Walter Becker
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View article: Dyr726, a brain-penetrant inhibitor of PI3Kα, Type III receptor tyrosine kinases, and WNT signaling
Dyr726, a brain-penetrant inhibitor of PI3Kα, Type III receptor tyrosine kinases, and WNT signaling Open
The vast majority of clinical small molecule multi-kinase inhibitors (mKI) report abject failures in targeting cancers with high stem cell contents like high-grade glioma and colorectal cancers. The FDA-approved mKIs to date ablate recepto…
View article: Elevated expression levels of the protein kinase DYRK1B induce mesenchymal features in A549 lung cancer cells
Elevated expression levels of the protein kinase DYRK1B induce mesenchymal features in A549 lung cancer cells Open
Background The protein kinase DYRK1B is a negative regulator of cell proliferation but has been found to be overexpressed in diverse human solid cancers. While DYRK1B is recognized to promote cell survival and adaption to stressful conditi…
View article: Differential regulation of expression of the protein kinases DYRK1A and DYRK1B in cancer cells
Differential regulation of expression of the protein kinases DYRK1A and DYRK1B in cancer cells Open
View article: Functional characterization of two DYRK1B variants causative of AOMS3
Functional characterization of two DYRK1B variants causative of AOMS3 Open
View article: Differential maturation and chaperone dependence of the paralogous protein kinases DYRK1A and DYRK1B
Differential maturation and chaperone dependence of the paralogous protein kinases DYRK1A and DYRK1B Open
View article: Discovery of novel 6-hydroxybenzothiazole urea derivatives as dual Dyrk1A/α-synuclein aggregation inhibitors with neuroprotective effects
Discovery of novel 6-hydroxybenzothiazole urea derivatives as dual Dyrk1A/α-synuclein aggregation inhibitors with neuroprotective effects Open
View article: The Unfolded Protein Response Is a Major Driver of LCN2 Expression in BCR–ABL- and JAK2V617F-Positive MPN
The Unfolded Protein Response Is a Major Driver of LCN2 Expression in BCR–ABL- and JAK2V617F-Positive MPN Open
Lipocalin 2 (LCN2), a proinflammatory mediator, is involved in the pathogenesis of myeloproliferative neoplasms (MPN). Here, we investigated the molecular mechanisms of LCN2 overexpression in MPN. LCN2 mRNA expression was 20-fold upregulat…
View article: How to Separate Kinase Inhibition from Undesired Monoamine Oxidase A Inhibition—The Development of the DYRK1A Inhibitor AnnH75 from the Alkaloid Harmine
How to Separate Kinase Inhibition from Undesired Monoamine Oxidase A Inhibition—The Development of the DYRK1A Inhibitor AnnH75 from the Alkaloid Harmine Open
The β-carboline alkaloid harmine is a potent DYRK1A inhibitor, but suffers from undesired potent inhibition of MAO-A, which strongly limits its application. We synthesized more than 60 analogues of harmine, either by direct modification of…
View article: Development of novel amide–derivatized 2,4-bispyridyl thiophenes as highly potent and selective Dyrk1A inhibitors. Part II: Identification of the cyclopropylamide moiety as a key modification
Development of novel amide–derivatized 2,4-bispyridyl thiophenes as highly potent and selective Dyrk1A inhibitors. Part II: Identification of the cyclopropylamide moiety as a key modification Open
View article: Development of novel 2,4-bispyridyl thiophene–based compounds as highly potent and selective Dyrk1A inhibitors. Part I: Benzamide and benzylamide derivatives
Development of novel 2,4-bispyridyl thiophene–based compounds as highly potent and selective Dyrk1A inhibitors. Part I: Benzamide and benzylamide derivatives Open
View article: Mutational analysis of two residues in the DYRK homology box of the protein kinase DYRK1A
Mutational analysis of two residues in the DYRK homology box of the protein kinase DYRK1A Open
When expressed in HeLa cells, DYRK1A-D138P and K150C showed no significant difference from wild type DYRK1A regarding the activating tyrosine autophosphorylation or catalytic activity towards exogenous substrates. However, both DYRK1A vari…
View article: Functional characterization of DYRK1A missense variants associated with a syndromic form of intellectual deficiency and autism
Functional characterization of DYRK1A missense variants associated with a syndromic form of intellectual deficiency and autism Open
Haploinsufficiency of DYRK1A is a cause of a neurodevelopmental syndrome termed mental retardation autosomal dominant 7 (MRD7). Several truncation mutations, microdeletions and missense variants have been identified and result in a recogni…
View article: Indole-3-Carbonitriles as DYRK1A Inhibitors by Fragment-Based Drug Design
Indole-3-Carbonitriles as DYRK1A Inhibitors by Fragment-Based Drug Design Open
Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) is a potential drug target because of its role in the development of Down syndrome and Alzheimer’s disease. The selective DYRK1A inhibitor 10-iodo-11H-indolo[3,2-c]quin…
View article: MOESM2 of Mutational analysis of two residues in the DYRK homology box of the protein kinase DYRK1A
MOESM2 of Mutational analysis of two residues in the DYRK homology box of the protein kinase DYRK1A Open
Additional file 2. Assay results underlying the column diagrams in table form.
View article: A wake‐up call to quiescent cancer cells – potential use of <scp>DYRK</scp>1B inhibitors in cancer therapy
A wake‐up call to quiescent cancer cells – potential use of <span>DYRK</span>1B inhibitors in cancer therapy Open
Nondividing cancer cells are relatively resistant to chemotherapeutic drugs and environmental stress factors. Promoting cell cycle re‐entry of quiescent cancer cells is a potential strategy to enhance the cytotoxicity of agents that target…
View article: DYRK1B mutations associated with metabolic syndrome impair the chaperone-dependent maturation of the kinase domain
DYRK1B mutations associated with metabolic syndrome impair the chaperone-dependent maturation of the kinase domain Open
View article: The adaptor protein DCAF7 mediates the interaction of the adenovirus E1A oncoprotein with the protein kinases DYRK1A and HIPK2
The adaptor protein DCAF7 mediates the interaction of the adenovirus E1A oncoprotein with the protein kinases DYRK1A and HIPK2 Open
View article: Selectivity Profiling and Biological Activity of Novel β-Carbolines as Potent and Selective DYRK1 Kinase Inhibitors
Selectivity Profiling and Biological Activity of Novel β-Carbolines as Potent and Selective DYRK1 Kinase Inhibitors Open
DYRK1A is a pleiotropic protein kinase with diverse functions in cellular regulation, including cell cycle control, neuronal differentiation, and synaptic transmission. Enhanced activity and overexpression of DYRK1A have been linked to alt…
View article: 10-Iodo-11<i>H</i>-indolo[3,2-<i>c</i>]quinoline-6-carboxylic Acids Are Selective Inhibitors of DYRK1A
10-Iodo-11<i>H</i>-indolo[3,2-<i>c</i>]quinoline-6-carboxylic Acids Are Selective Inhibitors of DYRK1A Open
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 assessment of the role of DYRK1A, selective synthetic inhib…
View article: Effect of tyrosine autophosphorylation on catalytic activity and subcellular localisation of homeodomain-interacting protein kinases (HIPK)
Effect of tyrosine autophosphorylation on catalytic activity and subcellular localisation of homeodomain-interacting protein kinases (HIPK) Open
These results show that HIPKs share the mechanism of activation by tyrosine autophosphorylation with the closely related DYRK family (dual-specificity tyrosine phosphorylation regulated kinase). However, members of the HIPK family differ r…
View article: CCDC 1036693: Experimental Crystal Structure Determination
CCDC 1036693: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Novel harmine analogues and the effect on dual specificity kinase activity of DYRK1A
Novel harmine analogues and the effect on dual specificity kinase activity of DYRK1A Open
Dual specificity tyrosine-(Y)-phosphorylation regulated kinase 1A (DYRK1A) is encoded on human chromosome 21 and triplication of this specific region leads to a 1.5-fold increased expression of DYRK1A in Down syndrome. Today there is a gro…