- Histone deacetylase activators: N-acetylthioureas serve as highly potent and isozyme selective activators for human histone deacetylase-8 on a fluorescent substrate.
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 (2011-08-26)
Raushan K Singh, Tanmay Mandal, Narayanaganesh Balsubramanian, Tajae Viaene, Travis Leedahl, Nitesh Sule, Gregory Cook, D K Srivastava
PMID21865040
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.
MATERIALS