ArticleACS infectious diseases2016
Antitumor/Antifungal Celecoxib Derivative AR-12 is a Non-Nucleoside Inhibitor of the ANL-Family Adenylating Enzyme Acetyl CoA Synthetase.
Article in ACS infectious diseases, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 31 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
31 citing papers in PubMed, 59 citations in OpenAlex.
- Article
- GPU-Accelerated Virtual Screening and Molecular Dynamics Simulations for Identification of Novel DPP‑4 Inhibitors.ACS omega · 2026Article
- Discovery and mechanism of a highly selective, antifungal acetyl-CoA synthetase inhibitor.Nature communications · 2025Article
- Targeting fungal lipid synthesis for antifungal drug development and potentiation of contemporary antifungals.npj antimicrobials and resistance · 2025Review
- Molecular Targets and Small Molecules Modulating Acetyl Coenzyme A in Physiology and Diseases.ACS pharmacology & translational science · 2025Review
- Overcoming antifungal resistance inFrontiers in cellular and infection microbiology · 2025Review
- Systematic analysis of themBio · 2024Article
- 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
- Challenges and Opportunities for Celecoxib Repurposing.Pharmaceutical research · 2023Review
- Identification of triazenyl indoles as inhibitors of fungal fatty acid biosynthesis with broad-spectrum activity.Cell chemical biology · 2023Article
- Combating increased antifungal drug resistance inActa biochimica et biophysica Sinica · 2023Review
- Human Kinase IGF1R/IR Inhibitor Linsitinib Controls the In Vitro and Intracellular Growth ofACS infectious diseases · 2022Article
- AR-12 Has a Bactericidal Activity and a Synergistic Effect with Gentamicin against Group AInternational journal of molecular sciences · 2021Article
- Prioritization of Molecular Targets for Antimalarial Drug Discovery.ACS infectious diseases · 2021Article
- Structural Characterization of the Reaction and Substrate Specificity Mechanisms of Pathogenic Fungal Acetyl-CoA Synthetases.ACS chemical biology · 2021Article
- The Future of Antifungal Drug Therapy: Novel Compounds and Targets.Antimicrobial agents and chemotherapy · 2021Review
- Drug Resistance and Novel Therapeutic Approaches in Invasive Candidiasis.Frontiers in cellular and infection microbiology · 2021Review
- Acetate Promotes a Differential Energy Metabolic Response in Human HCT 116 and COLO 205 Colon Cancer Cells Impacting Cancer Cell Growth and Invasiveness.Frontiers in oncology · 2021Article
Corrections and comments
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
AR-12/OSU-03012 is an antitumor celecoxib-derivative that has progressed to Phase I clinical trial as an anticancer agent and has activity against a number of infectious agents including fungi, bacteria and viruses. However, the mechanism of these activities has remained unclear. Based on a chemical-genetic profiling approach in yeast, we have found that AR-12 is an ATP-competitive, time-dependent inhibitor of yeast acetyl coenzyme A synthetase. AR-12-treated fungal cells show phenotypes consistent with the genetic reduction of acetyl CoA synthetase activity, including induction of autophagy, decreased histone acetylation, and loss of cellular integrity. In addition, AR-12 is a weak inhibitor of human acetyl CoA synthetase ACCS2. Acetyl CoA synthetase activity is essential in many fungi and parasites. In contrast, acetyl CoA is primarily synthesized by an alternate enzyme, ATP-citrate lyase, in mammalian cells. Taken together, our results indicate that AR-12 is a non-nucleoside acetyl CoA synthetase inhibitor and that acetyl CoA synthetase may be a feasible antifungal drug target.
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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.