组蛋白去乙酰化酶激活剂：N-乙酰基硫脲在荧光底物上作为高度有效且同工酶选择性的人组蛋白去乙酰化酶-8 的激活剂。
Histone deacetylase activators: N-acetylthioureas serve as highly potent and isozyme selective activators for human histone deacetylase-8 on a fluorescent substrate.
机构信息
Department of Chemistry and Biochemistry, North Dakota State University, Fargo, ND 58108, USA.
出版信息
Bioorg Med Chem Lett. 2011 Oct 1;21(19):5920-3. doi: 10.1016/j.bmcl.2011.07.080. Epub 2011 Aug 4.
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.
摘要
我们首次报告，某些 N-乙酰硫脲衍生物在含有 Fluor-de-Lys 作为荧光底物的检测系统中，作为高度有效的同工酶选择性激活剂，作用于重组人组蛋白去乙酰化酶-8。实验数据表明，这种激活特性是通过降低酶的底物的 K(m) 值和增加酶的催化周转率来体现的。
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