The DOI matches its Crossref record; 46 of the 46 references it cites were found in a registry or an index.
A synthetic inhibitor of histone deacetylase, MS-27-275, with marked in vivo antitumor activity against human tumors
Open accessAbstract
Synthetic benzamide derivatives were investigated for their ability to inhibit histone deacetylase (HDA). In this study, one of the most active benzamide derivatives, MS-27-275, was examined with regard to its biological properties and antitumor efficacy. MS-27-275 inhibited partially purified human HDA and caused hyperacetylation of nuclear histones in various tumor cell lines. It behaved in a manner similar to other HDA inhibitors, such as sodium butyrate and trichostatin A; MS-27-275 induced p21 WAF1/CIP1 and gelsolin and changed the cell cycle distribution, decrease of S-phase cells, and increase of G 1 -phase cells. The in vitro sensitivity spectrum of MS-27-275 against various human tumor cell lines showed a pattern different than that of a commonly used antitumor agent, 5-fluorouracil, and, of interest, the accumulation of p21 WAF1/CIP1 tended to be faster and greater in the cell lines sensitive to MS-27-275. MS-27-275 administered orally strongly inhibited the growth in seven of eight tumor lines implanted into nude mice, although most of these did not respond to 5-fluorouracil. A structurally analogous compound to MS-27-275 without HDA-inhibiting activity showed neither the biological effects in cell culture nor the in vivo therapeutic efficacy. These results suggest that MS-27-275 acts as an antitumor agent through HDA inhibition and may provide a novel chemotherapeutic strategy for cancers insensitive to traditional antitumor agents.
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Cited by
Histone deacetylases (HDACs): characterization of the classical HDAC family
RUIJTER, A. J. M. D., GENNIP, A. H. V., CARON, H. N., KEMP, S., & KUILENBURG, A. B. P. V. (2003) · Biochemical Journal · doi:10.1042/bj20021321 · Cited by 3,114
Histone deacetylases and cancer: causes and therapies
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Histone-deacetylase inhibitors: novel drugs for the treatment of cancer
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Epigenetic therapy of cancer: past, present and future
Yoo, C. B., & Jones, P. A. (2006) · Nature Reviews Drug Discovery · doi:10.1038/nrd1930 · Cited by 1,289
Histone Deacetylase Inhibitors: Inducers of Differentiation or Apoptosis of Transformed Cells
Marks, P. A., Richon, V. M., & Rifkind, R. A. (2000) · JNCI Journal of the National Cancer Institute · doi:10.1093/jnci/92.15.1210 · Cited by 1,157
Metadata
- Authors
- Saito, A., Yamashita, T., Mariko, Y., Nosaka, Y., Tsuchiya, K., Ando, T., Suzuki, T., Tsuruo, T., & Nakanishi, O.
- Venue
- Proceedings of the National Academy of Sciences
- Published
- 1999-04-13
- Volume
- 96
- Issue
- 8
- Pages
- 4592-4597
- ISSN
- 0027-8424 (ISSN-L)
- 1091-6490
- OpenAlex
- W2082739830
- Cited by
- 694
- References
- 46
- FWCI
- 9.35
- Type
- journal article
- Language
- en
- Open access
- green
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- Saito, A., Yamashita, T., Mariko, Y., Nosaka, Y., Tsuchiya, K., Ando, T., Suzuki, T., Tsuruo, T., & Nakanishi, O. (1999). A synthetic inhibitor of histone deacetylase, MS-27-275, with marked in vivo antitumor activity against human tumors. Proceedings of the National Academy of Sciences. https://doi.org/10.1073/pnas.96.8.4592
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