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

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:21

Article

Singh, Raushan K.¹  Mandal, Tanmay²  Balsubramanian, Narayanaganesh¹  Viaene, Tajae¹  Leedahl, Travis¹  Sule, Nitesh¹  Cook, Gregory¹  Srivastava, D. K.¹ 

[1] N Dakota State Univ, Dept Chem & Biochem, Fargo, ND 58108 USA

[2] Univ Leipzig, Dept Organ Chem, D-04103 Leipzig, Germany

关键词: Enzyme activation;    Epigenetic regulation;    Histone deacetylase;    Isozyme selectivity;    Thiourea derivative;   

DOI  :  10.1016/j.bmcl.2011.07.080

来源: Elsevier

【 摘 要 】

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. (C) 2011 Elsevier Ltd. All rights reserved.

【 授权许可】

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