Design and Synthesis of Dual EZH2/BRD4 Inhibitors to Target Solid Tumors.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c01876
Abstract: EZH2 inhibitors that prevent trimethylation of histone lysine 27 (H3K27) are often limited to the treatment of a subset of hematological malignancies. In most solid tumors, EZH2 inhibitors induce reciprocal H3K27 acetylation that subsequently results… read more here.
Keywords: design synthesis; ezh2; ezh2 brd4; brd4 inhibitors ... See more keywords
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
Therapeutic Targeting of EZH2 and BET BRD4 in Pediatric Rhabdoid Tumor.
Sign Up to like & getrecommendations! Published in 2022 at "Molecular cancer therapeutics"
DOI: 10.1158/1535-7163.mct-21-0646
Abstract: Aberrant activity of the H3K27 modifiers EZH2 and BRD4 is an important oncogenic driver for atypical teratoid/rhabdoid tumor (AT/RT), and each is potentially a possible therapeutic target for treating AT/RT. We therefore determined whether targeting… read more here.
Keywords: cell; targeting ezh2; ezh2 brd4; rhabdoid tumor ... See more keywords