ArticleCancer science2010
Rubratoxin A specifically and potently inhibits protein phosphatase 2A and suppresses cancer metastasis.
Article in Cancer science, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 45 citations in OpenAlex.
- Article
- Apoptotic Janus-faced mycotoxins against thoracal and breast metastases.Apoptosis : an international journal on programmed cell death · 2023Review
- Repurposing a Cyclin-Dependent Kinase 1 (CDK1) Mitotic Regulatory Network to Complete Terminal Differentiation in Lens Fiber Cells.Investigative ophthalmology & visual science · 2023Article
- Maleidride biosynthesis - construction of dimeric anhydrides - more than just heads or tails.Natural product reports · 2023Review
- ERK-mediated NELF-A phosphorylation promotes transcription elongation of immediate-early genes by releasing promoter-proximal pausing of RNA polymerase II.Nature communications · 2022Article
- In silico analyses of maleidride biosynthetic gene clusters.Fungal biology and biotechnology · 2022Article
- The potent protein phosphatase 2A inhibitors aminocytostatins: new derivatives of cytostatin.The Journal of antibiotics · 2021Article
- MX2-mediated innate immunity against HIV-1 is regulated by serine phosphorylation.Nature microbiology · 2021Article
- Polo-like kinase 1 (Plk1) is a positive regulator of DNA replication in theCell cycle (Georgetown, Tex.) · 2020Article
- Influence of OSMAC-Based Cultivation in Metabolome and Anticancer Activity of Fungi Associated with the Brown AlgaMarine drugs · 2019Article
- Inhibitory effects of rubratoxin A, a potent inhibitor of protein phosphatase 2, on the CaJournal of smooth muscle research = Nihon Heikatsukin Gakkai kikanshi · 2019Article
- 9-Membered Carbocycles: Strategies and Tactics for their Synthesis.Chemistry (Weinheim an der Bergstrasse, Germany) · 2018Article
- Recent examples of α-ketoglutarate-dependent mononuclear non-haem iron enzymes in natural product biosyntheses.Natural product reports · 2018Review
- Protein phosphatases 1 and 2A and their naturally occurring inhibitors: current topics in smooth muscle physiology and chemical biology.The journal of physiological sciences : JPS · 2018Review
- Heterologous Production of Fungal Maleidrides Reveals the Cryptic Cyclization Involved in their Biosynthesis.Angewandte Chemie (International ed. in English) · 2016Article
- Novel autophagy inducers lentztrehaloses A, B and C.The Journal of antibiotics · 2015Article
- PP2A: The Wolf in Sheep's Clothing?Cancers · 2015Review
- Cantharidins induce ER stress and a terminal unfolded protein response in OSCC.Journal of dental research · 2015Article
- Force-inhibiting effect of Ser/Thr protein phosphatase 2A inhibitors on bovine ciliary muscle.Journal of smooth muscle research = Nihon Heikatsukin Gakkai kikanshi · 2015Article
- Article
Corrections and comments
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Although cytostatin analog protein phosphatase 2A (PP2A)-specific inhibitors are promising candidates of a new type of anticancer drug, their development has been hindered because of their liability. To find new classes of PP2A-specific inhibitors, we conducted a screening with microbial metabolites and found that rubratoxin A, a classical mycotoxin, is a highly specific and potent inhibitor of the enzyme. While rubratoxin A inhibits PP2A at Ki = 28.7 nm, it hardly inhibited any other phosphatases examined. Rubratoxin B, a close analog, also specifically but weakly inhibits PP2A at Ki = 3.1 microM. The inhibition of intracellular PP2A in cultured cells is obviously observed with 20 microM rubratoxin A treatment for 3 h, inducing the overphosphorylation in PP2A substrate proteins. Although rubratoxins and cytostatin differ in the apparent structures, these compounds share similarities in the structures in detail and PP2A-binding manners. Rubratoxin A showed higher suppression of tumor metastasis and reduction of the primary tumor volume than cytostatin in mouse experiments. As a successor of cytostatin analogs, rubratoxin A should be a good compound leading to the development of antitumor drugs targeting PP2A.
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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.