7K0U
Crystal structure of the second bromodomain (BD2) of human TAF1 bound to PLK1 kinase inhibitor BI2536
Summary for 7K0U
Entry DOI | 10.2210/pdb7k0u/pdb |
Descriptor | Transcription initiation factor TFIID subunit 1, 4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl]amino}-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide (3 entities in total) |
Functional Keywords | taf1, non-bet, bet, kinase inhibitor, plk1, dual brd-kinase, gene regulation |
Biological source | Homo sapiens (Human) |
Total number of polymer chains | 2 |
Total formula weight | 33852.24 |
Authors | Karim, M.R.,Schonbrunn, E. (deposition date: 2020-09-06, release date: 2021-09-22, Last modification date: 2023-10-18) |
Primary citation | Karim, R.M.,Yang, L.,Chen, L.,Bikowitz, M.J.,Lu, J.,Grassie, D.,Shultz, Z.P.,Lopchuk, J.M.,Chen, J.,Schonbrunn, E. Discovery of Dual TAF1-ATR Inhibitors and Ligand-Induced Structural Changes of the TAF1 Tandem Bromodomain. J.Med.Chem., 65:4182-4200, 2022 Cited by PubMed: 35191694DOI: 10.1021/acs.jmedchem.1c01999 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2.52 Å) |
Structure validation
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