Screening for Histone Deacetylase (HDAC) Active Compounds - a poster from the SLAS 2014 poster series.
Introduction:
Histones are small basic proteins. DNA in a stacked configuration is bound around histones to build chromatin prior the replication procedure.
After translation, histone side chains are often modified. This includes acetylation and deacetylation as well as methylation, ADP-ribosylation, and phosphorylation.1 Histone deacetylation is carried out by enzymes that build a complex with histones. These complexes target specific promoters to repress transcription through deacetylation of histones in specific nucleosomes.2HDAC inhibitors (HDACi) have been used to treat neurological symptoms, as well as cancers, parasitic and inflammatory disease.
In order to find compounds that are potential inhibitors of HDAC activity (Class I and II), a chemiluminescent Proof-of-Concept Screen was performed on the PHERAstar FS microplate reader from BMG LABTECH.Assay PrincipleThe HDAC-Glo™ I/II assay from Promega measures the activity of HDAC class I and II.
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