Potent in vivo anti-breast cancer activity of IN-2001, a novel inhibitor of histone deacetylase, in MMTWc-Neu mice
- Authors
- Joung, Ki Eun; Min, Kyung-Nan; An, Jin Yong; Kim, Dae-Kee; Kong, Gu.; Sheen, Yhun Yhong
- Issue Date
- May-2006
- Publisher
- AMER ASSOC CANCER RESEARCH
- Citation
- CANCER RESEARCH, v.66, no.10, pp.5394 - 5402
- Indexed
- SCIE
SCOPUS
- Journal Title
- CANCER RESEARCH
- Volume
- 66
- Number
- 10
- Start Page
- 5394
- End Page
- 5402
- URI
- https://scholarworks.bwise.kr/hanyang/handle/2021.sw.hanyang/181519
- DOI
- 10.1158/0008-5472.CAN-05-3835
- ISSN
- 0008-5472
- Abstract
- A novel synthetic inhibitor of historic deacetylase (HDAC), 3-(4-dimethylaminophenyl)-N-hydroxy-2-propenamide (IN-2001), was examined for its antitumor activity and for the underlying molecular mechanisms of any such activity. IN-2001 effectively inhibited cellular HDAC activity (IC50, 5.42 nmol/L) in MCF-7 human breast cancer cells. Based on the Western blot analysis, this HDAC inhibitory effect of IN-2001 was confirmed by an increase in histone 114 acetylation from the IN-2001-treated breast cancer cells. IN-2001 suppressed mammary tumor growth in MMTV/c-Neu transgenic mice and also showed higher apoptotic index and lower lymphatic invasion compared with controls. In human breast cancer cells (MCF-7, T47D, MDA-MB-231, and MDA-MB-468), IN-2001 induced cell cycle arrest at G(2)-M phase through up-regulation of p21(WAF1) and p27(KIP1) and eventually caused apoptosis. IN-2001-induced apoptosis was caspase dependent and seems mediated through an increase in Bax/Bcl-2 ratio. Taken together, our data indicate that this novel HDAC inhibitor is a promising therapeutic agent against human breast cancer.
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