4WVL
Structure-Guided DOT1L Probe Optimization by Label-Free Ligand Displacement
Summary for 4WVL
Entry DOI | 10.2210/pdb4wvl/pdb |
Descriptor | Histone-lysine N-methyltransferase, H3 lysine-79 specific, N-[4-(acetylamino)butyl]-5'-[(3-{[(4-tert-butylphenyl)carbamoyl]amino}propyl)(propan-2-yl)amino]-5'-deoxyadenosine, SULFATE ION, ... (6 entities in total) |
Functional Keywords | dot1l, methyltransferase, inhibitor, leukemia, transferase-transferase inhibitor complex, transferase/transferase inhibitor |
Biological source | Homo sapiens (Human) |
Cellular location | Nucleus : Q8TEK3 |
Total number of polymer chains | 1 |
Total formula weight | 41539.08 |
Authors | Xu, X.,Dhe-Paganon, S.,Blacklow, S. (deposition date: 2014-11-06, release date: 2014-12-03, Last modification date: 2023-09-27) |
Primary citation | Yi, J.S.,Federation, A.J.,Qi, J.,Dhe-Paganon, S.,Hadler, M.,Xu, X.,St Pierre, R.,Varca, A.C.,Wu, L.,Marineau, J.J.,Smith, W.B.,Souza, A.,Chory, E.J.,Armstrong, S.A.,Bradner, J.E. Structure-Guided DOT1L Probe Optimization by Label-Free Ligand Displacement. Acs Chem.Biol., 10:667-674, 2015 Cited by PubMed: 25397901DOI: 10.1021/cb500796d PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2.41 Å) |
Structure validation
Download full validation report