Tigilanol tiglate is an oncolytic small molecule that is undergoing clinical trials. A recent study revealed the capacity of this pyroptosis inducer to elicit hallmarks of immunogenic cell death. In addition, intratumoral injection of tigilanol tiglate can sensitize subcutaneous cancers to subsequent immune checkpoint inhibitors targeting CTLA-4 alone or in combination with PD-1.
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| http://dx.doi.org/10.1080/2162402X.2024.2360230 | DOI Listing |
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Epoxytiglianes induce keratinocyte wound healing responses via classical protein kinase C activation to promote skin re-epithelialization.
Biochem Pharmacol
December 2024
Disease Mechanisms Group, School of Dentistry, College of Biomedical and Life Sciences, Cardiff University, UK. Electronic address:
Epoxytiglianes are a novel class of diterpene esters. The prototype epoxytigliane, EBC-46 (tigilanol tiglate), is a potent anti-cancer agent in clinical development for local treatment of a range of human and animal tumors. EBC-46 also consistently promotes wound re-epithelialization at the treatment sites, mediated via activation of classical protein kinase C (PKC) isoforms.
View Article and Find Full Text PDFResponse to tigilanol tiglate in dogs with mast cell tumors.
J Vet Intern Med
November 2024
Clinical Sciences, Flint Animal Cancer Center, Colorado State University, Fort Collins, Colorado, USA.
Background: Information regarding response rate to tigilanol tiglate for mast cell tumors in dogs is limited.
Objectives: Report the response rate and durability of tigilanol tiglate intratumoral treatment in dogs with mast cell tumors presented to veterinary oncologists.
Animals: One hundred forty-nine dogs; 151 individual tumors.
Tigilanol Tiglate-Induced Changes in Secretome Profiles Alter C-Met Phosphorylation and Cell Surface Protein Expression in H357 Head and Neck Cancer Cells.
Cells
June 2024
School of Dentistry, College of Biomedical and Life Sciences, Cardiff University, Cardiff CF14 4XY, UK.
Tigilanol tiglate (TT, also known as EBC-46) is a novel, plant-derived diterpene ester possessing anticancer and wound-healing properties. Here, we show that TT-evoked PKC-dependent S phosphorylation of the tyrosine kinase MET leads to subsequent degradation of tyrosine phosphorylated p-Y and p-Y MET species. PKC inhibition with BIM-1 blocked S phosphorylation of MET and led to MET cell surface accumulation.
View Article and Find Full Text PDFImmunogenic oncolysis by tigilanol tiglate.
Oncoimmunology
May 2024
Centre de Recherche des Cordeliers, Equipe labellisée par la Ligue contre le cancer, Université de Paris Cité, Sorbonne Université, Paris, France.
Tigilanol tiglate is an oncolytic small molecule that is undergoing clinical trials. A recent study revealed the capacity of this pyroptosis inducer to elicit hallmarks of immunogenic cell death. In addition, intratumoral injection of tigilanol tiglate can sensitize subcutaneous cancers to subsequent immune checkpoint inhibitors targeting CTLA-4 alone or in combination with PD-1.
View Article and Find Full Text PDFTigilanol 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.
J Immunother Cancer
April 2024
QIMR Berghofer Medical Research Institute, Herston, Queensland, Australia.
Background: Tigilanol tiglate (TT) is a protein kinase C (PKC)/C1 domain activator currently being developed as an intralesional agent for the treatment of various (sub)cutaneous malignancies. Previous work has shown that intratumoral (I.T.
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