ArticleBiochemistry2012
A peptide-based biosensor assay to detect intracellular Syk kinase activation and inhibition.
Article in Biochemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 27 citations in OpenAlex.
- Novel terbium-sensitizing peptide substrates for cyclin-dependent kinase 5 (CDK5) and their demonstration in luminescence kinase assays.RSC chemical biology · 2025Article
- An Acetyl-Click Chemistry Assay to Measure Histone Acetyltransferase 1 Acetylation.Journal of visualized experiments : JoVE · 2024Article
- Development of SYK NanoBRET cellular target engagement assays for gain-of-function variants.Frontiers in chemical biology · 2024Article
- Acetyl-Click Screening Platform Identifies Small-Molecule Inhibitors of Histone Acetyltransferase 1 (HAT1).Journal of medicinal chemistry · 2023Article
- Spleen Tyrosine Kinase-Mediated Autophagy Is Required for Epithelial-Mesenchymal Plasticity and Metastasis in Breast Cancer.Cancer research · 2019Article
- High-throughput Identification of FLT3 Wild-type and Mutant Kinase Substrate Preferences and Application to Design of SensitiveMolecular & cellular proteomics : MCP · 2019Article
- Assays for tyrosine phosphorylation in human cells.Methods in enzymology · 2019Article
- A Cell-Based Assay for Measuring Endogenous BcrAbl Kinase Activity and Inhibitor Resistance.PloS one · 2016Article
- Rapid Identification of Protein Kinase Phosphorylation Site Motifs Using Combinatorial Peptide Libraries.Methods in molecular biology (Clifton, N.J.) · 2016Article
- Multicolored, Tb³⁺-Based Antibody-Free Detection of Multiple Tyrosine Kinase Activities.Analytical chemistry · 2015Article
- KINATEST-ID: a pipeline to develop phosphorylation-dependent terbium sensitizing kinase assays.Journal of the American Chemical Society · 2015Article
- Global analysis of human nonreceptor tyrosine kinase specificity using high-density peptide microarrays.Journal of proteome research · 2014Article
- Fluorescence lifetime imaging of biosensor peptide phosphorylation in single live cells.Angewandte Chemie (International ed. in English) · 2013Article
- Time-resolved luminescence detection of spleen tyrosine kinase activity through terbium sensitization.Analytical chemistry · 2013Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
Spleen tyrosine kinase (Syk) has been implicated in a number of pathologies including cancer and rheumatoid arthritis and thus has been pursued as a novel therapeutic target. Because of the complex relationship between Syk's auto- and other internal phosphorylation sites, scaffolding proteins, enzymatic activation state and sites of phosphorylation on its known substrates, the role of Syk's activity in these diseases has not been completely clear. To approach such analyses, we developed a Syk-specific artificial peptide biosensor (SAStide) to use in a cell-based assay for direct detection of intracellular Syk activity and inhibition in response to physiologically relevant stimuli in both laboratory cell lines and primary splenic B cells. This peptide contains a sequence derived from known Syk substrate preference motifs linked to a cell permeable peptide, resulting in a biosensor that is phosphorylated in live cells in a Syk-dependent manner, thus serving as a reporter of Syk catalytic activity in intact cells. Because the assay is compatible with live, primary cells and can report pharmacodynamics for drug action on an intended target, this methodology could be used to facilitate a better understanding of Syk's function and the effect of its inhibition in disease.
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Registered trials
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.