BIX 01294, histone methyltransferase inhibitor

Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

EHMT1 also known as GLP (G9a-like protein) is a histone methyltransferase involved in the methylation of histone H3 on lysine 9 a modification leading to transcriptional repression. The EHMT1 protein has a mass of approximately 150 kDa and is expressed in numerous tissues including the brain and heart. It functions as part of a larger complex and acts in the modification of chromatin structure and gene expression regulation.

Biological function summary

EHMT1/GLP plays a critical role in cellular processes such as development and differentiation. It forms a complex with G9a another histone methyltransferase to facilitate these functions. This complex cooperates in controlling gene silencing and the preservation of cellular identity. Such complex mechanisms lead to alterations in gene expression patterns that are essential for normal cellular operation.

Pathways

The methylation activity of EHMT1/GLP participates in the epigenetic regulation pathway and chromatin remodeling pathways. Within these pathways it interacts closely with proteins like HP1 which binds to methylated histones to promote gene silencing. The connections with pathways that influence gene expression affirm its role in maintaining cellular processes like proliferation and embryonic development.

Researchers connect EHMT1/GLP to Kleefstra syndrome—a condition characterized by intellectual disability and developmental delays. It is also associated with some cancer types due to its epigenetic regulation influences. In these contexts abnormal EHMT1/GLP activity often involving other proteins like G9a can contribute to the disruptions in gene regulation that lead to disease manifestations.