Quinto appuntamento del Ciclo di Seminari del DSF 2018/19, mercoledì 5 dicembre dalle 13:00 alle 13:40 in aula seminari al II piano di l.go Donegani 2 (ex Wild).
Il talk dal titolo: Structure-activity relationships of the anticancer diterpene EBC-46 sarà tenuto dal prof. Giovanni Appendino.
The diterpene ester tiglianol tigliate (EBC-46) occurs in high concentration in the unpalatable seeds of Fontainea picrosperma C.T. White (blushwood), a subcanopy euphorbiaceous tree endemic to a restricted (ca. 20 Km2) area of the Queensland rainforest. Tiglianol tigliate is remarkably efficacious in the treatment of localized tumors, and has successfully completed Phase III clinical development for veterinarian use and Phase I human clinical studies. Intra-tumor injection of EBC46 triggers a triad of responses (massive destruction of tumor vasculature, tumor hemorrhagic necrosis, stimulation of wound healing) sensitive to PKC pan-inhibitors, suggesting that modulation of PKC is part of its mechanism of action. The PKC isoform activation of EBC-6 is significantly different from the one of tetradecanoyl phorbol acetate (PMA) and ingenol mebutate, and studies aimed at clarifying the role of PKC in the mechanism of action of EBC-46 by systematically modifying the functional groups of the natural product will be presented.