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| Item Type: | Article |
|---|---|
| Title: | HKI 46F08, a novel potent histone deacetylase inhibitor, exhibits antitumoral activity against embryonic childhood cancer cells |
| Creators Name: | Wegener, D., Deubzer, H.E., Oehme, I., Milde, T., Hildmann, C., Schwienhorst, A. and Witt, O. |
| Abstract: | Embryonic childhood cancer such as neuroblastoma and medulloblastoma are still a therapeutic challenge requiring novel treatment approaches. Here, we investigated the antitumoral effects of HKI 46F08, a novel trifluoromethyl ketone histone deacetylase (HDAC) inhibitor with a nonhydroxamic acid type structure. HKI 46F08 inhibits in-vitro HDAC activity in cell-free assays with a half maximal inhibitory concentration of 0.6 micromol/l and intracellular HDAC activity with a half maximal inhibitory concentration of 1.8 micromol/l. The compound reduces viability of both cultured neuroblastoma and medulloblastoma cells with an EC50 of 0.1-4 micromol/l. HKI 46F08 efficiently arrests tumor cell proliferation, represses clonogenic growth and induces differentiation and apoptosis in both MYCN-amplified and nonamplified neuroblastoma cells. In summary, we identified HKI 48F08 as a structural novel, potent HDAC inhibitor with strong antitumoral activity against embryonic childhood cancer cells in the low micromolar range. |
| Keywords: | Histone Deacetylase Inhibitor, HKI 46F08, Medulloblastoma, Neuroblastoma, Animals, Rats |
| Source: | Anti-Cancer Drugs |
| ISSN: | 0959-4973 |
| Publisher: | Lippincott Williams & Wilkins |
| Volume: | 19 |
| Number: | 9 |
| Page Range: | 849-857 |
| Date: | October 2008 |
| Official Publication: | https://doi.org/10.1097/CAD.0b013e32830efbeb |
| PubMed: | View item in PubMed |
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