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Set7/9, also known as SETD7, is a lysine-specific histone methyltransferase that plays a crucial role in the regulation of gene expression through the methylation of histone and non-histone proteins. This enzyme is involved in various cellular processes, including stemness, differentiation, and development.
Set7/9 was first identified in 2001 when it was purified and characterized from the human cervical cancer cell line HeLa . The enzyme contains a SET domain, which is responsible for its methyltransferase activity. The SET domain is a conserved region found in many proteins across different species, indicating its evolutionary importance .
Set7/9 specifically monomethylates lysine 4 on histone H3 (H3K4me1), a modification associated with transcriptional activation . The enzyme forms a complex with S-adenosyl-L-methionine (SAM), which serves as the methyl group donor. The active site of Set7/9 includes a binding pocket for SAM and a narrow substrate-specific channel that only allows unmethylated lysine residues to access .
In addition to histone methylation, Set7/9 also methylates several non-histone proteins, including p53, pRb, YAP, DNMT1, SOX2, and FOXO3 . These modifications play a significant role in regulating various cellular functions, such as cell cycle progression, apoptosis, and stem cell maintenance.
The methylation of histones by Set7/9 is essential for the regulation of chromatin structure and gene expression. This process influences various biological processes, including embryogenesis, tissue development, and cellular differentiation . The balance between cellular stemness and differentiation is crucial for the development of multicellular organisms, and Set7/9 plays a pivotal role in maintaining this balance .
Aberrant activity of Set7/9 has been linked to several pathological conditions, including cancer. The enzyme’s role in regulating the methylation of non-histone proteins, such as p53 and pRb, suggests that it may contribute to the formation and maintenance of cancer stem cells . Understanding the function and regulation of Set7/9 could provide valuable insights into the development of therapeutic strategies for cancer and other diseases associated with abnormal cellular differentiation and self-renewal.