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Record W3033452142 · doi:10.3389/fmicb.2020.00996

FDA Approved Drug Library Screening Identifies Robenidine as a Repositionable Antifungal

2020· article· en· W3033452142 on OpenAlexaff
Yikun Mei, Tong Jiang, Yun Zou, Yuanyuan Wang, Jia Zhou, Jinyang Li, Lin Liu, Jing-Cong Tan, Luqi Wei, Jingquan Li, Huanqin Dai, Yibing Peng, Lixin Zhang, José L. López-Ribot, Rebecca S. Shapiro, Changbin Chen, Ningning Liu, Hui Wang

Bibliographic record

VenueFrontiers in Microbiology · 2020
Typearticle
Languageen
FieldMedicine
TopicAntifungal resistance and susceptibility
Canadian institutionsUniversity of Guelph
FundersProgram for Professor of Special Appointment (Eastern Scholar) at Shanghai Institutions of Higher LearningSchool of Medicine, Shanghai Jiao Tong UniversityShanghai Jiao Tong UniversityChinese Academy of SciencesShanghai Municipal Education CommissionNational Natural Science Foundation of China
KeywordsCandida albicansMicrobiologyBiologyCorpus albicansAntifungal drugFluconazoleAntifungal

Abstract

fetched live from OpenAlex

New antifungal therapies have been imperative, largely due to the increasing burden of fungal infections worldwide, limited arsenal of available antifungal compounds, and the emergence of drug resistance among a variety of pathogenic fungi. In this study, we screened a library of 1068 FDA-approved drugs to identify hits that exhibit broad-spectrum antifungal activity. Robenidine, an anticoccidial agent which has been widely used to treat coccidian infections of poultry and rabbits, was identified in the screening. Physiological concentrations of robenidine were able to significantly inhibit yeast cell growth, filamentation and biofilm formation of Candida albicans, the most extensively studied human fungal pathogen associated with infections in immunocompromised patients. Moreover, we observed a broad-spectrum antifungal activity of this compound towards fluconazole resistant clinical isolates of C. albicans and a wide range of clinically relevant fungal pathogens as well. Intriguingly, the robenidine-treated C. albicans cells conferred hypersensitivity to diverse cell wall stressors and analysis of the cell wall structure by transmission electron microscopy (TEM) showed that cell wall was severely damaged by robenidine, both implying that this compound may target the cell wall integrity signaling pathway. Indeed, after robenidine treatment we found a dose dependent increase in the phosphorylation of cell wall integrity marker Mkc1 which was decreased after long exposure. Furthermore, we provided evidence by RNA-seq and qPCR that Rlm1, the downstream transcription factor of Mkc1, may represent a potential target of robenidine. Therefore, our data suggest that robenidine, a FDA approved anti-coccidiosis drug, displays a promising and broadly effective antifungal strategy and represents a potentially repositionable candidate for the treatment of increasing fungal infections.

Fetched live from OpenAlex and de-inverted. Abstracts are not stored in this database: the inverted indexes are 8.6 GB of the frame’s 9.3 GB of text, and the host has 13 GB free.

How this classification was reachedexpand

Direct model labels (unvalidated)

Per-model category and study-design labels from the labeling rounds. They are machine output, unvalidated, and the disagreement between models ships as data. No study design here is MEDLINE-validated yet.

Model armCategoriesStudy designConfidence
gemmano category
Domain: not available · Genre: Empirical
About the Canadian research system: no · About a Canadian topic: no
Bench or experimentalhigh
gptno category
Domain: not available · Genre: Empirical
About the Canadian research system: no · About a Canadian topic: no
Bench or experimentalhigh
models agreeAgreement compares identical category sets and study designs across arms.

Full frame machine prediction

Teacher imitation

Not calibrated prevalence, not ground truth. Human validation pending. The Gemma side is a direct model label for every work in the frame, read from the title-only record. The Codex side is a classifier learned from the 10,348 direct Codex labels and calibrated to design-weighted sample rates; fields without enough sample support carry no Codex call. Candidate is the union of the two sides; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels.

metaresearch head score (Codex)0.000
metaresearch head score (Gemma)0.000
Version: metacan-v3-hybrid-931329e0061cValidation status: machine_predicted_unvalidated
Candidate categoriesnone
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Bench or experimental · Consensus signal: Bench or experimental
GenreCandidate signal: Empirical · Consensus signal: Empirical
Teacher disagreement score0.005
Threshold uncertainty score0.016

Distilled classifier scores by category (both heads)

CategoryCodexGemma
Metaresearch0.0000.000
Meta-epidemiology (narrow)0.0010.000
Meta-epidemiology (broad)0.0010.001
Bibliometrics0.0010.001
Science and technology studies0.0000.000
Scholarly communication0.0010.000
Open science0.0000.000
Research integrity0.0010.001
Insufficient payload (model declined to judge)0.0050.001

Machine scores (provisional)

The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.

Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.

Opus teacher head0.011
GPT teacher head0.228
Teacher spread0.218 · how far apart the two teachers sit on this one work
Validation statusscore_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from it

Classification

machine, unvalidated

Labeled directly by 2 models reading the full record.

The models applied no category: nothing in the taxonomy fit this work.
Study designBench or experimental
Domainnot available
GenreEmpirical

How this classification was reached, model by model and score by score, is at the end of the page under "How this classification was reached".

Quick stats

Citations27
Published2020
Admission routes1
Has abstractyes

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