Design, Synthesis, and Biological Evaluation of a Potent Dual EZH2-BRD4 Inhibitor for the Treatment of Some Solid Tumors.
Sign Up to like & getrecommendations! Published in 2023 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01607
Abstract: Enhancer of zeste homolog 2 (EZH2) mediates the trimethylation of histone 3 lysine 27 (H3K27) to promote gene silencing. Inhibition of EZH2 is a viable strategy for cancer treatment; however, only a small subset of… read more here.
Keywords: ezh2; ezh2 brd4; solid tumors; treatment ... See more keywords
Design of First-in-Class Dual EZH2/HDAC Inhibitor: Biochemical Activity and Biological Evaluation in Cancer Cells.
Sign Up to like & getrecommendations! Published in 2020 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.0c00014
Abstract: Since the histone modifying enzymes EZH2 and HDACs control a number of epigenetic-dependent carcinogenic pathways, we designed the first-in-class dual EZH2/HDAC inhibitor 5 displaying (sub)micromolar inhibition against both targets. When tested in several cancer cell… read more here.
Keywords: class dual; dual ezh2; ezh2 hdac; hdac inhibitor ... See more keywords