The DOI matches its Crossref record; 42 of the 42 references it cites were found in a registry or an index.
Discovery of Novel Antifungal (1,3)-β- d -Glucan Synthase Inhibitors
Open accessAbstract
The increasing incidence of life-threatening fungal infections has driven the search for new, broad-spectrum fungicidal agents that can be used for treatment and prophylaxis in immunocompromised patients. Natural-product inhibitors of cell wall (1,3)-β- d -glucan synthase such as lipopeptide pneumocandins and echinocandins as well as the glycolipid papulacandins have been evaluated as potential therapeutics for the last two decades. As a result, MK-0991 (caspofungin acetate; Cancidas), a semisynthetic analogue of pneumocandin B o , is being developed as a broad-spectrum parenteral agent for the treatment of aspergillosis and candidiasis. This and other lipopeptide antifungal agents have limited oral bioavailability. Thus, we have sought new chemical structures with the mode of action of lipopeptide antifungal agents but with the potential for oral absorption. Results of natural-product screening by a series of newly developed methods has led to the identification of four acidic terpenoid (1,3)-β- d -glucan synthase inhibitors. Of the four compounds, the in vitro antifungal activity of one, enfumafungin, is comparable to that of L-733560, a close analogue of MK-0991. Like the lipopeptides, enfumafungin specifically inhibits glucan synthesis in whole cells and in (1,3)-β- d -glucan synthase assays, alters the morphologies of yeasts and molds, and produces a unique response in Saccharomyces cerevisiae strains with point mutations in FKS1 , the gene which encodes the large subunit of glucan synthase.
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The global problem of antifungal resistance: prevalence, mechanisms, and management
Perlin, D. S., Rautemaa-Richardson, R., & Alastruey-Izquierdo, A. (2017) · The Lancet Infectious Diseases · doi:10.1016/s1473-3099(17)30316-x · Cited by 1,055
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Antifungal Drug Development: Challenges, Unmet Clinical Needs, and New Approaches
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Campoy, S., & Adrio, J. L. (2017) · Biochemical Pharmacology · doi:10.1016/j.bcp.2016.11.019 · Cited by 511
Metadata
- Authors
- Onishi, J., Meinz, M., Thompson, J., Curotto, J., Dreikorn, S., Rosenbach, M., Douglas, C., Abruzzo, G., Flattery, A., Kong, L., Cabello, A., Vicente, F., Pelaez, F., Diez, M. T., Martin, I., Bills, G., Giacobbe, R., Dombrowski, A., Schwartz, R., Morris, S., Harris, G., Tsipouras, A., Wilson, K., & Kurtz, M. B.
- Venue
- Antimicrobial Agents and Chemotherapy
- Publisher
- American Society for Microbiology
- Published
- 2000-02
- Volume
- 44
- Issue
- 2
- Pages
- 368-377
- ISSN
- 0066-4804 (ISSN-L)
- 1098-6596
- OpenAlex
- W2108491966
- Cited by
- 326
- References
- 42
- FWCI
- 11.65
- Type
- journal article
- Language
- en
- Open access
- green
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- Onishi, J., Meinz, M., Thompson, J., Curotto, J., Dreikorn, S., Rosenbach, M., Douglas, C., Abruzzo, G., Flattery, A., Kong, L., Cabello, A., Vicente, F., Pelaez, F., Diez, M. T., Martin, I., Bills, G., Giacobbe, R., Dombrowski, A., Schwartz, R., . . . Kurtz, M. B. (2000). Discovery of Novel Antifungal (1,3)-β- d -Glucan Synthase Inhibitors. Antimicrobial Agents and Chemotherapy. https://doi.org/10.1128/aac.44.2.368-377.2000
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
