gsk-2816126 and Triple-Negative-Breast-Neoplasms

gsk-2816126 has been researched along with Triple-Negative-Breast-Neoplasms* in 1 studies

Other Studies

1 other study(ies) available for gsk-2816126 and Triple-Negative-Breast-Neoplasms

Article	Year
Discovery of precision targeting EZH2 degraders for triple-negative breast cancer. European journal of medicinal chemistry, 2022, Aug-05, Volume: 238 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

Article

Year

Discovery of precision targeting EZH2 degraders for triple-negative breast cancer.

European journal of medicinal chemistry, 2022, Aug-05, Volume: 238

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