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dc.contributor.authorKharel, Yugeshen
dc.contributor.authorAgah, Sayehen
dc.contributor.authorHuang, Taoen
dc.contributor.authorMendelson, Anna J.en
dc.contributor.authorEletu, Oluwafunmilayo T.en
dc.contributor.authorBarkey-Bircannl, Peteren
dc.contributor.authorGesualdil, Jamesen
dc.contributor.authorSmith, Jeffrey S.en
dc.contributor.authorSantos, Webster L.en
dc.contributor.authorLynch, Kevin R.en
dc.description.abstractSuccessful medicinal chemistry campaigns to discover and optimize sphingosine kinase inhibitors require a robust assay for screening chemical libraries and for determining rank order potencies. Existing assays for these enzymes are laborious, expensive and/or low throughput. The toxicity of excessive levels of phosphorylated sphingoid bases for the budding yeast, Saccharomyces cerevisiae, affords an assay wherein inhibitors added to the culture media rescue growth in a dose-dependent fashion. Herein, we describe our adaptation of a simple, inexpensive, and high throughput assay for assessing inhibitors of sphingosine kinase types 1 and 2 as well as ceramide kinase and for testing enzymatic activity of sphingosine kinase type 2 mutants. The assay was validated using recombinant enzymes and generally agrees with the rank order of potencies of existing inhibitors.en
dc.description.sponsorshipNIH/NIGMS [R01 GM104366, R01 GM121075]; NIH [R01 GM075240]; NIGMS; University of Virginia Summer Research Internship Program fellowshipsen
dc.rightsCreative Commons Attribution 4.0 Internationalen
dc.titleSaccharomyces cerevisiae as a platform for assessing sphingolipid lipid kinase inhibitorsen
dc.typeArticle - Refereeden
dc.description.notesThis work was supported by NIH/NIGMS R01 GM104366 & NIH/NIGMS R01 GM121075 to KRL & WLS, NIH R01 GM075240 to JSS, NIGMS:; University of Virginia Summer Research Internship Program fellowships to JG and PBB The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.en
dc.title.serialPLOS ONEen

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Creative Commons Attribution 4.0 International
License: Creative Commons Attribution 4.0 International