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

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.

SUBMITTER: Singh RK

PROVIDER: S-EPMC3171571 | biostudies-literature | 2011 Oct

REPOSITORIES: biostudies-literature

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

Singh Raushan K RK Mandal Tanmay T Balsubramanian Narayanaganesh N Viaene Tajae T Leedahl Travis T Sule Nitesh N Cook Gregory G Srivastava D K DK

Bioorganic & medicinal chemistry letters 20110804 19

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. ...[more]

PMID: 21865040

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