5H24

EED in complex with PRC2 allosteric inhibitor compound 8

Summary for 5H24

• Entry DOI: 10.2210/pdb5h24/pdb
• Related: 5H13 5H14 5H15 5H17 5H19 5H25
• Descriptor: Polycomb protein EED, Histone-lysine N-methyltransferase EZH2, 5-(furan-2-ylmethylamino)-[1,2,4]triazolo[4,3-a]pyridine-6-carbonitrile, ... (4 entities in total)
• Functional Keywords: eed, prc2, inhibitor, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• Biological source: Homo sapiens (Human); More
• Cellular location: Nucleus: O75530 Q15910
• Total number of polymer chains: 4
• Total formula weight: 92435.29

Authors

Zhao, K.,Zhao, M.,Luo, X.,Zhang, H. (deposition date: 2016-10-14, release date: 2017-01-25, Last modification date: 2023-11-08)

• Primary citation: Huang, Y.,Zhang, J.,Yu, Z.,Zhang, H.,Wang, Y.,Lingel, A.,Qi, W.,Gu, J.,Zhao, K.,Shultz, M.D.,Wang, L.,Fu, X.,Sun, Y.,Zhang, Q.,Jiang, X.,Zhang, J.,Zhang, C.,Li, L.,Zeng, J.,Feng, L.,Zhang, C.,Liu, Y.,Zhang, M.,Zhang, L.,Zhao, M.,Gao, Z.,Liu, X.,Fang, D.,Guo, H.,Mi, Y.,Gabriel, T.,Dillon, M.P.,Atadja, P.,Oyang, C.; Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy; J. Med. Chem., 60:2215-2226, 2017; PubMed: 28092155; DOI: 10.1021/acs.jmedchem.6b01576

Experimental method

X-RAY DIFFRACTION (2.5 Å)