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Lysine methyltransferase 5C (KMT5C), also known as SUV420H2, is an enzyme that plays a pivotal role in epigenetic regulation by specifically catalyzing the trimethylation of histone H4 at lysine 20 (H4K20me3) (UniProt Q86V97). This histone modification is a hallmark of constitutive heterochromatin and is essential for maintaining genomic stability, proper chromosome segregation, and the DNA damage response (PubMed: 28115311). KMT5C is frequently dysregulated in various malignancies; for example, reduced levels of H4K20me3 are often observed in cancer progression and are associated with increased genomic instability and epithelial-mesenchymal transition (PubMed: 25100700). While no drugs targeting KMT5C are currently approved for clinical use, small molecule inhibitors such as A-196 have been developed as chemical probes to study its function and therapeutic potential in oncology (Nature Chemical Biology, 2017). Targeting the KMT5C mRNA through RNA-based technologies like siRNA or antisense oligonucleotides represents a strategy to modulate these epigenetic pathways for therapeutic benefit (NCBI Gene: 84787).
Inhibition of histone methyltransferase activity; mRNA degradation via RNA interference
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