDICINE

Inhibition of DYRK1A and GSK3B induces human β-cell proliferation

(2015) Weijun Shen et al.   Nature Communications

Identification of a DYRK1A Inhibitor that Induces Degradation of the Target Kinase using Co-chaperone CDC37 fused with Luciferase nanoKAZ

(2015) Rie Sonamoto et al.   Scientific Reports

Mechanism of dual specificity kinase activity of DYRK1A

(2013) Agnes Walte et al.   FEBS Journal

Triplication of DYRK1A causes retinal structural and functional alterations in Down syndrome

(2013) Ariadna Laguna et al.   HUMAN MOLECULAR GENETICS

Chaperones as thermodynamic sensors of drug-target interactions reveal kinase inhibitor specificities in living cells

(2013) Mikko Taipale et al.   NATURE BIOTECHNOLOGY

ATP-competitive inhibitors block protein kinase recruitment to the Hsp90-Cdc37 system

(2013) Sigrun Polier et al.   Nature Chemical Biology

Structures of Down Syndrome Kinases, DYRKs, Reveal Mechanisms of Kinase Activation and Substrate Recognition

(2013) Meera Soundararajan et al.   STRUCTURE

Quantitative Analysis of Hsp90-Client Interactions Reveals Principles of Substrate Recognition

(2012) Mikko Taipale et al.   CELL

Increased dosage of the chromosome 21 ortholog Dyrk1a promotes megakaryoblastic leukemia in a murine model of Down syndrome

(2012) Sébastien Malinge et al.   JOURNAL OF CLINICAL INVESTIGATION

Cotranslational cis-phosphorylation of the COOH-terminal tail is a key priming step in the maturation of cAMP-dependent protein kinase

(2012) M. M. Keshwani et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Privileged Scaffolds or Promiscuous Binders: A Comparative Study on Rhodanines and Related Heterocycles in Medicinal Chemistry

(2011) Thomas Mendgen et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

New Substructure Filters for Removal of Pan Assay Interference Compounds (PAINS) from Screening Libraries and for Their Exclusion in Bioassays

(2010) Jonathan B. Baell et al.   JOURNAL OF MEDICINAL CHEMISTRY

Characterization of a Domain That Transiently Converts Class 2 DYRKs into Intramolecular Tyrosine Kinases

(2010) R. Kinstrie et al.   Science Signaling

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

(2010) Yasushi Ogawa et al.   Nature Communications

Identification of the Autophosphorylation Sites of LRRK2

(2009) Shogo Kamikawaji et al.   BIOCHEMISTRY

Targeting protein kinases in central nervous system disorders

(2009) Laura K. Chico et al.   NATURE REVIEWS DRUG DISCOVERY

Protein Kinase Activation Loop Autophosphorylation in Cis: Overcoming a Catch-22 Situation

(2009) P. A. Lochhead   Science Signaling

Overexpression of Dyrk1A contributes to neurofibrillary degeneration in Down syndrome

(2008) Fei Liu et al.   FASEB JOURNAL

The Parkinson Disease-associated Leucine-rich Repeat Kinase 2 (LRRK2) Is a Dimer That Undergoes Intramolecular Autophosphorylation

(2008) Elisa Greggio et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

CRAF Autophosphorylation of Serine 621 Is Required to Prevent Its Proteasome-Mediated Degradation

(2008) Catherine Noble et al.   MOLECULAR CELL

A quantitative analysis of kinase inhibitor selectivity

(2008) Mazen W Karaman et al.   NATURE BIOTECHNOLOGY