5LS6
Structure of Human Polycomb Repressive Complex 2 (PRC2) with inhibitor
Summary for 5LS6
Entry DOI | 10.2210/pdb5ls6/pdb |
Descriptor | Histone-lysine N-methyltransferase EZH2,Histone-lysine N-methyltransferase EZH2,Histone-lysine N-methyltransferase EZH2, Polycomb protein EED, Polycomb protein SUZ12, ... (6 entities in total) |
Functional Keywords | human prc2, inhibitor, h3k27, transferase-inhibitor complex, transferase/inhibitor |
Biological source | Homo sapiens (Human) More |
Total number of polymer chains | 16 |
Total formula weight | 557894.22 |
Authors | Zhang, Y.,Justin, N.,Chen, S.,Wilson, J.,Gamblin, S. (deposition date: 2016-08-22, release date: 2017-02-22, Last modification date: 2024-01-17) |
Primary citation | Vaswani, R.G.,Gehling, V.S.,Dakin, L.A.,Cook, A.S.,Nasveschuk, C.G.,Duplessis, M.,Iyer, P.,Balasubramanian, S.,Zhao, F.,Good, A.C.,Campbell, R.,Lee, C.,Cantone, N.,Cummings, R.T.,Normant, E.,Bellon, S.F.,Albrecht, B.K.,Harmange, J.C.,Trojer, P.,Audia, J.E.,Zhang, Y.,Justin, N.,Chen, S.,Wilson, J.R.,Gamblin, S.J. Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymphomas. J. Med. Chem., 59:9928-9941, 2016 Cited by PubMed: 27739677DOI: 10.1021/acs.jmedchem.6b01315 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (3.47 Å) |
Structure validation
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