A. D. Axtman

Discovery and Characterization of a Chemical Probe for Cyclin-Dependent Kinase-Like 2

The paper identifies and characterizes a chemical probe for CDKL2, demonstrating its selectivity and biological impact in neurons and cancer cells.

Synthesis of 5-Benzylamino and 5-Alkylamino-substituted Pyrimidoquinoline Derivatives as CSNK2A Inhibitors with Antiviral Activity

The paper synthesizes pyrimidoquinoline derivatives as CSNK2A inhibitors with antiviral activity, finding that certain substituents improve potency while maintaining solubility.

Discovery and Optimization of Narrow Spectrum Inhibitors of Tousled Like Kinase 2 (TLK2) Using Quantitative Structure Activity Relationships

The paper identifies and optimizes narrow-spectrum TLK2 inhibitors using QSAR analysis and structural studies.

Optimization of 3-Cyano-7-cyclopropylamino-pyrazolopyrimidines Toward the Development of an In Vivo Chemical Probe for CSNK2

The paper develops analogs of SGC-CK2-1 to improve pharmacokinetic properties in mice by inhibiting GST and P450 enzymes through co-dosing protocols.

A Potent and Selective CDKL5/GSK3 Chemical Probe is Neuroprotective

The paper develops a potent and selective CDKL5/GSK3 chemical probe and demonstrates its neuroprotective effects in human motor neurons under ER stress.

Identification of a chemical probe for lipid kinase phosphatidylinositol-5-phosphate 4-kinase gamma (PI5P4Kγ)

This paper identifies a chemical probe for PI5P4Kγ, demonstrating its selectivity and cellular activity, and shows it activates mTORC1 signaling in breast cancer cells.

Modulation of Tau Tubulin Kinases (TTBK1 and TTBK2) Impacts Ciliogenesis

The paper identifies chemical tools that inhibit TTBK1 and TTBK2, showing that TTBK2 inhibition reduces ciliogenesis in iPSCs.

Host kinase CSNK2 is a target for inhibition of pathogenic β-coronaviruses including SARS-CoV-2

The paper shows that inhibiting the kinase CSNK2 blocks replication of several beta-coronaviruses, including SARS-CoV-2, by preventing viral entry.

Protein proximity networks and functional evaluation of the Casein Kinase 1 γ family reveals unique roles for CK1γ3 in WNT signaling

This study identifies unique roles for CK1γ3 in WNT signaling through proximity biotinylation, functional assays, and inhibitor testing, showing its distinct activation of β-catenin and Notch pathways.

PKIS Deep Dive Yields a Chemical Starting Point for Dark Kinases and a Cell Active BRSK2 Inhibitor

The paper investigates GW296115, a PKIS compound, showing it inhibits six dark kinases, including BRSK2, with IC50 values under 100nM and demonstrates cell activity.

The Kinase Chemogenomic Set (KCGS): An open science resource for kinase vulnerability identification

The paper introduces the Kinase Chemogenomic Set (KCGS), a curated collection of 187 selective kinase inhibitors covering 215 human kinases, for use in cell-based screens.

Substrate binding allosterically relieves autoinhibition of the TRIB1 pseudokinase

The paper shows that substrate binding to TRIB1 pseudokinase induces allosteric changes enabling complex formation with COP1 ubiquitin ligase.

Progress Towards a Public Chemogenomic Set for Protein Kinases and a Call for Contributions

The paper shares progress on a kinase chemogenomic set, releases inhibitor profiling data, and calls for community collaboration to complete the set.