Histone Methylation by PRC2 Is Inhibited by Active Chromatin Marks

Frank W. Schmitges, Archana Bairavasundaram Prusty, Mahamadou Faty, +18

Molecular Cell

Histone ModificationsChromatinChromatin RemodelingMedicineGenetics +12

Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation

Wei Qi, Homan Chan, Lin Teng, +24

Proceedings of the National Academy of Sciences

Selective InhibitionTumor BiologyMethyl GroupLymphoid NeoplasiaOncology +13

Disordered methionine metabolism in MTAP/CDKN2A-deleted cancers leads to dependence on PRMT5

Konstantinos J. Mavrakis, E. Robert McDonald, Michael R. Schlabach, +41

Science

An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED

Wei Qi, Kehao Zhao, Justin Gu, +37

Nature Chemical Biology

Signal TransductionSignaling PathwayCell RegulationReceptor Tyrosine KinaseReceptor (Biochemistry) +5

Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy

Ying Huang, Jeff Zhang, Zhengtian Yu, +31

Journal of Medicinal Chemistry

NSD2 Is Recruited through Its PHD Domain to Oncogenic Gene Loci to Drive Multiple Myeloma

Zheng Huang, Haiping Wu, Shannon Chuai, +25

Cancer Research

Structure of Human SMYD2 Protein Reveals the Basis of p53 Tumor Suppressor Methylation

Li Wang, Ling Li, Hailong Zhang, +8

Journal of Biological Chemistry

Structure-Guided Design of EED Binders Allosterically Inhibiting the Epigenetic Polycomb Repressive Complex 2 (PRC2) Methyltransferase

Andreas Lingel, Martin Sendzik, Ying Huang, +24

Journal of Medicinal Chemistry

Histone ModificationsEed Binders AllostericallyEpigenetic ChangeMolecular BiologyEpigenetics +19

Discovery and Molecular Basis of a Diverse Set of Polycomb Repressive Complex 2 Inhibitors Recognition by EED

Ling Li, Hailong Zhang, Man Zhang, +24

PLoS ONE

Histone ModificationsHistone H3Drug TargetEpigenetic ChangeNovel Eed Binder +22

Discovery of the Clinical Candidate MAK683: An EED-Directed, Allosteric, and Selective PRC2 Inhibitor for the Treatment of Advanced Malignancies

Ying Huang, Martin Sendzik, Jeff Zhang, +38

Journal of Medicinal Chemistry