The DOI matches its Crossref record; 46 of the 47 references it cites were found in a registry or an index.
High-Throughput Screening of a Collection of Known Pharmacologically Active Small Compounds for Identification of Candida albicans Biofilm Inhibitors
Open accessAbstract
Candida albicans is the most common etiologic agent of systemic fungal infections with unacceptably high mortality rates. The existing arsenal of antifungal drugs is very limited and is particularly ineffective against C. albicans biofilms. To address the unmet need for novel antifungals, particularly those active against biofilms, we have screened a small molecule library consisting of 1,200 off-patent drugs already approved by the Food and Drug Administration (FDA), the Prestwick Chemical Library, to identify inhibitors of C. albicans biofilm formation. According to their pharmacological applications that are currently known, we classified these bioactive compounds as antifungal drugs, as antimicrobials/antiseptics, or as miscellaneous drugs, which we considered to be drugs with no previously characterized antifungal activity. Using a 96-well microtiter plate-based high-content screening assay, we identified 38 pharmacologically active agents that inhibit C. albicans biofilm formation. These drugs were subsequently tested for their potency and efficacy against preformed biofilms, and we identified three drugs with novel antifungal activity. Thus, repurposing FDA-approved drugs opens up a valuable new avenue for identification and potentially rapid development of antifungal agents, which are urgently needed.
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“| Zotepine | | | | | | (High affinity to dopamine | | | | | | receptors, affects serotonin receptors, its active metabolite, | C. albicans | 0.1-40 µM (0.03-12 µg/mL) | Inhibits biofilm development | [10] |”
From Antimicrobial Properties of Antidepressants and Antipsychotics—Possibilities and Implications (2021) · cites this paper as [10]
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Self-citationCalderone, R. (2012) · ASM Press eBooks · Cited by 912
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Drug repurposing for antimicrobial discovery
Farha, M. A., & Brown, E. D. (2019) · Nature Microbiology · doi:10.1038/s41564-019-0357-1 · Cited by 382
Drug repositioning and repurposing: terminology and definitions in literature
Langedijk, J., Mantel-Teeuwisse, A. K., Slijkerman, D. S., & Schutjens, M.-H. D. B. (2015) · Drug Discovery Today · doi:10.1016/j.drudis.2015.05.001 · Cited by 327
Drug-Resistant Fungi: An Emerging Challenge Threatening Our Limited Antifungal Armamentarium
Arastehfar, A. A., Gabaldón, T., Garcia‐Rubio, R., Jenks, J. D., Hoenigl, M., Salzer, H. J. F., İlkit, M., Lass‐Flörl, C., & Perlin, D. S. (2020) · Antibiotics · doi:10.3390/antibiotics9120877 · Cited by 302
Mechanistic Understanding of Candida albicans Biofilm Formation and Approaches for Its Inhibition
Atriwal, T., Azeem, K., Husain, F. M., Hussain, A., Khan, M. N., Alajmi, M. F., & Abid, M. (2021) · Frontiers in Microbiology · doi:10.3389/fmicb.2021.638609 · Cited by 222
Current Antimycotics, New Prospects, and Future Approaches to Antifungal Therapy
Wall, G., & Lopez-Ribot, J. L. (2020) · Antibiotics · doi:10.3390/antibiotics9080445 · Cited by 183
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Metadata
- Authors
- Siles, S. A., Srinivasan, A., Pierce, C. G., Lopez-Ribot, J. L., & Ramasubramanian, A. K.
- Affiliations
- The University of Texas at San Antonio (US)
- Departments of Biology, The University of Texas at San Antonio, San Antonio, Texas, USA
- Venue
- Antimicrobial Agents and Chemotherapy
- Publisher
- American Society for Microbiology
- Published
- 2013-08
- Volume
- 57
- Issue
- 8
- Pages
- 3681-3687
- ISSN
- 0066-4804 (ISSN-L)
- 1098-6596
- PMC
- PMC3719724
- OpenAlex
- W2171146043
- Cited by
- 120
- References
- 47
- Citations by year
- 2026: 4 · 2025: 5 · 2024: 5 · 2023: 10 · 2022: 11 · 2021: 10 · 2020: 16 · 2019: 10 · 2018: 14 · 2017: 6 · 2016: 9 · 2015: 14 · 2014: 3 · 2013: 2
- FWCI
- 6.78
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- Antimicrobial Agents and Chemotherapy (publishedVersion)
- Europe PMC (PubMed Central) (publishedVersion)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- Funders
- U.S. Department of Defense
- San Antonio Area Foundation
- National Heart, Lung, and Blood Institute (SC1HL112629)
- National Institute of Dental and Craniofacial Research (R01DE023510)
- Army Research Office
- Topics
- Health Sciences › Medicine › Infectious Diseases › Antifungal resistance and susceptibility
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Bacterial biofilms and quorum sensing
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Fungal and yeast genetics research
- Keywords
- Candida albicans, biofilm formation, antibiofilm agents, antifungal drug repurposing, FDA-approved drugs, Prestwick Chemical Library, high-content screening, drug discovery, systemic fungal infection
- MeSH terms
- Amphotericin B, Antifungal Agents, Benzethonium, Candida albicans, Dimethyl Sulfoxide, Disinfectants, Dose-Response Relationship, Drug, Microbial Sensitivity Tests, Biofilms, Microbial Viability, Small Molecule Libraries, High-Throughput Screening Assays
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