Screening assay for inhibitors of a recombinant Streptococcus pneumoniae UDP-glucose pyrophosphorylase

The UDP-glucose pyrophosphorylase of Streptococcus pneumoniae (GalU(Spn)) is absolutely required for the biosynthesis of capsular polysaccharide, the sine qua non virulence factor of pneumococcus. Since the eukaryotic enzymes are completely unrelated to their prokaryotic counterparts, we propose tha...

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Autores principales: Zavala, Agustín, Kovacec, Verónica, Levín, Gustavo, Moglioni, Albertina, Miranda, María Victoria, García, Ernesto, Bonofiglio, Laura, Mollerach, Marta
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2017
Materias:
Short Communication
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6009895/
https://www.ncbi.nlm.nih.gov/pubmed/28114831
http://dx.doi.org/10.1080/14756366.2016.1247055
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author Zavala, Agustín
Kovacec, Verónica
Levín, Gustavo
Moglioni, Albertina
Miranda, María Victoria
García, Ernesto
Bonofiglio, Laura
Mollerach, Marta
author_facet Zavala, Agustín
Kovacec, Verónica
Levín, Gustavo
Moglioni, Albertina
Miranda, María Victoria
García, Ernesto
Bonofiglio, Laura
Mollerach, Marta
author_sort Zavala, Agustín
collection PubMed
description The UDP-glucose pyrophosphorylase of Streptococcus pneumoniae (GalU(Spn)) is absolutely required for the biosynthesis of capsular polysaccharide, the sine qua non virulence factor of pneumococcus. Since the eukaryotic enzymes are completely unrelated to their prokaryotic counterparts, we propose that the GalU enzyme is a critical target to fight the pneumococcal disease. A recombinant GalU(Spn) was overexpressed and purified. An enzymatic assay that is rapid, sensitive and easy to perform was developed. This assay was appropriate for screening chemical libraries for searching GalU inhibitors. This work represents a fundamental step in the exploration of novel antipneumococcal drugs.
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spelling pubmed-60098952018-07-11 Screening assay for inhibitors of a recombinant Streptococcus pneumoniae UDP-glucose pyrophosphorylase Zavala, Agustín Kovacec, Verónica Levín, Gustavo Moglioni, Albertina Miranda, María Victoria García, Ernesto Bonofiglio, Laura Mollerach, Marta J Enzyme Inhib Med Chem Short Communication The UDP-glucose pyrophosphorylase of Streptococcus pneumoniae (GalU(Spn)) is absolutely required for the biosynthesis of capsular polysaccharide, the sine qua non virulence factor of pneumococcus. Since the eukaryotic enzymes are completely unrelated to their prokaryotic counterparts, we propose that the GalU enzyme is a critical target to fight the pneumococcal disease. A recombinant GalU(Spn) was overexpressed and purified. An enzymatic assay that is rapid, sensitive and easy to perform was developed. This assay was appropriate for screening chemical libraries for searching GalU inhibitors. This work represents a fundamental step in the exploration of novel antipneumococcal drugs. Taylor & Francis 2017-01-23 /pmc/articles/PMC6009895/ /pubmed/28114831 http://dx.doi.org/10.1080/14756366.2016.1247055 Text en © 2017 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group http://creativecommons.org/Licenses/by/4.0/ This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/Licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Short Communication
Zavala, Agustín
Kovacec, Verónica
Levín, Gustavo
Moglioni, Albertina
Miranda, María Victoria
García, Ernesto
Bonofiglio, Laura
Mollerach, Marta
Screening assay for inhibitors of a recombinant Streptococcus pneumoniae UDP-glucose pyrophosphorylase
title Screening assay for inhibitors of a recombinant Streptococcus pneumoniae UDP-glucose pyrophosphorylase
title_full Screening assay for inhibitors of a recombinant Streptococcus pneumoniae UDP-glucose pyrophosphorylase
title_fullStr Screening assay for inhibitors of a recombinant Streptococcus pneumoniae UDP-glucose pyrophosphorylase
title_full_unstemmed Screening assay for inhibitors of a recombinant Streptococcus pneumoniae UDP-glucose pyrophosphorylase
title_short Screening assay for inhibitors of a recombinant Streptococcus pneumoniae UDP-glucose pyrophosphorylase
title_sort screening assay for inhibitors of a recombinant streptococcus pneumoniae udp-glucose pyrophosphorylase
topic Short Communication
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6009895/
https://www.ncbi.nlm.nih.gov/pubmed/28114831
http://dx.doi.org/10.1080/14756366.2016.1247055
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