ArticleAntimicrobial agents and chemotherapy2016
The Celecoxib Derivative AR-12 Has Broad-Spectrum Antifungal Activity In Vitro and Improves the Activity of Fluconazole in a Murine Model of Cryptococcosis.
Article in Antimicrobial agents and chemotherapy, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 48 papers.
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Who cites it
48 citing papers in PubMed, 85 citations in OpenAlex.
- Article
- Target product profile and discovery and development path for novel cryptococcal disease treatments.The Journal of infection · 2025Review
- Discovery and mechanism of a highly selective, antifungal acetyl-CoA synthetase inhibitor.Nature communications · 2025Article
- Next-generation antifungal drugs: Mechanisms, efficacy, and clinical prospects.Acta pharmaceutica Sinica. B · 2025Review
- Dermatophytosis in context of Trichophyton rubrum: host defense mechanisms, virulence factors, and treatment innovations.Molecular biology reports · 2025Review
- Targeting fungal lipid synthesis for antifungal drug development and potentiation of contemporary antifungals.npj antimicrobials and resistance · 2025Review
- Antifungal activity of a maleimide derivative: disruption of cell membranes and interference with iron ion homoeostasis.Mycology · 2025Article
- Sustainable Primary Cell Banking for Topical Compound Cytotoxicity Assays: Protocol Validation on Novel Biocides and Antifungals for Optimized Burn Wound Care.European burn journal · 2024Article
- Vitamin B5 metabolism is essential for vacuolar and mitochondrial functions and drug detoxification in fungi.Communications biology · 2024Article
- Cryptococcosis and Cryptococcal Meningitis: A Narrative Review and the Up-to-Date Management Approach.Cureus · 2024Review
- New anticancer therapeutics impact fungal pathobiology, infection dynamics, and outcome.PLoS pathogens · 2023Article
- Kicking sleepers out of bed: Macrophages promote reactivation of dormant Cryptococcus neoformans by extracellular vesicle release and non-lytic exocytosis.PLoS pathogens · 2023Article
- Challenges and Opportunities for Celecoxib Repurposing.Pharmaceutical research · 2023Review
- Recent drug development and treatments for fungal infections.Brazilian journal of microbiology : [publication of the Brazilian Society for Microbiology] · 2023Review
- Epidemiology, Modern Diagnostics, and the Management of Mucorales Infections.Journal of fungi (Basel, Switzerland) · 2023Review
- Atazanavir Resensitizes Candida auris to Azoles.Antimicrobial agents and chemotherapy · 2023Article
- Combating increased antifungal drug resistance inActa biochimica et biophysica Sinica · 2023Review
- Antifungal Susceptibility Testing and Drug Discovery in the Dimorphic Fungus Histoplasma Capsulatum.Methods in molecular biology (Clifton, N.J.) · 2023Article
- Article
- Pseudomonas Synergizes with Fluconazole againstInfection and immunity · 2022Article
Corrections and comments
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Authors and funding
11 authors at 4 institutions in 1 country.
Funding
Abstract
Only one new class of antifungal drugs has been introduced into clinical practice in the last 30 years, and thus the identification of small molecules with novel mechanisms of action is an important goal of current anti-infective research. Here, we describe the characterization of the spectrum of in vitro activity and in vivo activity of AR-12, a celecoxib derivative which has been tested in a phase I clinical trial as an anticancer agent. AR-12 inhibits fungal acetyl coenzyme A (acetyl-CoA) synthetase in vitro and is fungicidal at concentrations similar to those achieved in human plasma. AR-12 has a broad spectrum of activity, including activity against yeasts (e.g., Candida albicans, non-albicans Candida spp., Cryptococcus neoformans), molds (e.g., Fusarium, Mucor), and dimorphic fungi (Blastomyces, Histoplasma, and Coccidioides) with MICs of 2 to 4 μg/ml. AR-12 is also active against azole- and echinocandin-resistant Candida isolates, and subinhibitory AR-12 concentrations increase the susceptibility of fluconazole- and echinocandin-resistant Candida isolates. Finally, AR-12 also increases the activity of fluconazole in a murine model of cryptococcosis. Taken together, these data indicate that AR-12 represents a promising class of small molecules with broad-spectrum antifungal activity.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.