Structure-Based Identification of HDAC8 Non-histone Substrates
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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Histone deacetylases (HDACs) are a growing family of enzymes implicated in transcriptional regulation by affecting the acetylation state of core histones in the nucleus of cells. HDACs are known to have key roles in the regulation of cell proliferation [Brehm, Miska, McCance, Reid, Bannister and Kouzarides (1998) Nature (London) 391, 597-600], and aberrant recruitment of an HDAC complex has bee...
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Histone deacetylase 8 (HDAC8) is an enzyme involved in deacetylating the amino groups of terminal lysine residues, thereby repressing the transcription of various genes including tumor suppressor gene. The over expression of HDAC8 was observed in many cancers and thus inhibition of this enzyme has emerged as an efficient cancer therapeutic strategy. In an effort to facilitate the future discove...
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HDAC8 inhibitors have become an attractive treatment for cancer. This study aimed to facilitate the identification of potential chemical scaffolds for the selective inhibition of histone deacetylase 8 (HDAC8) using in silico approaches. Non-linear QSAR classification and regression models of HDAC8 inhibitors were developed with support vector machine. Mean impact value-based sequential forward ...
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Histone deacetylases 8 (HDAC8) is an enzyme repressing the transcription of various genes including tumour suppressor gene and has already become a target of human cancer treatment. In an effort to facilitate the discovery of HDAC8 inhibitors, two quantitative structure-activity relationship (QSAR) classification models were developed using K nearest neighbours (KNN) and neighbourhood classifie...
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ژورنال
عنوان ژورنال: Structure
سال: 2016
ISSN: 0969-2126
DOI: 10.1016/j.str.2016.02.002