5U5T

Crystal structure of EED in complex with H3K27Me3 peptide and 3-(benzo[d][1,3]dioxol-4-ylmethyl)piperidine-1-carboximidamide

Summary for 5U5T

• Entry DOI: 10.2210/pdb5u5t/pdb
• Related: 5U5H 5U5K 5U62
• Descriptor: Polycomb protein EED, Histone-lysine N-methyltransferase EZH2, (3R)-3-[(2H-1,3-benzodioxol-4-yl)methyl]piperidine-1-carboximidamide, ... (5 entities in total)
• Functional Keywords: eed, fragment-based generation, oncology, transcription-transferase complex, transcription/transferase
• Biological source: Homo sapiens (Human); More
• Cellular location: Nucleus: O75530 Q15910
• Total number of polymer chains: 4
• Total formula weight: 92915.63

Authors

Bussiere, D.,Shu, W. (deposition date: 2016-12-07, release date: 2017-01-11, Last modification date: 2024-03-06)

• Primary citation: Lingel, A.,Sendzik, M.,Huang, Y.,Shultz, M.D.,Cantwell, J.,Dillon, M.P.,Fu, X.,Fuller, J.,Gabriel, T.,Gu, J.,Jiang, X.,Li, L.,Liang, F.,McKenna, M.,Qi, W.,Rao, W.,Sheng, X.,Shu, W.,Sutton, J.,Taft, B.,Wang, L.,Zeng, J.,Zhang, H.,Zhang, M.,Zhao, K.,Lindvall, M.,Bussiere, D.E.; Structure-Guided Design of EED Binders Allosterically Inhibiting the Epigenetic Polycomb Repressive Complex 2 (PRC2) Methyltransferase.; J. Med. Chem., 60:415-427, 2017; PubMed: 27992714; DOI: 10.1021/acs.jmedchem.6b01473

Experimental method

X-RAY DIFFRACTION (1.6 Å)