Journal
MOLECULAR DIVERSITY
Volume 15, Issue 2, Pages 401-416Publisher
SPRINGER
DOI: 10.1007/s11030-010-9299-5
Keywords
Histone acetyltransferases; Natural compounds; Polyisoprenylated benzophenone derivatives; Anacardic acid; Polyphenols
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Histone acetyltransferases (HATs) are a class of epigenetic enzymes crucial for chromatin restructuring and transcriptional regulation in eukaryotic cells, thus being a promising target for therapeutic development. Nonetheless, differently from histone deacetylases (HDACs) inhibitors, there is still paucity of small-molecule modulators of HAT activity. After a decline during past decade, natural products and their derivatives could be once again a valuable tool in the lead discovery process and meet such need of Novel Chemical Entities (NCEs). In this review, we will provide a comprehensive summary on the discovery of small-molecule HAT modulators from naturally occurring molecular scaffolds.
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