Anti-tumor activity of N-hydroxy-7-(2-naphthylthio) heptanomide, a novel histone deacetylase inhibitor.
作者： Dong Hoon Kim , Jiyong Lee , Kyung Noo Kim , Hye Jin Kim , Hei Cheul Jeung
DOI: 10.1016/J.BBRC.2007.02.126
关键词: Carcinogenesis 、 HDAC11 、 Cell growth 、 Cancer research 、 Biology 、 Histone deacetylase 5 、 Histone deacetylase 、 HT1080 、 Molecular biology 、 Histone deacetylase inhibitor 、 Histone deacetylase 2
摘要: Histone deacetylase (HDAC), a key enzyme in gene expression and carcinogenesis, is considered an attractive target molecule for cancer therapy. Here, we report new synthetic small molecule, N-hydroxy-7-(2-naphthylthio) heptanomide (HNHA), as HDAC inhibitor with anti-tumor activity both vitro vivo. The compound inhibited well proliferation of human fibrosarcoma cells (HT1080) vitro. Treatment HNHA elicited histone hyperacetylation leading to up-regulation p21 transcription, cell cycle arrest, inhibition HT1080 invasion. Moreover, effectively the growth tumor tissue mouse xenograph assay Together, these data demonstrate that this novel could be developed potential agent targeting HDAC.
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