What does PRC2 complex do?

What does PRC2 complex do?

PRC2 is involved in various biological processes, including differentiation, maintaining cell identity and proliferation, and stem-cell plasticity. Recent studies of PRC2 have expanded our perspectives on its function and regulation, and uncovered a role for non-coding RNA in the recruitment of PRC2 to target genes.

Which is the PRC complex that contains the enzyme with H3K27 methyltransferase activity?

The PRC2 complex comprises four core subunits including EZH2 (or EZH1), Suppressor of Zeste 12 (SUZ12), Embryonic Ectoderm Development (EED) and Retinoblastoma protein associated protein 46/48 (RbAp46/48) and this complex has been shown to be involved in the methylation of H3K27 [62–64].

Is PRC2 a methyltransferase?

PRC2 is a methyltransferase with activity toward lysine 27 on histone H3 (H3K27). The SET-domain-containing component (EZH1 or EZH2) is closely associated with several other subunits.

What is heterochromatin euchromatin?

Heterochromatin is defined as the area of the chromosome which is darkly stained with a DNA specific stain and is in comparatively condensed form. Euchromatin is defined as the area of the chromosome which is rich in gene concentration and actively participates in the transcription process.

What is PRC1 and PRC2?

PRC2 (polycomb repressive complex 2) is one of the two classes of polycomb-group proteins or (PcG). The other component of this group of proteins is PRC1 (Polycomb Repressive Complex 1). PRC2 has a role in X chromosome inactivation, in maintenance of stem cell fate, and in imprinting.

What is polypolycomb Repressive Complex 2 (PRC2)?

Polycomb repressive complex 2 (PRC2) is one of the two PcG proteins core complexes and mediates gene silencing mostly by modulating chromatin structure [ 1 ]. EZH2 is an enzymatic catalytic subunit of PRC2 that can alter gene expression by trimethylation of Lys-27 in histone 3 (H3K27me3) [ 2 ].

Are there any novel inhibitors of PRC2?

Thus, development of novel inhibitors against other components of PRC2 has gained attention, as demonstrated by the development of EED inhibitors ( 33, 35–38 ). One of EED inhibitors is currently in clinical trial ( NCT02000651 ).

How does PRC2 activity affect cancer risk?

Increased activity of PRC2 results in high global levels of H3K27me3, which are linked to different types of cancer, including lymphoma, prostate, breast, and myeloma cancers ( 28 ). The importance of PRC2 linked to tumorigenesis has been validated by disrupting the PRC2 enzymatic activity using a number of EZH2 inhibitors ( 29–31 ).

Are pyrimidone compounds potent allosteric inhibitors of PRC2?

The WD40 repeat-containing protein EED is a core component of PRC2 and enhances PRC2 activity through interaction with H3K27me3. In this study, we report the discovery of a class of pyrimidone compounds, represented by BR-001, as potent allosteric inhibitors of PRC2.