Characterisation of the Candida albicans Phosphopantetheinyl Transferase Ppt2 as a Potential Antifungal Drug Target
نویسندگان
چکیده
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.
منابع مشابه
A 4'-phosphopantetheinyl transferase mediates non-ribosomal peptide synthetase activation in Aspergillus fumigatus.
Aspergillus fumigatus is a significant human pathogen. Non-ribosomal peptide (NRP) synthesis is thought to be responsible for a significant proportion of toxin and siderophore production in the organism. Furthermore, it has been shown that 4'-phosphopantetheinylation is required for the activation of key enzymes involved in non-ribosomal peptide synthesis in other species. Here we report the cl...
متن کاملStudy of Antifungal Synergism Effects of Chitosan with Thymol, Carvacrol and Isothiocyanate against Candida albicans
Background and Aim: Prevalence of drug resistance in Candida albicans hinders common treatments with conventional antifungal drugs. A stockpile of research is being done to discover novel antifungal drugs. Chitosan has emerged as a promising antimicrobial and biodegradable polymer with various medical applications. The significant antimicrobial potential of some of the secondary metabolites fro...
متن کاملAntifungal Screening of Bridelia ferruginea Benth (Euphorbiaceae) Stem Bark Extract in Mouthwash Formulations
The plant Bridelia ferruginea Benth (Euphorbiaceae) has been known for its use in the management of oral thrush ethnomedicinally in various parts of Africa, a practice which has been justified by results of certain scientific studies. The aim of this study was to develop an appropriate dosage formulation, a mouthwash and evaluate the antifungal potential of this dosage formulation against a maj...
متن کاملInvestigation of the Antifungal Effect of Rosa Damascena Essential Oil and Mixed Mouthwash (Grape Vinegar and Rosa Damascena essential oil) Against Candida albicans, Candida dubliniensis, Candida parapsilosis and Candida glabrata
Background and Objective: Oral candidiasis is often caused by Candida albicans, followed by C. dubliniensis, C. parapsilosis, and C. glabrata. The present study aimed to investigate the antifungal effects of Rosa damascena (R. damascena) essential oil, mixed mouthwash of R. damascena essential oil and grape vinegar, as well as nystatin against various standard Candida species. Materials and Me...
متن کاملEffects of depleting the essential central metabolic enzyme fructose-1,6-bisphosphate aldolase on the growth and viability of Candida albicans: implications for antifungal drug target discovery.
The central metabolic enzyme fructose-1,6-bisphosphate aldolase (Fba1p) catalyzes a reversible reaction required for both glycolysis and gluconeogenesis. Fba1p is a potential antifungal target because it is essential in yeast and because fungal and human aldolases differ significantly. To test the validity of Fba1p as an antifungal target, we have examined the effects of depleting this enzyme i...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
عنوان ژورنال:
دوره 10 شماره
صفحات -
تاریخ انتشار 2015