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Mode of Action of 5-Fluorocytosine and Mechanisms of Resistance
Abstract
Mode of action of 5-fluorocytosine (5-FC) and mechanisms of resistance to the drug are discussed on the basis of experiments performed with Candida albicans ATCC 26790 and with 50 selected clinical isolates of C. albicans belonging to serological type A or B and representing various degrees and models of 5-FC resistance (sensitivity). Incorporation of 5-fluorouridylic acid into RNA appeared as a prerequisite to antifungal activity, although at a given incorporation rate, growth inhibition varied considerably from one strain to the other. The amino acid pool was unbalanced, and there was evidence for disturbance of protein synthesis. These dysfunctions of RNA probably account for growth inhibition and cell death, whereas up to the present, there was no proof of formation of 5-fluorodeoxyuridylic acid nor of subsequent inhibition of thymidylate synthetase. Incorporation of fluorinated pyrimidine into RNA was lower in normally sensitive type B strains than in normally sensitive ones of type A, whereas the frequency of 5-FC-resistant mutants was the same. The two serological types did not differ in the activity of cytosine permease nor in that of cytosine deaminase. Among 29 clinical isolates with 5-FC resistance (or impaired sensitivity) no instance of cytosine permease deficiency was found. Two isolates (belonging to the serological type A) were deficient in cytosine deaminase, whereas the majority was probably deficient in uridine monophosphate pyrophosphorylase or had a surplus of de novo synthesis of pyrimidines. Relative 5-FC resistance was more common than complete resistance.
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“5-Flucytosine enters fungal cells via cytosine permease (Paluszynski et al. 2006) and is subsequently converted to 5-fluorouracil by cytosine deaminase (Polak and Scholer 1975) and then modified to 5-fluoro-UMP by phosphoribo-syltransferase.”
Pyrimidinones as biodynamic agents
Saxena, A. K., & Sinha, S. (1987) · Birkhäuser Basel eBooks · doi:10.1007/978-3-0348-9289-6_3 · Cited by 2
Somlai, C., Correché, E. R., Olivella, M. S., Tolosa, L., Lechón, M. J. G., Dombi, G., Tóth, G. K., Penke, B., & Enriz, R. D. (2012) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2012.05.045 · Cited by 2
Suivi thérapeutique des médicaments antifongiques
Blanchet, B., Huet, E., Astier, A., & Lesne-Hulin, A. (2004) · Revue Française des Laboratoires · doi:10.1016/s0338-9898(04)80204-x · Cited by 2
Metadata
- Authors
- Polak, A., & Scholer, H. J.
- Affiliations
- F. Hoffmann-La Roche AG (CH)
- ORCID
- Polak, Annemarie
- Venue
- Chemotherapy
- Publisher
- S. Karger AG
- Published
- 2009-05-25
- Volume
- 21
- Issue
- 3-4
- Pages
- 113-130
- ISSN
- 0009-3157 (ISSN-L)
- 1421-9794
- OpenAlex
- W2072785474
- Cited by
- 250
- References
- 0
- Citations by year
- 2026: 3 · 2025: 6 · 2024: 10 · 2023: 12 · 2022: 7 · 2021: 6 · 2020: 10 · 2019: 7 · 2018: 7 · 2017: 4 · 2016: 5 · 2015: 2 · 2014: 8 · 2013: 4 · 2012: 6
- FWCI
- 7.57
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Chemotherapy (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Infectious Diseases › Antifungal resistance and susceptibility
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Biochemical and Molecular Research
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Fungal and yeast genetics research
- Keywords
- 5-fluorocytosine, Candida albicans, antifungal resistance, mechanism of action, cytosine deaminase, protein synthesis inhibition, clinical isolates
- MeSH terms
- Candida albicans, Cell Division, Cytidine Deaminase, Cytosine, Drug Resistance, Microbial, Flucytosine, RNA, Serotyping, Uracil Nucleotides, Membrane Transport Proteins
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