Histone deacetylase activators: N-acetylthioureas serve as highly potent and isozyme selective activators for human histone deacetylase-8 on a fluorescent substrate
作者:Raushan K. Singh、Tanmay Mandal、Narayanaganesh Balsubramanian、Tajae Viaene、Travis Leedahl、Nitesh Sule、Gregory Cook、D.K. Srivastava
DOI:10.1016/j.bmcl.2011.07.080
日期:2011.8
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.