Anti-tumor activity of N-hydroxy-7-(2-naphthylthio) heptanomide, a novel histone deacetylase inhibitor

Dong Hoon Kim; Jiyong Lee; Kyung Noo Kim; Hye Jin Kim; Hei Cheul Jeung; Hyun Cheol Chung; Ho Jeong Kwon

doi:10.1016/j.bbrc.2007.02.126

Anti-tumor activity of N-hydroxy-7-(2-naphthylthio) heptanomide, a novel histone deacetylase inhibitor

Dong Hoon Kim, Jiyong Lee, Kyung Noo Kim, Hye Jin Kim, Hei Cheul Jeung, Hyun Cheol Chung, Ho Jeong Kwon

Research output: Contribution to journal › Article › peer-review

13 Citations (Scopus)

Abstract

Histone deacetylase (HDAC), a key enzyme in gene expression and carcinogenesis, is considered an attractive target molecule for cancer therapy. Here, we report a new synthetic small molecule, N-hydroxy-7-(2-naphthylthio) heptanomide (HNHA), as a HDAC inhibitor with anti-tumor activity both in vitro and in vivo. The compound inhibited HDAC enzyme activity as well as proliferation of human fibrosarcoma cells (HT1080) in vitro. Treatment of cells with HNHA elicited histone hyperacetylation leading to an up-regulation of p21 transcription, cell cycle arrest, and an inhibition of HT1080 cell invasion. Moreover, HNHA effectively inhibited the growth of tumor tissue in a mouse xenograph assay in vivo. Together, these data demonstrate that this novel HDAC inhibitor could be developed as a potential anti-tumor agent targeting HDAC.

Original language	English
Pages (from-to)	233-238
Number of pages	6
Journal	Biochemical and Biophysical Research Communications
Volume	356
Issue number	1
DOIs	https://doi.org/10.1016/j.bbrc.2007.02.126
Publication status	Published - 2007 Apr 27

Bibliographical note

Funding Information:
This study was supported by grants from the National R&D Program for Cancer Control, Ministry of Health & Welfare (0620360-1), and from the Brain Korea 21 Project, Republic of Korea.

All Science Journal Classification (ASJC) codes

Biophysics
Biochemistry
Molecular Biology
Cell Biology

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10.1016/j.bbrc.2007.02.126

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title = "Anti-tumor activity of N-hydroxy-7-(2-naphthylthio) heptanomide, a novel histone deacetylase inhibitor",

abstract = "Histone deacetylase (HDAC), a key enzyme in gene expression and carcinogenesis, is considered an attractive target molecule for cancer therapy. Here, we report a new synthetic small molecule, N-hydroxy-7-(2-naphthylthio) heptanomide (HNHA), as a HDAC inhibitor with anti-tumor activity both in vitro and in vivo. The compound inhibited HDAC enzyme activity as well as proliferation of human fibrosarcoma cells (HT1080) in vitro. Treatment of cells with HNHA elicited histone hyperacetylation leading to an up-regulation of p21 transcription, cell cycle arrest, and an inhibition of HT1080 cell invasion. Moreover, HNHA effectively inhibited the growth of tumor tissue in a mouse xenograph assay in vivo. Together, these data demonstrate that this novel HDAC inhibitor could be developed as a potential anti-tumor agent targeting HDAC.",

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note = "Funding Information: This study was supported by grants from the National R&D Program for Cancer Control, Ministry of Health & Welfare (0620360-1), and from the Brain Korea 21 Project, Republic of Korea.",

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AU - Kim, Hye Jin

AU - Jeung, Hei Cheul

AU - Chung, Hyun Cheol

AU - Kwon, Ho Jeong

N1 - Funding Information: This study was supported by grants from the National R&D Program for Cancer Control, Ministry of Health & Welfare (0620360-1), and from the Brain Korea 21 Project, Republic of Korea.

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Anti-tumor activity of N-hydroxy-7-(2-naphthylthio) heptanomide, a novel histone deacetylase inhibitor

Abstract

Bibliographical note

All Science Journal Classification (ASJC) codes

UN SDGs

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