Spermine-NBD as fluorescent probe for studies of the polyamine transport system in Leishmania donovani

Spermine-NBD as fluorescent probe for studies of the polyamine transport system in Leishmania donovani

[Display omitted] This study describes the synthesis of fluorescent probes as potential substrates for the polyamine transport system (PTS) of Leishmania donovani. A competitive radioassay was used to determine the most efficient probe. We observed that the conjugate spermine-nitrobenzofurazan (Spm-...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters Vol. 29; no. 14; pp. 1710 - 1713
Main Authors: Jagu, Elodie, Pomel, Sébastien, Pethe, Stéphanie, Cintrat, Jean-Christophe, Loiseau, Philippe M., Labruère, Raphaël
Format: Journal Article
Language:English
Published: England Elsevier Ltd 15-07-2019
Elsevier
Subjects:
Chemical Sciences
Fluorescence
Leishmania donovani
Polyamine transport
Radioisotopic method
Fluorescence
Polyamine transport
Leishmania donovani
Radioisotopic method
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Summary:[Display omitted] This study describes the synthesis of fluorescent probes as potential substrates for the polyamine transport system (PTS) of Leishmania donovani. A competitive radioassay was used to determine the most efficient probe. We observed that the conjugate spermine-nitrobenzofurazan (Spm-NBD) was able to compete with [3H]-spermidine in L. donovani at a potent IC50 of 60 µM.
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ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2019.05.030