Inhibitors of enzymes catalyzing modifications to histone lysine residues: structure, function and activity

作者: Ryan Lillico , Nicholas Stesco , Tina Khorshid Amhad , Claudia Cortes , Mike P Namaka

DOI: 10.4155/FMC-2016-0021

关键词:

摘要: Gene expression is partly controlled by epigenetic mechanisms including histone-modifying enzymes. Some diseases are caused changes in gene that can be mitigated inhibiting This review covers the enzyme inhibitors targeting histone lysine modifications. We summarize enzymatic of acetylation, deacetylation, methylation and demethylation discuss biochemical roles these modifications disease. defining their structure-activity relationships potential mechanisms. show there potentially indiscriminant off-target effects on even with use selective inhibitors.

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