Bioorganic & Medicinal Chemistry Letters 2011-10-01

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

Raushan K Singh, Tanmay Mandal, Narayanaganesh Balsubramanian, Tajae Viaene, Travis Leedahl, Nitesh Sule, Gregory Cook, D K Srivastava

Index: Bioorg. Med. Chem. Lett. 21(19) , 5920-3, (2011)

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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.Copyright © 2011 Elsevier Ltd. All rights reserved.