Novel orally bioavailable EZH1/2 dual inhibitors with greater antitumor efficacy than an EZH2 selective inhibitor - Honma, Daisuke; Kanno, Osamu; Watanabe, Jun; Kinoshita, Junzo; Hirasawa, Makoto; Nosaka, Emi; Shiroishi, Machiko; Takizawa, Takeshi; Yasumatsu, Isao; Horiuchi, Takao; Nakao, Akira; Suzuki, Keisuke; et al. (Cancer science, 2017)
Keywords: Administration, Oral; AML1 protein; Animals; Antitumor activity; Binding sites; Bioavailability; Biological Availability; Cancer; Cell differentiation; Cell Line, Tumor; Cell proliferation; Cell Proliferation - drug effects; Cell Survival - drug effects; Chromatin remodeling; Colorectal cancer; Drug Screening Assays, Antitumor - methods; Dual inhibitor; Employees; Enhancer of Zeste Homolog 2 Protein - antagonists & inhibitors; Enhancer of Zeste Homolog 2 Protein - chemistry; EZH1; EZH2; Gene expression; H3K27me3; Histone H3; histone methyltransferase; Homocysteine; Humans; Lethality; Lymphocytes B; Lymphoma; Lysine; Methyltransferase; Models, Molecular; Multiple myeloma; Mutation; NMR; Nuclear magnetic resonance; Original; Ovarian cancer; Polycomb group proteins; Polycomb-Group Proteins - antagonists & inhibitors; Polycomb-Group Proteins - chemistry; Rats; Small Molecule Libraries - chemistry; Small Molecule Libraries - pharmacokinetics; Small Molecule Libraries - pharmacology; Stem cells; Structure-Activity Relationship; Sucrose; Therapeutic applications; Toxicity; Tumor cell lines; Tumorigenesis; Tumors; histone methyltransferase; Dual inhibitor; EZH1; EZH2; H3K27me3