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Bioorg Med Chem Lett. 2011 Oct 1;21(19):5920-3. doi: 10.1016/j.bmcl.2011.07.080. Epub 2011 Aug 4.

Histone deacetylase activators: N-acetylthioureas serve as highly potent and isozyme selective activators for human histone deacetylase-8 on a fluorescent substrate.

Author information

1
Department of Chemistry and Biochemistry, North Dakota State University, Fargo, ND 58108, USA.

Abstract

We report, for the first time, that certain N-acetylthiourea derivatives serve as highly potent and isozyme selective activators for the recombinant form of human histone deacetylase-8 in the assay system containing Fluor-de-Lys as a fluorescent substrate. The experimental data reveals that such activating feature is manifested via decrease in the K(m) value of the enzyme's substrate and increase in the catalytic turnover rate of the enzyme.

PMID:
21865040
PMCID:
PMC3171571
DOI:
10.1016/j.bmcl.2011.07.080
[Indexed for MEDLINE]
Free PMC Article

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