Abstract
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.
MeSH terms
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Alkaloids / chemistry
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Alkaloids / metabolism
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Anacardic Acids / chemistry
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Anacardic Acids / metabolism
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Animals
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Benzophenones / chemistry
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Benzophenones / metabolism
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Benzoquinones / chemistry
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Benzoquinones / metabolism
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Biological Products / chemistry*
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Biological Products / metabolism*
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Enzyme Inhibitors / chemistry*
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Enzyme Inhibitors / metabolism*
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Flavonoids / chemistry
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Flavonoids / metabolism
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Histone Acetyltransferases / antagonists & inhibitors*
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Histone Acetyltransferases / metabolism*
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Humans
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Peptides / chemistry
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Peptides / metabolism
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Phenols / chemistry
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Phenols / metabolism
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Polyphenols
Substances
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Alkaloids
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Anacardic Acids
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Benzophenones
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Benzoquinones
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Biological Products
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Enzyme Inhibitors
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Flavonoids
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Peptides
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Phenols
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Polyphenols
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polyisoprenyl benzophenone
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quinone
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Histone Acetyltransferases