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Finnin, M.S., Donigian, J.R., Cohen, A., Richon, V.M., Rifkind, R.A., Marks, P.A., Breslow, R. and Pavletich, N.P. (1999) Structures of a histone deacetylase homologue bound to the TSA and SAHA inhibitors. Nature, 401, 188-193. doi:10.1038/43710

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• TITLE: Novel histone deacetylase inhibitor exhibits antitumor activity via apoptosis induction in oral squamous cell carcinoma

  AUTHORS: Osamu Takahashi, Toshinori Okinaga, Kenjiro Iwanaga, Manabu Habu, Wataru Ariyoshi, Kazuhiro Tominaga, Norikazu Nishino, Tatsuji Nishihara

  KEYWORDS: Histone Deacetylase Inhibitor; Apoptosis; Squamous Cell Carcinoma; Hydroxamic Acid

  JOURNAL NAME: Journal of Biophysical Chemistry, Vol.2 No.3, August 9, 2011

  ABSTRACT: Epigenetic modifications such as histone deacetylation are commonly related to tumor development and histone deacetylase (HDAC) inhibitors have been shown to be potential drugs for cancer treatment. In the present study, we investigated the effects of a novel HDAC inhibitor, Ky-2, on oral squamous carcinoma cells in vitro. Cell viability was significantly reduced by treatment with Ky-2 at 25 nM, while it also led to augmentation of the proportion of cells in the sub-G1 phase and DNA fragmentation. In addition, immunoblot analysis revealed that Ky-2 enhanced the expression of apoptosis-related proteins. Our results showed that a low concentration of Ky-2 induced apoptosis in oral squamous carcinoma cells via activation of apoptotic cascades.