EZH2 contributes to the response to PARP inhibitors through its PARP …
Jan 11, 2018 · To enhance the clinical response to PARP inhibitors (PARPis), understanding the mechanisms underlying PARPi sensitivity is urgently needed. Here, we show enhancer of zeste homolog 2 (EZH2), an enzyme that catalyzes H3 lysine trimethylation and associates with oncogenic function, contributes to PARPi sensitivity in breast cancer cells.
EZH2 directly methylates PARP1 and regulates its activity in cancer
Nov 27, 2024 · Here, we report that enhancer of zeste homolog 2 (EZH2) directly methylates poly (adenosine diphosphate–ribose) polymerase-1 (PARP-1), an essential enzyme involved in DNA repair, and regulates its activity.
Combined inhibition of PARP and EZH2 for cancer treatment: …
Oct 3, 2022 · Tumors with BRCA1/2 mutations or homologous recombination repair defects are sensitive to PARP inhibitors through the mechanism of synthetic lethality. Several PARP inhibitors are currently approved for ovarian, breast and pancreatic cancer in clinical practice. However, more than 40% of patients wi …
EZH2 contributes to the response to PARP inhibitors through its PARP …
Sep 18, 2017 · In contrast, inhibition of PARP by PARPi attenuates alkylating DNA damage-induced EZH2 downregulation, thereby promoting EZH2-mediated gene silencing and cancer stem cell property compared with ...
Dual target PARP1/EZH2 inhibitors inducing excessive autophagy …
Feb 5, 2024 · EZH2 is a leading candidate of epigenetic modulators associated with the TNBC subtype, when the function of EZH2 is inhibited or silenced, the sensitivity of serous ovarian cancer cells with high expression of coactivator-associated arginine methyltransferase 1 (CARM1) to PARP inhibitors is enhanced, resulting in cell mitotic disorder and cell ...
Discovery of First-in-Class Dual PARP and EZH2 Inhibitors for …
Sep 1, 2021 · PARP inhibitors have highly significant effects on BRCA mutant cells, allowing targeted therapy of triple-negative breast cancer (TNBC). However, some TBNC patients lack BRCA mutations. Recent studies have shown that EZH2 inhibitors can increase the sensitivity of wild-type BRCA cells to PARP inhibi …
EZH2 inhibition sensitizes MYC-high medulloblastoma cancers to PARP …
Nov 19, 2024 · In this study, we investigated the combined effects of EZH2 and PARP inhibitors in MYC-high medulloblastoma and demonstrated that EZH2 inhibition significantly increased the sensitivity of MYC ...
Combined inhibition of PARP and EZH2 for cancer treatment: …
Oct 2, 2022 · This review summarizes the interactions between EZH2 and PARP, suggests the potential PARP inhibitor sensitization effect of EZH2 inhibitors, and further discusses the potential populations that benefit from the combination of EZH2 inhibitors and PARP inhibitors.
Nov 27, 2024 · Meanwhile, EZH2- mediated methylation regu-lates PARP1 transcriptional and oncogenic activity, at least in part, through impairing PARP1- E2F1 interaction and E2F1 transcription factor activity. EZH2 and PARP1 inhibitors …
Discovery of First-in-Class Dual PARP and EZH2 Inhibitors for …
Aug 29, 2021 · PARP inhibitors have highly significant effects on BRCA mutant cells, allowing targeted therapy of triple-negative breast cancer (TNBC). However, some TBNC patients lack BRCA mutations. Recent studies have shown that EZH2 inhibitors can increase the sensitivity of wild-type BRCA cells to PARP inhibitors. We designed a series of dual PARP and EZH2 inhibitors, and the most promising compound, 5a ...