Liver X receptors (LXRs) are nuclear receptors that regulate the metabolism of cholesterol and bile acids. LXRs function as nuclear cholesterol sensors that are activated in response to elevated intracellular cholesterol levels in multiple cell types.
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Classical histone deacetylases (HDACs classes I, II, and IV) are a promising novel class of epigenetic anti-cancer drug targets. Inhibition of histone deacetylases results in hyperacetylation of histones and modulates gene expression by creating an open chromatin state that leads to expression of previously silenced genes.
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Histone methyltransferases are promising epigenetic drug targets. Several drugs that inhibit histone methyltransferases have been developed for anticancer therapy. DOT1L histone H3 methyltransferase methylates lysine 79 on histone H3 (H3K79), within the globular histone domain upon which DNA is wrapped.
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