Jun 4, 2024 · The study identified genetic alterations in EZH2 itself, along with alterations that converge on RB1-E2F-mediated cell-cycle control, and demonstrated that inhibition of cell-cycle kinases, such as Aurora Kinase B (AURKB) could bypass EZH2 inhibitor resistance to enhance treatment efficacy.

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 …

tic drug-drug interactions, which allow for promising clinical implementation. This investigation aims to create novel compound combinations of Aurora kinase, EZH2, and BET inhibitors to determine whether pharmacotherapies such as these can efectively treat GB.

We demonstrate that N-Myc overexpression in multiple pre-clinical models drives aggressive prostate cancer that molecularly mimics clinical NEPC and sensitizes cells to the allosteric Aurora-A inhibitor MLN8237 and EZH2 SET domain inhibitors.

Mar 14, 2011 · EZH2 overexpression induces levels of Aurora A and B in asynchronized cultures, and upregulates p-Aurora A and B, p-Plk1, and the Aurora kinase substrate p-H3 Ser10 in nocodazole-treated cells.

Increased levels of EZH2, a critical regulator of cellular memory, signal the presence of metastasis and poor outcome in breast cancer patients. High levels of EZH2 are associated with nuclear...

Aug 5, 2022 · EZH2, the catalytic subunit of PRC2, catalyzes histone H3 lysine 27 (H3K27) trimethylation to induce the agglutination of chromosomes and in turn represses the transcription of the target genes. Numerous reports indicate that EZH2 is overexpressed in a variety of malignant tumor tissues.

We found that compared with in PN and NN tissues, the expression of FOXO1 is significantly repressed and the expression of AURKA, AURKB and EZH2 is significantly up-regulated in PP tissues (P < 0.001).

To investigate unexpected clusterings, sets of BTK, Aurora and PI3K inhibitors were profiled in biochemical enzyme activity assays and surface plasmon resonance binding assays. The BTK inhibitor ibrutinib clusters with EGFR inhibitors, because it cross-reacts with EGFR.

Dec 7, 2018 · This paper reviews the evidence supporting the role of EZH2 in MM pathophysiology and drug resistance, with an emphasis on interactions between EZH2 and microRNAs, as well as the prognostic significance of EZH2 expression in MM.