HDAC8 substrates: Histones and beyond
نویسندگان
چکیده
منابع مشابه
Invited Review HDAC8 Substrates: Histones and Beyond
A cetylation of lysine side chains in proteins is a reversible post-translational modification that occurs in a wide range of organisms. This modification affects the properties of proteins, including protein–protein association, protein–DNA interactions, and protein stability. Initially, acetylation gained recognition as a post-translational modification to histones. Acetylation of histones ca...
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Posttranslational modifications (PTMs) of histone proteins, such as acetylation, methylation, phosphorylation, and ubiquitylation, play essential roles in regulating chromatin dynamics. Combinations of different modifications on the histone proteins, termed 'histone code' in many cases, extend the information potential of the genetic code by regulating DNA at the epigenetic level. Many PTMs occ...
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This paper introduces a flexible assay for characterizing the activities of the histone deacetylase enzymes. The approach combines mass spectrometry with self-assembled monolayers that present acetylated peptides and enables a label-free and one-step assay of this biochemical activity. The assay was used to characterize the activity of HDAC8 toward peptides taken from the N-terminal tail of the...
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In the past years, a lot of attention has been given to the identification and characterization of selective and potent inhibitors of chromatin-modifying enzymes to better understand their specific role in transcriptional regulation. As aberrant histone methylation is involved in different pathological processes, the search for methyltransferase and demethylase inhibitors has emerged as a cruci...
متن کاملInhibition and Mechanism of HDAC8 Revisited
Histone deacetylases (HDACs) have found intense interest as drug targets for a variety of diseases, but there is disagreement about basic aspects of the inhibition and mechanism of HDACs. QM/MM calculations of HDAC8 including a large QM region provide a model that is consistent with the available crystal structures and structure-activity relationships of different HDAC inhibitors. The calculati...
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ژورنال
عنوان ژورنال: Biopolymers
سال: 2012
ISSN: 0006-3525
DOI: 10.1002/bip.22135