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Potent in vivo anti-breast cancer activity of IN-2001, a novel inhibitor of histone deacetylase, in MMTV/c-Neu Mice

Title
Potent in vivo anti-breast cancer activity of IN-2001, a novel inhibitor of histone deacetylase, in MMTV/c-Neu Mice
Authors
Joung K.E.Min K.N.An J.Y.Kim D.-K.Kong G.Sheen Y.Y.
Ewha Authors
신윤용김대기
SCOPUS Author ID
신윤용scopus; 김대기scopus
Issue Date
2006
Journal Title
Cancer Research
ISSN
0008-5472JCR Link
Citation
Cancer Research vol. 66, no. 10, pp. 5394 - 5402
Indexed
SCI; SCIE; SCOPUS WOS scopus
Document Type
Article
Abstract
A novel synthetic inhibitor of histone 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 (IC 50, 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 H4 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. ©2006 American Association for Cancer Research.
DOI
10.1158/0008-5472.CAN-05-3835
Appears in Collections:
약학대학 > 약학과 > Journal papers
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