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Methylated CpG dinucleotide in DNA refers to the addition of a methyl group to the cytosine base of a CpG site, producing 5-methylcytosine in double-stranded DNA[3][5][6]. This is a key epigenetic modification in vertebrates and is catalyzed by DNA methyltransferase enzymes[3]. Methylation at CpG sites is involved in the regulation of gene expression, often leading to the silencing of genes when present in gene promoters or CpG islands[2][4][5]. The methylation pattern plays a critical role in genomic imprinting, embryonic development, X-chromosome inactivation, and cell differentiation[4][5]. Aberrant CpG methylation patterns are associated with a variety of diseases, especially cancer (via promoter hypermethylation or hypomethylation leading to oncogene/tumor suppressor misregulation), as well as neurodevelopmental and aging-related disorders[5]. Although "methylated CpG dinucleotide in DNA" is not itself a therapeutic target (like a receptor, enzyme, or transporter), it is a structural motif recognized by specific proteins (e.g., methyl-CpG binding domain proteins) and is the functional site of action for certain epigenetic drugs[1][4][5]. Thus, the entry is not a conventional target, but rather a biomolecular modification central to epigenetic regulation and disease pathology.
Inhibition of DNA methyltransferases, resulting in hypomethylation, reactivation of silenced genes, induction of apoptosis
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