6E23
Displacement of WDR5 from chromatin by a pharmacological WIN site inhibitor with picomolar affinity
Summary for 6E23
Entry DOI | 10.2210/pdb6e23/pdb |
Related | 6D9X |
Descriptor | WD repeat-containing protein 5, N-[(3,4-dichlorophenyl)methyl]-3-(6-fluoro-2-methylpyridin-3-yl)-5-{[(2E)-2-imino-3-methyl-2,3-dihydro-1H-imidazol-1-yl]methyl}benzamide, 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, ... (4 entities in total) |
Functional Keywords | wdr5, win-site, fragment screening, structure-based design, mixed-lineage leukemia, dna binding protein, dna binding protein-inhibitor complex, gene regulation, gene regulation-inhibitor complex, gene regulation/inhibitor |
Biological source | Homo sapiens (Human) |
Total number of polymer chains | 2 |
Total formula weight | 70017.05 |
Authors | Phan, J.,Fesik, S.W. (deposition date: 2018-07-10, release date: 2019-03-13, Last modification date: 2023-10-11) |
Primary citation | Aho, E.R.,Wang, J.,Gogliotti, R.D.,Howard, G.C.,Phan, J.,Acharya, P.,Macdonald, J.D.,Cheng, K.,Lorey, S.L.,Lu, B.,Wenzel, S.,Foshage, A.M.,Alvarado, J.,Wang, F.,Shaw, J.G.,Zhao, B.,Weissmiller, A.M.,Thomas, L.R.,Vakoc, C.R.,Hall, M.D.,Hiebert, S.W.,Liu, Q.,Stauffer, S.R.,Fesik, S.W.,Tansey, W.P. Displacement of WDR5 from Chromatin by a WIN Site Inhibitor with Picomolar Affinity. Cell Rep, 26:2916-2928.e13, 2019 Cited by PubMed: 30865883DOI: 10.1016/j.celrep.2019.02.047 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (1.66 Å) |
Structure validation
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