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4ER6

Crystal structure of human DOT1L in complex with inhibitor SGC0946

Summary for 4ER6
Entry DOI10.2210/pdb4er6/pdb
Related4EQZ 4ER0 4ER3 4ER5 4ER7
DescriptorHistone-lysine N-methyltransferase, H3 lysine-79 specific, BROMIDE ION, 5-bromo-7-{5-[(3-{[(4-tert-butylphenyl)carbamoyl]amino}propyl)(propan-2-yl)amino]-5-deoxy-beta-D-ribofuranosyl}-7H-pyrrolo[2,3-d]pyrimidin-4-amine, ... (5 entities in total)
Functional Keywordshistone, methyltransferase, epigenetics, transferase-transferase inhibitor complex, structural genomics, structural genomics consortium, sgc, transferase/transferase inhibitor
Biological sourceHomo sapiens (human)
Cellular locationNucleus : Q8TEK3
Total number of polymer chains1
Total formula weight47772.00
Authors
Primary citationYu, 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: 23250418
DOI: 10.1038/ncomms2304
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (2.3 Å)
Structure validation

217705

數據於2024-03-27公開中

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