Cargando…

Characterisation of the Candida albicans Phosphopantetheinyl Transferase Ppt2 as a Potential Antifungal Drug Target

Antifungal drugs acting via new mechanisms of action are urgently needed to combat the increasing numbers of severe fungal infections caused by pathogens such as Candida albicans. The phosphopantetheinyl transferase of Aspergillus fumigatus, encoded by the essential gene pptB, has previously been id...

Descripción completa

Detalles Bibliográficos
Autores principales: Dobb, Katharine S., Kaye, Sarah J., Beckmann, Nicola, Thain, John L., Stateva, Lubomira, Birch, Mike, Oliver, Jason D.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Public Library of Science 2015
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4659657/
https://www.ncbi.nlm.nih.gov/pubmed/26606674
http://dx.doi.org/10.1371/journal.pone.0143770
_version_ 1782402660491591680
author Dobb, Katharine S.
Kaye, Sarah J.
Beckmann, Nicola
Thain, John L.
Stateva, Lubomira
Birch, Mike
Oliver, Jason D.
author_facet Dobb, Katharine S.
Kaye, Sarah J.
Beckmann, Nicola
Thain, John L.
Stateva, Lubomira
Birch, Mike
Oliver, Jason D.
author_sort Dobb, Katharine S.
collection PubMed
description Antifungal drugs acting via new mechanisms of action are urgently needed to combat the increasing numbers of severe fungal infections caused by pathogens such as Candida albicans. The phosphopantetheinyl transferase of Aspergillus fumigatus, encoded by the essential gene pptB, has previously been identified as a potential antifungal target. This study investigated the function of its orthologue in C. albicans, PPT2/C1_09480W by placing one allele under the control of the regulatable MET3 promoter, and deleting the remaining allele. The phenotypes of this conditional null mutant showed that, as in A. fumigatus, the gene PPT2 is essential for growth in C. albicans, thus fulfilling one aspect of an efficient antifungal target. The catalytic activity of Ppt2 as a phosphopantetheinyl transferase and the acyl carrier protein Acp1 as a substrate were demonstrated in a fluorescence transfer assay, using recombinant Ppt2 and Acp1 produced and purified from E.coli. A fluorescence polarisation assay amenable to high-throughput screening was also developed. Therefore we have identified Ppt2 as a broad-spectrum novel antifungal target and developed tools to identify inhibitors as potentially new antifungal compounds.
format Online
Article
Text
id pubmed-4659657
institution National Center for Biotechnology Information
language English
publishDate 2015
publisher Public Library of Science
record_format MEDLINE/PubMed
spelling pubmed-46596572015-12-02 Characterisation of the Candida albicans Phosphopantetheinyl Transferase Ppt2 as a Potential Antifungal Drug Target Dobb, Katharine S. Kaye, Sarah J. Beckmann, Nicola Thain, John L. Stateva, Lubomira Birch, Mike Oliver, Jason D. PLoS One Research Article Antifungal drugs acting via new mechanisms of action are urgently needed to combat the increasing numbers of severe fungal infections caused by pathogens such as Candida albicans. The phosphopantetheinyl transferase of Aspergillus fumigatus, encoded by the essential gene pptB, has previously been identified as a potential antifungal target. This study investigated the function of its orthologue in C. albicans, PPT2/C1_09480W by placing one allele under the control of the regulatable MET3 promoter, and deleting the remaining allele. The phenotypes of this conditional null mutant showed that, as in A. fumigatus, the gene PPT2 is essential for growth in C. albicans, thus fulfilling one aspect of an efficient antifungal target. The catalytic activity of Ppt2 as a phosphopantetheinyl transferase and the acyl carrier protein Acp1 as a substrate were demonstrated in a fluorescence transfer assay, using recombinant Ppt2 and Acp1 produced and purified from E.coli. A fluorescence polarisation assay amenable to high-throughput screening was also developed. Therefore we have identified Ppt2 as a broad-spectrum novel antifungal target and developed tools to identify inhibitors as potentially new antifungal compounds. Public Library of Science 2015-11-25 /pmc/articles/PMC4659657/ /pubmed/26606674 http://dx.doi.org/10.1371/journal.pone.0143770 Text en © 2015 Dobb et al http://creativecommons.org/licenses/by/4.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are properly credited.
spellingShingle Research Article
Dobb, Katharine S.
Kaye, Sarah J.
Beckmann, Nicola
Thain, John L.
Stateva, Lubomira
Birch, Mike
Oliver, Jason D.
Characterisation of the Candida albicans Phosphopantetheinyl Transferase Ppt2 as a Potential Antifungal Drug Target
title Characterisation of the Candida albicans Phosphopantetheinyl Transferase Ppt2 as a Potential Antifungal Drug Target
title_full Characterisation of the Candida albicans Phosphopantetheinyl Transferase Ppt2 as a Potential Antifungal Drug Target
title_fullStr Characterisation of the Candida albicans Phosphopantetheinyl Transferase Ppt2 as a Potential Antifungal Drug Target
title_full_unstemmed Characterisation of the Candida albicans Phosphopantetheinyl Transferase Ppt2 as a Potential Antifungal Drug Target
title_short Characterisation of the Candida albicans Phosphopantetheinyl Transferase Ppt2 as a Potential Antifungal Drug Target
title_sort characterisation of the candida albicans phosphopantetheinyl transferase ppt2 as a potential antifungal drug target
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4659657/
https://www.ncbi.nlm.nih.gov/pubmed/26606674
http://dx.doi.org/10.1371/journal.pone.0143770
work_keys_str_mv AT dobbkatharines characterisationofthecandidaalbicansphosphopantetheinyltransferaseppt2asapotentialantifungaldrugtarget
AT kayesarahj characterisationofthecandidaalbicansphosphopantetheinyltransferaseppt2asapotentialantifungaldrugtarget
AT beckmannnicola characterisationofthecandidaalbicansphosphopantetheinyltransferaseppt2asapotentialantifungaldrugtarget
AT thainjohnl characterisationofthecandidaalbicansphosphopantetheinyltransferaseppt2asapotentialantifungaldrugtarget
AT statevalubomira characterisationofthecandidaalbicansphosphopantetheinyltransferaseppt2asapotentialantifungaldrugtarget
AT birchmike characterisationofthecandidaalbicansphosphopantetheinyltransferaseppt2asapotentialantifungaldrugtarget
AT oliverjasond characterisationofthecandidaalbicansphosphopantetheinyltransferaseppt2asapotentialantifungaldrugtarget