SETD6 Activators

SETD6, or SET Domain Containing 6, is a protein encoded by the SETD6 gene in humans. It belongs to the SET domain protein family, which is known for its involvement in histone modification and chromatin remodeling. Histone modifications play a critical role in regulating gene expression and DNA repair, influencing a wide range of cellular processes.SETD6 is characterized by its SET domain, a region involved in the methylation of histone proteins. Specifically, SETD6 acts as a histone methyltransferase that primarily targets histone H2A. It adds a methyl group to lysine 20 of histone H2A (H2AK20me1), a modification that has implications for the structure and function of chromatin.

The methylation of histones by SETD6 is associated with the regulation of gene expression. This modification can influence how tightly DNA is wound around histones, affecting the accessibility of DNA to transcription factors and, consequently, the transcription of genes. Through this mechanism, SETD6 plays a role in controlling various cellular processes, including cell cycle progression, development, and differentiation.In addition to its role in histone modification, there is growing interest in the involvement of SETD6 in various diseases, particularly in cancer. Aberrant histone modification patterns are a hallmark of many cancers, and enzymes like SETD6 that regulate these modifications can contribute to the development and progression of cancer.