Feb 7, 2023 · Enhancer of zeste homolog 2 (EZH2) is the enzymatic subunit of polycomb repressive complex 2 (PRC2), which catalyzes trimethylation of histone H3 lysine 27 (H3K27me3) for transcriptional repression. EZH2 have been implicated in numerous hematological malignancies, including MM.

EZH2 is involved in the cell cycle, DNA damage repair, cell differentiation, autophagy, apoptosis, and immunological modulation. The main function of EZH2 is to catalyze the methylation of H3 histone of H3K27Me3, which inhibits the transcription of target …

Heterozygous point mutations of EZH2 occurring at tyrosine 641 (Y641) within the C-terminal catalytic SET domain of EZH2 are observed in 22% of germinal center B-cell (GCB) diffuse large B-cell lymphomas (DLBCL) and 7%—12% of follicular lymphomas (FL), and contribute to EZH2’s oncogenic potential.

Oct 2, 2020 · Increasing evidence shows that enhancer of zeste homolog 2 (EZH2), the catalytic subunit of PRC2, functions as an oncogene or tumor suppressor gene depending on the context.

To target EZH2-dependent cancers, we developed a novel and potent EZH2 inhibitor JQEZ5 that promoted the regression of EZH2-driven tumors in vivo, confirming oncogenic addiction to EZH2 in established tumors and providing the rationale for epigenetic therapy in a subset of lung cancer.

Aug 4, 2021 · While numerous studies have reported epigenetic functions of EZH2 that inhibit tumor suppressor genes and promote tumorigenesis, discordance between EZH2 and H3K27 methylation has been reported.

Oct 28, 2022 · To sustain prostate tumorigenicity, EZH2 establishes non-canonical biochemical interaction with AR for mediating oncogene activation, in addition to its canonical role as a transcriptional repressor and enzymatic subunit of Polycomb Repressive Complex 2 (PRC2).

Jan 7, 2025 · EZH2 is the enzymatically active subunit of the Polycomb Repressive Complex 2 (PRC2), a multi-protein complex mediating the formation and maintenance of heterochromatin. It deposits...

The Polycomb group (PcG) protein Enhancer of Zeste Homolog 2 (EZH2) is one of the three core subunits of the Polycomb Repressive Complex 2 (PRC2). It harbors histone methyltransferase activity (MTase) that specifically catalyze histone 3 lysine 27 …

Jan 7, 2025 · These non-canonical roles of EZH2 are considered as a part of its oncogenic activity. We discuss the experimental approaches undertaken to inhibit EZH2 activity, and dual inhibitors and degraders of EZH2 protein are reviewed in more detail.