ArticleMolecular omics2018
Kinome chemoproteomics characterization of pyrrolo[3,4-c]pyrazoles as potent and selective inhibitors of glycogen synthase kinase 3.
Article in Molecular omics, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 16 citations in OpenAlex.
- DYNO-MILL-Assisted Mechanochemistry: Design of Experiments Optimization for Sustainable Synthesis of Pyrrolo[3,4-c]pyrazoles.ChemSusChem · 2026Article
- MEK interactions tune RAF kinase sensitivity to conformation-selective inhibition.Nature chemical biology · 2026Article
- Proteomic approaches for interrogating kinase signaling networks.The Journal of investigative dermatology · 2026Article
- Synthesis, docking, SAR and ADMET evaluation of novel pyrrolo[3,4-c]pyrazole-4,6-dione derivatives.Scientific reports · 2026Article
- Multiplexed kinase interactome profiling quantifies cellular network activity and plasticity.Molecular cell · 2023Article
- ATP-competitive partial antagonists of the IRE1α RNase segregate outputs of the UPR.Nature chemical biology · 2021Article
- How ATP-Competitive Inhibitors Allosterically Modulate Tyrosine Kinases That Contain a Src-like Regulatory Architecture.ACS chemical biology · 2020Article
- Kinobead/LC-MS Phosphokinome Profiling Enables Rapid Analyses of Kinase-Dependent Cell Signaling Networks.Journal of proteome research · 2020Article
- Development of a Chemical Toolset for Studying the Paralog-Specific Function of IRE1.ACS chemical biology · 2019Article
- Targeting Dynamic ATP-Binding Site Features Allows Discrimination between Highly Homologous Protein Kinases.ACS chemical biology · 2019Article
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
Abstract
Glycogen synthase kinase 3 has evolutionarily conserved roles in cell signaling and metabolism and is a recognized drug target in neurological pathologies, most prominently bipolar disorder. More recently it has been suggested that GSK3 may be a target for the treatment of trypanosomatid parasite infections, e.g. with T. brucei, due to the lethal phenotype observed in parasite GSK3 short RNAi knockdown experiments. Here we investigated the kinome selectivity of a library of pyrrolo[3,4-c]pyrazol inhibitors that were developed against T. brucei GSK3 but that also interact with the human orthologue and other protein kinases. We applied label-free MS-based kinome chemoproteomics profiling with kinobeads to obtain the selectivity profiles of all 39 library members against 217 human protein and lipid kinases. This allowed us to study the structure-activity relationship of the library members as well as the chemical genetic relationships between kinase targets. As a result, we identified a novel and highly selective HsGSK3 inhibitor containing a 2-chloroaniline-substituted squaric acid amide pharmacophore that confers low nanomolar (IC
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.