ArticleChemMedChem2016
Alkylation of Staurosporine to Derive a Kinase Probe for Fluorescence Applications.
Article in ChemMedChem, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
7 citing papers in PubMed, 15 citations in OpenAlex.
- A cell-impermeable kinase inhibitor uncovers outside-in signaling pathways that promote HIV-1 infection.Journal of virology · 2026Article
- Reflectometric-based sensor arrays for the screening of kinase-inhibitor interactions and kinetic determination.Analytical and bioanalytical chemistry · 2025Article
- Glypican-1 upregulation elicited in response to a cell-impermeable kinase inhibitor and its overexpression enhance HIV-1 infection.bioRxiv : the preprint server for biology · 2025Article
- A multicomponent reaction for modular assembly of indole-fused heterocycles.Chemical science · 2024Article
- Natural-product-based fluorescent probes: recent advances and applications.RSC medicinal chemistry · 2023Review
- Article
- Alkylation of Staurosporine to Derive a Kinase Probe for Fluorescence Applications.ChemMedChem · 2016Article
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The natural product staurosporine is a high-affinity inhibitor of nearly all mammalian protein kinases. The labelling of staurosporine has proven effective as a means of generating protein kinase research tools. Most tools have been generated by acylation of the 4'-methylamine of the sugar moiety of staurosporine. Herein we describe the alkylation of this group as a first step to generate a fluorescently labelled staurosporine. Following alkylation, a polyethylene glycol linker was installed, allowing subsequent attachment of fluorescein. We report that this fluorescein-staurosporine conjugate binds to cAMP-dependent protein kinase in the nanomolar range. Furthermore, its binding can be antagonised with unmodified staurosporine as well as ATP, indicating it targets the ATP binding site in a similar fashion to native staurosporine. This reagent has potential application as a screening tool for protein kinases of interest.
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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.