ArticleJournal of the American Chemical Society2008
Recognition-domain focused chemosensors: versatile and efficient reporters of protein kinase activity.
Article in Journal of the American Chemical Society, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 47 papers.
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Who cites it
47 citing papers in PubMed, 113 citations in OpenAlex.
- Let the peptides shine: SOX (Sulfonamido-OXine)-labelled peptides for direct kinase and phosphatase monitoring.RSC chemical biology · 2026Review
- A Constellation of Fluorescent Biosensors to Illuminate the Galaxy of Protein Kinases.Chembiochem : a European journal of chemical biology · 2026Review
- The role of kinase domain dimerization in EGFR activation.Structure (London, England : 1993) · 2026Article
- STX-721, a Covalent EGFR/HER2 Exon 20 Inhibitor, Utilizes Exon 20-Mutant Dynamic Protein States and Achieves Unique Mutant Selectivity Across Human Cancer Models.Clinical cancer research : an official journal of the American Association for Cancer Research · 2025Article
- A "Ligand First" Approach toward Selective, Covalent JNK2/3 Inhibitors.Journal of medicinal chemistry · 2025Article
- New pyrano-pyridine conjugates as potential anticancer agents: design, synthesis and computational studies.Future medicinal chemistry · 2024Article
- Steady State and Time-Dependent Fluorescent Peptide Assays for Protein Kinases.Current protocols · 2024Article
- Evaluation of STK17B as a cancer immunotherapy target utilizing highly potent and selective small molecule inhibitors.Frontiers in immunology · 2024Article
- Circulating tumor DNA reveals mechanisms of lorlatinib resistance in patients with relapsed/refractory ALK-driven neuroblastoma.Nature communications · 2023Article
- Design, synthesis, and anti-cancer evaluation of new pyrido[2,3-d]pyrimidin-4(3H)-one derivatives as potential EGFRWT and EGFRT790M inhibitors and apoptosis inducers.Journal of enzyme inhibition and medicinal chemistry · 2022Article
- Biochemical and structural basis for differential inhibitor sensitivity of EGFR with distinct exon 19 mutations.Nature communications · 2022Article
- AktAR and Akt-STOPS: Genetically Encodable Molecular Tools to Visualize and Perturb Akt Kinase Activity at Different Subcellular Locations in Living Cells.Current protocols · 2022Article
- Shining Light on Protein Kinase Biomarkers with Fluorescent Peptide Biosensors.Life (Basel, Switzerland) · 2022Review
- A novel GSK-3 inhibitor binds to GSK-3β via a reversible, time and Cys-199-dependent mechanism.Bioorganic & medicinal chemistry · 2021Article
- Versatile small molecule kinase assay through real-time, ratiometric fluorescence changes based on a pyrene-DPA-ZnRSC advances · 2021Article
- Fluorescent Peptide Biosensors for Probing CDK Kinase Activity in Cell Extracts.Methods in molecular biology (Clifton, N.J.) · 2021Article
- A fluorescent probe for monitoring PTP-PEST enzymatic activity.The Analyst · 2020Article
- Fluorogenic probes for imaging cellular phosphatase activity.Current opinion in chemical biology · 2020Review
- A Panel of Protein Kinase Chemosensors Distinguishes Different Types of Fatty Liver Disease.Biochemistry · 2019Article
- Safety profiling of genetically engineered Pim-1 kinase overexpression for oncogenicity risk in human c-kit+ cardiac interstitial cells.Gene therapy · 2019Article
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
Catalyzed by kinases, serine/threonine and tyrosine phosphorylation is a vital mechanism of intracellular regulation. Thus, assays that easily monitor kinase activity are critical in both academic and pharmaceutical settings. We previously developed sulfonamido-oxine (Sox)-based fluorescent peptides following a beta-turn focused (BTF) design for the continuous assay of kinase activity in vitro and in cell lysates. Upon phosphorylation of the Sox-containing peptide, the chromophore binds Mg (2+) and undergoes chelation-enhanced fluorescence (CHEF). Although the design was applied successfully to the development of several kinase sensors, an intrinsic limitation was that only residues C- or N-terminal to the phosphorylated residue could be used to derive specificity for the target kinase. To address this limitation, a new, recognition-domain focused (RDF) strategy was developed that also relies on CHEF. In this approach, the requirement for the constrained beta-turn motif is obviated by alkylation of a cysteine residue with a Sox-based derivative to afford an amino acid termed C-Sox. The RDF design allows inclusion of extended binding determinants to maximize recognition by the cognate kinase, which has now permitted the construction of chemosensors for a variety of representative Ser/Thr (PKC alpha, PKC betaIota, PKC delta, Pim2, Akt1, MK2, and PKA) as well as receptor (IRK) and nonreceptor (Src, Abl) Tyr kinases with greatly enhanced selectivity. The new sensors have up to 28-fold improved catalytic efficiency and up to 66-fold lower K M when compared to the corresponding BTF probes. The improved generality of the strategy is exemplified with the synthesis and analysis of Sox-based probes for PKC betaIota and PKC delta, which were previously unattainable using the BTF approach.
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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.