4ER7
Crystal Structure of human DOT1L in complex with inhibitor SGC0947
Summary for 4ER7
Entry DOI | 10.2210/pdb4er7/pdb |
Related | 4EQZ 4ER0 4ER3 4ER5 4ER6 |
Descriptor | Histone-lysine N-methyltransferase, H3 lysine-79 specific, 5-bromo-7-{5-[(3-{[(4-tert-butylphenyl)carbamoyl]amino}propyl)amino]-5-deoxy-beta-D-ribofuranosyl}-7H-pyrrolo[2,3-d]pyrimidin-4-amine, GLYCEROL, ... (4 entities in total) |
Functional Keywords | histone, methyltransferase, epigenetics, transferase-transferase inhibitor complex, structural genomics, structural genomics consortium, sgc, transferase/transferase inhibitor |
Biological source | Homo sapiens (human) |
Cellular location | Nucleus : Q8TEK3 |
Total number of polymer chains | 1 |
Total formula weight | 48649.27 |
Authors | Wernimont, A.K.,Tempel, W.,Yu, W.,Scopton, A.,Li, Y.,Nguyen, K.T.,Vedadi, M.,Bradner, J.E.,Schapira, M.,Arrowsmith, C.H.,Edwards, A.M.,Bountra, C.,Brown, P.J.,Structural Genomics Consortium (SGC) (deposition date: 2012-04-19, release date: 2012-05-16, Last modification date: 2024-02-28) |
Primary citation | Yu, W.,Chory, E.J.,Wernimont, A.K.,Tempel, W.,Scopton, A.,Federation, A.,Marineau, J.J.,Qi, J.,Barsyte-Lovejoy, D.,Yi, J.,Marcellus, R.,Iacob, R.E.,Engen, J.R.,Griffin, C.,Aman, A.,Wienholds, E.,Li, F.,Pineda, J.,Estiu, G.,Shatseva, T.,Hajian, T.,Al-Awar, R.,Dick, J.E.,Vedadi, M.,Brown, P.J.,Arrowsmith, C.H.,Bradner, J.E.,Schapira, M. Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat Commun, 3:1288-1288, 2012 Cited by PubMed: 23250418DOI: 10.1038/ncomms2304 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2.2 Å) |
Structure validation
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