ArticleScientific reports2021
Activation of PKC supports the anticancer activity of tigilanol tiglate and related epoxytiglianes.
Article in Scientific reports, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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15 citing papers in PubMed, 34 citations in OpenAlex.
- Jurkat T-Cell Antigen-Independent Elimination of PMA-Activated Neuroblastoma Cells Is Triggered by CCL2/CCR2, Depends Upon Lipid Raft LFA1/ICAM1 Immune Synapses, Is Mediated by m-TRAIL and Is Augmented by the TrkAIII Oncoprotein.International journal of molecular sciences · 2026Article
- Intratumoural tigilanol tiglate in the multicentre treatment of equine sarcoids and cutaneous melanomas.Equine veterinary journal · 2026Article
- Synthesis and preclinical evaluation of tigilanol tiglate analogs as latency-reversing agents for the eradication of HIV.Science advances · 2025Article
- Australian Rainforests-A Living Museum of Natural Product Chemical Diversity.Progress in the chemistry of organic natural products · 2025Review
- Topological Heterogeneity of Protein Kinase C Modulators in Human T-Cells Resolved with In-Cell Dynamic Nuclear Polarization NMR Spectroscopy.Journal of the American Chemical Society · 2024Article
- Article
- Tigilanol tiglate is an oncolytic small molecule that induces immunogenic cell death and enhances the response of both target and non-injected tumors to immune checkpoint blockade.Journal for immunotherapy of cancer · 2024Article
- Tigliane Diterpenoids.Progress in the chemistry of organic natural products · 2024Review
- Tigliane and daphnane diterpenoids from Thymelaeaceae family: chemistry, biological activity, and potential in drug discovery.Journal of natural medicines · 2023Review
- DefiningJournal of oral microbiology · 2023Article
- Cryptic Epoxytiglianes from the Kernels of the Blushwood Tree (Journal of natural products · 2022Review
- Treatment of multiple synchronous canine mast cell tumours using intratumoural tigilanol tiglate.Frontiers in veterinary science · 2022Article
- Article
- Targeting Protein Kinase C in Glioblastoma Treatment.Biomedicines · 2021Review
- Tigilanol Tiglate-Mediated Margins: A Comparison With Surgical Margins in Successful Treatment of Canine Mast Cell Tumours.Frontiers in veterinary science · 2021Article
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Authors and funding
19 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The long-standing perception of Protein Kinase C (PKC) as a family of oncoproteins has increasingly been challenged by evidence that some PKC isoforms may act as tumor suppressors. To explore the hypothesis that activation, rather than inhibition, of these isoforms is critical for anticancer activity, we isolated and characterized a family of 16 novel phorboids closely-related to tigilanol tiglate (EBC-46), a PKC-activating epoxytigliane showing promising clinical safety and efficacy for intratumoral treatment of cancers. While alkyl branching features of the C12-ester influenced potency, the 6,7-epoxide structural motif and position was critical to PKC activation in vitro. A subset of the 6,7-epoxytiglianes were efficacious against established tumors in mice; which generally correlated with in vitro activation of PKC. Importantly, epoxytiglianes without evidence of PKC activation showed limited antitumor efficacy. Taken together, these findings provide a strong rationale to reassess the role of PKC isoforms in cancer, and suggest in some situations their activation can be a promising strategy for anticancer drug discovery.
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