ArticleMedical oncology (Northwood, London, England)2004
Gliotoxin is a dual inhibitor of farnesyltransferase and geranylgeranyltransferase I with antitumor activity against breast cancer in vivo.
Article in Medical oncology (Northwood, London, England), 2004. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 45 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.
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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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
45 citing papers in PubMed, 102 citations in OpenAlex.
- Anticancer Secondary Metabolites Produced by Fungi: Potential and Representative Compounds.International journal of molecular sciences · 2025Review
- Total Synthesis and Anticancer Study of (+)-Verticillin A.Journal of the American Chemical Society · 2025Article
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- UtilizingArchives of Razi Institute · 2025Review
- Modeling Melanoma Heterogeneity In Vitro: Redox, Resistance and Pigmentation Profiles.Antioxidants (Basel, Switzerland) · 2024Article
- 2,5-Diketopiperazines (DKPs): Promising Scaffolds for Anticancer Agents.Current pharmaceutical design · 2024Review
- Epipolythiodioxopiperazine-Based Natural Products: Building Blocks, Biosynthesis and Biological Activities.Chembiochem : a European journal of chemical biology · 2022Review
- Inhibition of the HIF-1 Survival Pathway as a Strategy to Augment Photodynamic Therapy Efficacy.Methods in molecular biology (Clifton, N.J.) · 2022Article
- The Toxic Mechanism of Gliotoxins and Biosynthetic Strategies for Toxicity Prevention.International journal of molecular sciences · 2021Review
- Article
- A microbial metabolite synergizes with endogenous serotonin to triggerProceedings of the National Academy of Sciences of the United States of America · 2020Article
- Article
- Synthesis of Potent Cytotoxic Epidithiodiketopiperazines Designed for Derivatization.The Journal of organic chemistry · 2020Article
- Dechdigliotoxins A-C, Three Novel Disulfide-Bridged Gliotoxin Dimers from Deep-Sea Sediment Derived FungusMarine drugs · 2019Article
- Novel Action Targets of Natural Product Gliotoxin in Photosynthetic Apparatus.Frontiers in plant science · 2019Article
- De Novo Transcriptome Sequencing of the Deep-Sea-Derived FungusInternational journal of molecular sciences · 2018Article
- Effects of the Combination of Gliotoxin and Adriamycin on the Adriamycin-Resistant Non-Small-Cell Lung Cancer A549 Cell Line.Marine drugs · 2018Article
- Structural Diversity and Biological Activities of the Cyclodipeptides from Fungi.Molecules (Basel, Switzerland) · 2017Review
- Quantitative Modeling of Bis(pyridine)silver(I) Permanganate Oxidation of Hydantoin Derivatives: Guidelines for Predicting the Site of Oxidation in Complex Substrates.Journal of the American Chemical Society · 2017Article
- Marine-Derived Penicillium Species as Producers of Cytotoxic Metabolites.Marine drugs · 2017Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
8 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Gliotoxin is a natural mycotoxin with immunosuppressive and antimicrobial activity. Inhibition of farnesyltransferase (IC50 80 microM) and geranylgeranyltransferase I (IC50 17 microM) stimulated interest in the potential antitumor activity of this epidithiodioxopiperazine. Gliotoxin inhibited proliferation of six breast cancer cell lines in culture with mean +/- SD IC50 289 +/- 328 microM (range 38-985 microM); intracellular farnesylation of Lamin B and geranylgeranylation of Rap1A were inhibited in a dose-dependent manner. In randomized controlled studies using the N-methyl-N-nitrosourea rat mammary carcinoma model, gliotoxin had pronounced antitumor activity in vitro and little systemic toxicity when administered to 10 animals at 10 mg/kg by subcutaneous injection weekly for 4 wk compared with 10 controls. Single doses up to 25 mg/kg were well tolerated. The present studies confirm that gliotoxin is a dual inhibitor of farnesyltransferase and geranylgeranyltransferase I with pronounced antitumor activity and favorable toxicity profile against breast cancer in vitro and in vivo.
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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.