Epigenetic modifications of histones such as acetylation cause conformational changes in the chromatin structure, thereby regulating transcriptional activity. Histone acetyltransferases (HATs) and histone deacetylases (HDACs) are enzymes responsible for such post-translational modification of core histones. HDACs remove acetyl groups from lysine residues and are separated into four categories: Class I (HDAC1, 2, 3 & 8), Class II (HDAC4-9), Class III (SIRT1-7) and Class IV (HDAC11). Class I, II, and IV are zinc-dependent deacetylases while class III is NAD-dependent. HDACs have been shown to play a significant role in the development of neurodegenerative and metabolic disorders. Thus, HDAC modulators could provide viable treatment options and are currently targeted for drug discovery.
What We Offer
SAMDI Tech offers a plug-and-play format for quantitative analysis of deacetylase activity using native substrates. Native peptide and protein substrates can be captured and purified onto SAMDI 384 or 1536 biochip arrays for analysis by mass spectrometry. No need for cumbersome fluorescent-labeled substrates that can interfere with activity and lead to increase false positive rates. SAMDI has the capability to monitor all acetylation states simultaneously in a single assay.