Selective sensitivity of EZH2 inhibitors based on synthetic lethality in ARID1A-deficient gastric cancer
Sign Up to like & getrecommendations! Published in 2020 at "Gastric Cancer"
DOI: 10.1007/s10120-020-01094-0
Abstract: Background AT-rich interactive domain 1A ( ARID1A ) is a tumor suppressor gene that is frequently mutated in gastric cancer (GC). Although ARID1A mutations are not a druggable target for conventional treatments, novel therapeutic strategies… read more here.
Keywords: deficient; ezh2 inhibitors; arid1a deficient; cancer ... See more keywords
Discovery of Dual Lysine Methyltransferase G9a and EZH2 Inhibitors with In Vivo Efficacy against Malignant Rhabdoid Tumor.
Sign Up to like & getrecommendations! Published in 2023 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.3c00003
Abstract: In recent years, it has been proposed that G9a/EZH2 dual inhibition is a promising cancer treatment strategy. Herein, we present the discovery of G9a/EZH2 dual inhibitors that merge the pharmacophores of G9a and EZH2 inhibitors.… read more here.
Keywords: g9a ezh2; tumor; rhabdoid tumor; ezh2 inhibitors ... See more keywords
SWI/SNF catalytic subunits’ switch drives resistance to EZH2 inhibitors in ARID1A-mutated cells
Sign Up to like & getrecommendations! Published in 2018 at "Nature Communications"
DOI: 10.1038/s41467-018-06656-6
Abstract: Inactivation of the subunits of SWI/SNF complex such as ARID1A is synthetically lethal with inhibition of EZH2 activity. However, mechanisms of de novo resistance to EZH2 inhibitors in cancers with inactivating SWI/SNF mutations are unknown.… read more here.
Keywords: ezh2 inhibitors; ezh2; swi snf; resistance ezh2 ... See more keywords
Intercept’s NASH hopes dashed
Sign Up to like & getrecommendations! Published in 2020 at "Nature Biotechnology"
DOI: 10.1038/s41587-020-0638-5
Abstract: NAtURe BioteChNology | VOL 38 | AuguST 2020 | 905–916 | www.nature.com/naturebiotechnology EZH2 drug resistance in lymphoma is also a puzzle. Later-stage tumors, under the pressure of therapy, may develop clones that can tolerate the… read more here.
Keywords: intercept nash; ezh2 inhibitor; ezh2 inhibitors; ezh2 ... See more keywords
EZH2 Inhibitors: The Unpacking Revolution
Sign Up to like & getrecommendations! Published in 2022 at "Cancer Research"
DOI: 10.1158/0008-5472.can-21-4311
Abstract: The methylation of lysine 27 on histone H3 (H3K27me3) is a chromatin mark associated with nucleosome condensation and gene expression silencing. EZH2 is a lysine methyltransferase that catalyzes H3K27me3. In this issue of Cancer Research,… read more here.
Keywords: inhibitors unpacking; ezh2 inhibitors; unpacking revolution;
EZH2 inhibitors reverse resistance to gefitinib in primary EGFR wild-type lung cancer cells
Sign Up to like & getrecommendations! Published in 2020 at "BMC Cancer"
DOI: 10.1186/s12885-020-07667-7
Abstract: Background Lung cancer is the leading cause of cancer-related deaths worldwide. Non-small cell lung cancer (NSCLC) is the most common type of lung cancer. In traditional anti-cancer therapy, epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitors… read more here.
Keywords: egfr wild; ezh2 inhibitors; cancer; cell ... See more keywords
Combining EZH2 inhibitors with other therapies for solid tumors: more choices for better effects.
Sign Up to like & getrecommendations! Published in 2023 at "Epigenomics"
DOI: 10.2217/epi-2022-0320
Abstract: EZH2 is an epigenetic regulator that methylates lysine 27 on histone H3 (H3K27) and is closely related to the development and metastasis of tumors. It often shows gain-of-function mutations in hematological tumors, while it is… read more here.
Keywords: therapies solid; combining ezh2; tumors choices; inhibitors therapies ... See more keywords
EZH2 inhibitors abrogate upregulation of trimethylation of H3K27 by CDK9 inhibitors and potentiate its activity against diffuse large B-cell lymphoma
Sign Up to like & getrecommendations! Published in 2019 at "Haematologica"
DOI: 10.3324/haematol.2019.222935
Abstract: Aberrant expression of CDK9/cyclin T1 has been found in diffuse large B-cell lymphoma (DLBCL), and suggests that CDK9 is a potential therapeutic target for DLBCL. Here, we firstly demonstrated that CDKI-73, a novel cyclin-dependent kinases… read more here.
Keywords: cdk9 inhibitors; ezh2 inhibitors; cdk9; trimethylation h3k27 ... See more keywords
Combined inhibition of PARP and EZH2 for cancer treatment: Current status, opportunities, and challenges
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Pharmacology"
DOI: 10.3389/fphar.2022.965244
Abstract: 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.… read more here.
Keywords: parp inhibitor; parp; parp inhibitors; resistance ... See more keywords