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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.

Authors:
 [1];  [1];  [1];  [1];  [2];  [2];  [3]
  1. Chemical Genomics Laboratory, Department of Biotechnology, College of Engineering, Yonsei University, 134 Shinchon-dong, Seodaemun-gu, Seoul 120-749 (Korea, Republic of)
  2. Cancer Metastasis Research Center, Yonsei University College of Medicine, 134 Shinchon-dong, Seodaemun-gu, Seoul 120-752 (Korea, Republic of)
  3. Chemical Genomics Laboratory, Department of Biotechnology, College of Engineering, Yonsei University, 134 Shinchon-dong, Seodaemun-gu, Seoul 120-749 (Korea, Republic of). E-mail: kwonhj@yonsei.ac.kr
Publication Date:
OSTI Identifier:
20991316
Resource Type:
Journal Article
Resource Relation:
Journal Name: Biochemical and Biophysical Research Communications; Journal Volume: 356; Journal Issue: 1; Other Information: DOI: 10.1016/j.bbrc.2007.02.126; PII: S0006-291X(07)00420-2; Copyright (c) 2007 Elsevier Science B.V., Amsterdam, The Netherlands, All rights reserved; Country of input: International Atomic Energy Agency (IAEA)
Country of Publication:
United States
Language:
English
Subject:
60 APPLIED LIFE SCIENCES; CARCINOGENESIS; CELL CYCLE; CELL PROLIFERATION; ENZYME ACTIVITY; ENZYMES; GENE REGULATION; GROWTH; HUMAN POPULATIONS; IN VITRO; IN VIVO; INHIBITION; MICE; NEOPLASMS; THERAPY

Citation Formats

Kim, Dong Hoon, Lee, Jiyong, Kim, Kyung Noo, Kim, Hye Jin, Jeung, Hei Cheul, Chung, Hyun Cheol, and Kwon, Ho Jeong. Anti-tumor activity of N-hydroxy-7-(2-naphthylthio) heptanomide, a novel histone deacetylase inhibitor. United States: N. p., 2007. Web. doi:10.1016/j.bbrc.2007.02.126.
Kim, Dong Hoon, Lee, Jiyong, Kim, Kyung Noo, Kim, Hye Jin, Jeung, Hei Cheul, Chung, Hyun Cheol, & Kwon, Ho Jeong. Anti-tumor activity of N-hydroxy-7-(2-naphthylthio) heptanomide, a novel histone deacetylase inhibitor. United States. doi:10.1016/j.bbrc.2007.02.126.
Kim, Dong Hoon, Lee, Jiyong, Kim, Kyung Noo, Kim, Hye Jin, Jeung, Hei Cheul, Chung, Hyun Cheol, and Kwon, Ho Jeong. Fri . "Anti-tumor activity of N-hydroxy-7-(2-naphthylthio) heptanomide, a novel histone deacetylase inhibitor". United States. doi:10.1016/j.bbrc.2007.02.126.
@article{osti_20991316,
title = {Anti-tumor activity of N-hydroxy-7-(2-naphthylthio) heptanomide, a novel histone deacetylase inhibitor},
author = {Kim, Dong Hoon and Lee, Jiyong and Kim, Kyung Noo and Kim, Hye Jin and Jeung, Hei Cheul and Chung, Hyun Cheol and Kwon, Ho Jeong},
abstractNote = {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.},
doi = {10.1016/j.bbrc.2007.02.126},
journal = {Biochemical and Biophysical Research Communications},
number = 1,
volume = 356,
place = {United States},
year = {Fri Apr 27 00:00:00 EDT 2007},
month = {Fri Apr 27 00:00:00 EDT 2007}
}