A non-isotopic assay for histone deacetylase activity.
نویسندگان
چکیده
Inhibitors of histone deacetylase (HD) bear great potential as new drugs due to their ability to modulate transcription and to induce apoptosis or differentiation in cancer cells. To study the activity of HD and the effect of potential inhibitors in vitro so far only radio-active assays have existed. For the search of new inhibitors and for the use in HD identification and purification we established a simple, non-radioactive assay that allows screening of large numbers of compounds. The assay is based on an aminocoumarin derivative of an Omega-acetylated lysine as enzyme substrate.
منابع مشابه
Histone deacetylase inhibitory and cytotoxic activities of the constituents from the roots of three species of Ferula
Objective(s): Histone deacetylase inhibitory and cytotoxic activities of 18 naturally occuring terpenoids (ferutinin, stylosin, tschimgine and guaiol), coumarins (umbelliprenin, farnesiferone B, conferone, feselol, ligupersin A, conferdione, conferoside) and sulfur-containing derivatives (latisulfies A-E, persicasulphides A and C) from the roots of three species of Ferula (Ferula latisecta, Fer...
متن کاملEffect of trichostatin A on histone deacetylase 1 (HDAC 1) and CIP/KIP (p21CIP1/WAF1, p27KIP1, and p57KIP2) gene expression, cell growth inhibition and apoptosis induction in lung cancer COR-L105 cell line. Abstract
Effect of trichostatin A on histone deacetylase 1 (HDAC 1) and CIP/KIP (p21CIP1/WAF1, p27KIP1, and p57KIP2) gene expression, cell growth inhibition and apoptosis induction in lung cancer COR-L105 cell line. Abstract Background: Lung cancer is one the leading cause of cancer-related death worldwide, with more than 1.2 million deaths each year. In addition to genetic mutations, epigenetic modif...
متن کاملSearch for the Pharmacophore of Histone Deacetylase Inhibitors Using Pharmacophore Query and Docking Study
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...
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...
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...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
عنوان ژورنال:
- Nucleic acids research
دوره 27 9 شماره
صفحات -
تاریخ انتشار 1999