Polycomb Group (PcG) proteins play a vital role in establishing and maintaining gene expression patterns during cellular differentiation and development. PcG proteins function as multimeric, chromatin-associated protein complexes and are responsible for the repression of target genes. The two major Polycomb Repressive Complexes in mammals namely, PRC2 and PRC1 regulate the epigenome through methylation of histone H3K27. The major components of human PRC2 include the histone methyltransferase, Enhancer of Zeste Homolog 2 (EZH2), and its known binding partners, Embryonic Ectoderm Development (EED) and Suppressor of Zeste 12 (SUZ12). The leading hypothesis regarding the PRC2 and PRC1 interaction is that PRC2-mediated tri-methylation of H3K27 recruits PRC1 to genomic loci leading to chromatin condensation and epigenetic silencing of target genes. EED, previously considered a critical component of PRC2, is instead a shared component of PRC2 and PRC1 that functions to interchange these epigenetic complexes at sites of histone modification. This observation markedly enhances our understanding of how PRC2 and PRC1 coordinate epigenetic regulation and may have implications in therapeutically targeting these master regulators of transcription. Here you can see a recent crystal structure of human EED protein in complex with a small organic inhibitor (PDB code: 7SI4)
#molecularart ... #immolecular ... #repressor ... #polycomb ... #EED ... #histone ... #transcription .. #inhibitor ... #xray
Structure rendered with @proteinimaging and depicted with @corelphotopaint
#molecularart ... #immolecular ... #repressor ... #polycomb ... #EED ... #histone ... #transcription .. #inhibitor ... #xray
Structure rendered with @proteinimaging and depicted with @corelphotopaint
