Search results for " HDAC inhibitor."
showing 2 items of 2 documents
The HDAC inhibitor SAHA synergistically stimulates the cytotoxic effect induced by Parthenolide in MDA-MB231 cells
2014
We showed that the sesquiterpene lactone Parthenolide (PN) exerts strong cytotoxic effects on triple negative breast cancer MDA-MB231 cells. Our recent results suggest that PN exerts in these cells a cytoprotective effect, which is due to the activation of mTOR pathway. To inhibit this protective response we employ the HDAC inhibitor SAHA, which is known to prevent AKT/mTOR pathway. We show that PN activates Akt, mTOR, p70S6kinase and NRF2 while SAHA abolishes these effects. Further cell pretreatment with SAHA synergistically sensitizes the cells to the cytotoxic effect of PN. Moreover SAHA alone activates the autophagic process. The addition of PN to SAHA reduces this effect and induces ap…
The histone deacetylase inhibitor ITF2357 targets oncogenic BRAF in human melanoma cells
2016
ITF2357 (Givinostat) is a potent antineoplastic histone deacetylase inhibitor which is currently used in clinical trials for leukemias and myelomas and in the therapy for systemic juvenile idiopathic arthritis. Here evidence is provided that ITF2357 reduces the viability of human melanoma SK-Mel28 cells thereby inducing cell death. This compound was more efficacious than SAHA, another well known HDAC inhibitor belonging to the same class of hydroxamic acids. Moreover, we demonstrated for the first time that ITF2357 determines in SK-Mel28 cells a remarkable reduction in the level of oncogenic B-Raf, the product of the BRAF V600E mutated gene in melanoma. Western blot analysis showed that the…