ArticleAnalytical biochemistry2011
A rapid assay for assessment of sphingosine kinase inhibitors and substrates.
Article in Analytical biochemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 33 citations in OpenAlex.
- Assessment of Spinster homologue 2 (Spns2)-dependent transport of sphingosine-1-phosphate as a therapeutic target.British journal of pharmacology · 2025Article
- Probing the substitution pattern of indole-based scaffold reveals potent and selective sphingosine kinase 2 inhibitors.European journal of medicinal chemistry · 2021Article
- Lipophilic tail modifications of 2-(hydroxymethyl)pyrrolidine scaffold reveal dual sphingosine kinase 1 and 2 inhibitors.Bioorganic & medicinal chemistry · 2021Article
- A Novel Function of Sphingosine Kinase 2 in the Metabolism of Sphinga-4,14-Diene Lipids.Metabolites · 2020Article
- Discovery of a Small Side Cavity in Sphingosine Kinase 2 that Enhances Inhibitor Potency and Selectivity.Journal of medicinal chemistry · 2020Article
- Increasing circulating sphingosine-1-phosphate attenuates lung injury during ex vivo lung perfusion.The Journal of thoracic and cardiovascular surgery · 2018Article
- Saccharomyces cerevisiae as a platform for assessing sphingolipid lipid kinase inhibitors.PloS one · 2018Article
- Transforming Sphingosine Kinase 1 Inhibitors into Dual and Sphingosine Kinase 2 Selective Inhibitors: Design, Synthesis, and in Vivo Activity.Journal of medicinal chemistry · 2017Article
- Scintillation Proximity Assay to Detect the Changes in Cellular Dihydrosphingosine 1-Phosphate Levels.Lipids · 2016Article
- Structural Requirements and Docking Analysis of Amidine-Based Sphingosine Kinase 1 Inhibitors Containing Oxadiazoles.ACS medicinal chemistry letters · 2016Article
- Structure-Activity Relationship Studies and Molecular Modeling of Naphthalene-Based Sphingosine Kinase 2 Inhibitors.ACS medicinal chemistry letters · 2016Article
- A real-time high-throughput fluorescence assay for sphingosine kinases.Journal of lipid research · 2014Article
- Targeting sphingosine kinase 1 attenuates bleomycin-induced pulmonary fibrosis.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2013Article
- Targeting the sphingosine kinase/sphingosine 1-phosphate pathway in disease: review of sphingosine kinase inhibitors.Biochimica et biophysica acta · 2013Review
- Effect of alkyl chain length on sphingosine kinase 2 selectivity.Bioorganic & medicinal chemistry letters · 2012Article
- Sphingosine kinase type 2 inhibition elevates circulating sphingosine 1-phosphate.The Biochemical journal · 2012Article
- Design, synthesis and biological activity of sphingosine kinase 2 selective inhibitors.Bioorganic & medicinal chemistry · 2012Article
- Sphingosine kinase type 1 inhibition reveals rapid turnover of circulating sphingosine 1-phosphate.The Biochemical journal · 2011Article
- Development of amidine-based sphingosine kinase 1 nanomolar inhibitors and reduction of sphingosine 1-phosphate in human leukemia cells.Journal of medicinal chemistry · 2011Article
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Authors and funding
6 authors at 1 institution in 1 country.
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Abstract
Sphingosine kinases (SphKs) catalyze the transfer of phosphate from adenosine triphosphate (ATP) to sphingosine to generate sphingosine 1-phosphate (S1P), an important bioactive lipid molecule that mediates a diverse range of cell signaling processes. The conventional assay of SphK enzymatic activity uses [γ-(32)P]ATP and sphingosine as substrates, with the radiolabeled S1P product recovered by organic extraction, displayed by thin layer chromatography, and quantified by liquid scintillation counting. Although this assay is sensitive and accurate, it is slow and labor-intensive; thus, it precludes the simultaneous screening of more than a few inhibitor compounds. Here we describe a 96-well assay for SphKs that is rapid and reproducible. Our method, which takes advantage of the limited solubility of S1P, detects radioactive S1P adhering to the plate by scintillation proximity counting. Our procedure obviates extraction into organic solvents, postreaction transfers, and chromatography. Furthermore, our assay enables assessment of both inhibitors and substrates, and it can detect endogenous SphK activity in cell and tissue extracts. The SphK kinetic parameter, K(m), and the K(i) values of inhibitors determined with our assay and the conventional assay were indistinguishable. These results document that our assay is well-suited for the screening of chemical libraries of SphK inhibitors.
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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.