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- W3119832823 abstract "Abstract Histones control gene expression by regulating chromatin structure and function. The posttranslational modifications (PTMs) on the side chains of histones form the epigenetic landscape, which is tightly controlled by epigenetic modulator enzymes and further recognized by so-called reader domains. Histone microarrays have been widely applied to investigate histone–reader interactions, but not the transient interactions of Zn 2+ -dependent histone deacetylase (HDAC) eraser enzymes. Here, we synthesize hydroxamic acid-modified histone peptides and use them in femtomolar microarrays for the direct capture and detection of the four class I HDAC isozymes. Follow-up functional assays in solution provide insights into their suitability to discover HDAC substrates and inhibitors with nanomolar potency and activity in cellular assays. We conclude that similar hydroxamic acid-modified histone peptide microarrays and libraries could find broad application to identify class I HDAC isozyme-specific substrates and facilitate the development of isozyme-selective HDAC inhibitors and probes." @default.
- W3119832823 created "2021-01-18" @default.
- W3119832823 creator A5035890430 @default.
- W3119832823 creator A5041984050 @default.
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- W3119832823 creator A5056161844 @default.
- W3119832823 creator A5059071312 @default.
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- W3119832823 date "2021-01-04" @default.
- W3119832823 modified "2023-10-11" @default.
- W3119832823 title "Hydroxamic acid-modified peptide microarrays for profiling isozyme-selective interactions and inhibition of histone deacetylases" @default.
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- W3119832823 doi "https://doi.org/10.1038/s41467-020-20250-9" @default.
- W3119832823 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/7782793" @default.
- W3119832823 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/33397936" @default.
- W3119832823 hasPublicationYear "2021" @default.
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