Fig. 3
From: Small molecules in targeted cancer therapy: advances, challenges, and future perspectives
Commonly altered epigenetic regulatory proteins implicated in cancer. Gene silencing in mammalian cells is usually caused by methylation of DNA CpG islands as well as hypermethylation or hypoacetylation of histones. The writers (DNMTs, HATs, and HMTs) refer to enzymes that transfer chemical groups to DNA or histones; the erasers (HDACs and KDMs) are enzymes responsible for removing chemical groups from histones; the proteins (MBDs and BET family proteins) that can recognize the methyl-CpGs and modified histones are readers. Mutated IDH1/2 catalyzes the reduction of α-KG to 2-HG, which inhibits the activity of TET and lysine demethylases, resulting in DNA hypermethylation and increased histone lysine methylation. Figure created with BioRender.com
