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Título

Synthesis of a Novel Ceramide Analogue and its Use in a High-Throughput Fluorogenic Assay for Ceramidases

AutorBedia Girbés, Carmen; Casas Brugulat, Josefina; Garcia, Virginie; Levade, Thierry; Fabriàs, Gemma
Palabras claveAcidic ceramidase
Amides
Enzymes
Fluorescence
Inhibitors
Fecha de publicación16-mar-2007
EditorJohn Wiley & Sons
CitaciónChembiochem 8(6): 642-648 (2007)
ResumenSeveral investigations have shown that acid ceramidase inhibitors are potential antiproliferative and cytostatic drugs for cancer chemotherapy. The combinatorial chemistry approach for the discovery of acid ceramidase inhibitors requires the availability of a high-throughput enzyme assay. The synthesis of a novel fluorogenic ceramidase substrate, and its processing both in vitro and in cultured cells in a microtiter plate layout, are reported in this article. This coumarinic substrate was hydrolyzed in vitro (rat liver lysosomes) with Km and Vmax values of 113 μm and 3.6 pmol min-1 mg-1, respectively. Similarly, hydrolysis occurred in intact cultured cells that overexpressed acidic ceramidase. The assay was validated for the identification and characterization of acidic ceramidase inhibitors by using several α-ketoamide ceramide analogues, whose inhibitory activity had been previously described.
Descripción7 pages, 3 figures.-- PMID: 17361980 [PubMed].
Versión del editorhttp://dx.doi.org/10.1002/cbic.200600533
URIhttp://hdl.handle.net/10261/9267
DOI10.1002/cbic.200600533
ISSN1439-7633
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