Du, Daohai published the artcileStructure-Guided Development of Small-Molecule PRC2 Inhibitors Targeting EZH2-EED Interaction, Name: 1-(Chloromethyl)-4-(trifluoromethyl)benzene, the publication is Journal of Medicinal Chemistry (2021), 64(12), 8194-8207, database is CAplus and MEDLINE.
The cocrystal structure of EZH2-embryonic ectoderm development (EED) in complex with astemizole at 2.15 Å was reported. The structure elucidated the detailed binding mode of astemizole to EED and provided a structure-guided design for the discovery of a novel EZH2-EED interaction inhibitor, DC-PRC2in-01 I, with an affinity Kd of 4.56μM. DC-PRC2in-01 I destabilized the PRC2 complex, thereby leading to the degradation of PRC2 core proteins and the decrease of global H3K27me3 levels in cancer cells. The proliferation of PRC2-driven lymphomas cells was effectively inhibited, and the cell cycle was arrested in the G0/G1 phase. Together, these data demonstrated that DC-PRC2in-01 I could be an effective chem. probe for investigating the PRC2-related physiol. and pathol. and providing a promising chem. scaffold for further development.
Journal of Medicinal Chemistry published new progress about 939-99-1. 939-99-1 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Benzyl chloride,Benzene, name is 1-(Chloromethyl)-4-(trifluoromethyl)benzene, and the molecular formula is C8H6ClF3, Name: 1-(Chloromethyl)-4-(trifluoromethyl)benzene.
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