D. H. Drewry

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.

SGC-CAMKK2-1: A chemical probe for CAMKK2

This paper introduces SGC-CAMKK2-1, a selective chemical probe for CAMKK2, demonstrating its potential as a tool to study the therapeutic benefits of CAMKK2 inhibition.

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.

An open source plant kinase chemogenomics set

The paper presents a plant kinase chemogenomics set, identifying compounds that affect root development in Arabidopsis and rice, with implications for understanding plant kinase function.

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.

Temozolomide-induced guanine mutations create exploitable vulnerabilities of guanine-rich DNA and RNA regions in drug resistant gliomas

This study identifies guanine mutations in TMZ-resistant gliomas that disrupt G4 structures and splice sites, creating vulnerabilities targeted by G4 stabilizers and splicing inhibitors.

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.

Identification and Optimization of cell active 4-anilino-quin(az)oline Inhibitors for Protein Kinase Novel 3 (PKN3)

The paper identifies 7-iodo-N-(3,4,5-trimethoxyphenyl)quinolin-4-amine as a potent PKN3 inhibitor with an IC50 of 1.3 μM in cells, suggesting its potential as a tool for studying PKN3 biology and therapeutic applications.

In depth analysis of kinase cross screening data to identify CAMKK2 inhibitory scaffolds

This paper reviews CAMKK2's role in biology and disease, identifies starting points for inhibitor development using literature and databases, and highlights potential for selective inhibitors in oncology, metabolism, and inflammation.

Crowdsourced mapping of unexplored target space of kinase inhibitors

The paper benchmarks predictive models for kinase inhibitor potencies using crowdsourced data and identifies new compound-kinase interactions.

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.

Structural and binding studies of human CAMKK2 kinase domain bound to small molecule ligands

This study presents six novel co-structures of CAMKK2 bound to small molecule ligands and shows some ligand binding is enthalpy driven.

Cyclin F-Chk1 synthetic lethality mediated by E2F1 degradation

The paper identifies synthetic lethality between Chk1 inhibition and cyclin F loss, revealing Cyclin F's role in preventing DNA replication stress via E2F1 degradation.

Design of a GAK/EGFR inhibitor set to interrogate the relationship of EGFR and GAK in chordoma

The paper designs a set of GAK/EGFR inhibitors to study their relationship in chordoma and characterizes their activity in vitro and through target engagement assays.

In depth analysis of kinase cross screening data to identify chemical starting points for inhibition of the Nek family of kinases

The paper analyzes kinase cross-screening data to identify potential chemical starting points for inhibiting Nek kinases, aiming to advance drug discovery for these understudied targets.

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.