epz-6438 has been researched along with Triple-Negative-Breast-Neoplasms* in 2 studies
2 other study(ies) available for epz-6438 and Triple-Negative-Breast-Neoplasms
| Article | Year |
|---|---|
Discovery of precision targeting EZH2 degraders for triple-negative breast cancer.
EZH2 is usually overexpressed in TNBC and other tumors, which has a great influence on the occurrence, development and prognosis of tumors. However, current EZH2 inhibitors, including Tazemetostat and GSK126, affect the methyl catalytic capacity of EZH2 and have little effect on the tumorigenic activity of EZH2 itself, resulting in poor efficacy against most solid tumors. Herein, we designed and optimized proteolytic targeting chimeras (PROTACs) precision targeting EZH2. The most active PROTAC molecule U3i has a high affinity for PRC2 complex (K Topics: Apoptosis; Enhancer of Zeste Homolog 2 Protein; Enzyme Inhibitors; Humans; Triple Negative Breast Neoplasms | 2022 |
CDK2-mediated site-specific phosphorylation of EZH2 drives and maintains triple-negative breast cancer.
Topics: Animals; Benzamides; Biphenyl Compounds; Bridged Bicyclo Compounds, Heterocyclic; Cyclic N-Oxides; Cyclin-Dependent Kinase 2; Enhancer of Zeste Homolog 2 Protein; Estrogen Receptor alpha; Female; Humans; Indolizines; Mammary Glands, Human; Mammary Neoplasms, Experimental; Mice; Mice, Transgenic; Morpholines; Phosphorylation; Pyridinium Compounds; Pyridones; Receptor, ErbB-2; Receptors, Progesterone; Triple Negative Breast Neoplasms | 2019 |