A miniaturized readout strategy for endogenous histone deacetylase activity.
نویسندگان
چکیده
Histone deacetylases are important drug targets, which are difficult to characterize due to their poor accessibility. We have developed a miniaturized assay for the multi-site readout of deacetylase activity and profiled the substrate selectivity of HDACs for acetylation sites on histone H4 and tumor suppressor protein p53.
منابع مشابه
Histone deacetylase inhibitory and cytotoxic activities of the constituents from the roots of three species of Ferula
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متن کاملHistone Deacetylase Inhibitory and Cytotoxic Activities of the Constituents from the Roots of Sophora Pachycarpa
Four prenylated flavonoids including isosophoranone, sophoraflavanone G, alopecurone J, alopecurone P and a resveratrol derivative HPD (2-(4-hydroxyphenyl)-2,3-dihydrobenzo[b] furan-3,4,6-triol), were isolated from the roots of Sophora pachycarpa. The cytotoxic activity of obtained compounds was evaluated against A2780, A549, HeLa, and HCT116 human cancer cell lines. We also evaluated their his...
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Histone deacetylase inhibitors have gained a great deal of attention recently for the treatment of cancers and inflammatory diseases. So design of new inhibitors is of great importance in pharmaceutical industries and labs. Creating pharmacophor models in order to design new molecules or search a library for finding lead compounds is of great interest. This approach reduces the overall cost ass...
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عنوان ژورنال:
- Molecular bioSystems
دوره 11 7 شماره
صفحات -
تاریخ انتشار 2015