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5I86

Crystal structure of the bromodomain of human CREBBP bound to the benzodiazepinone G02778174

Summary for 5I86
Entry DOI10.2210/pdb5i86/pdb
Related5I83 5I89
DescriptorCREB-binding protein, 1,2-ETHANEDIOL, THIOCYANATE ION, ... (5 entities in total)
Functional Keywordsbromodomain inhibitor, protein binding-inhibitor complex, protein binding/inhibitor
Biological sourceHomo sapiens (Human)
Cellular locationCytoplasm: Q92793
Total number of polymer chains2
Total formula weight28784.96
Authors
Jayaram, H.,Poy, F.,Setser, J.W.,Bellon, S.F. (deposition date: 2016-02-18, release date: 2016-04-20, Last modification date: 2023-09-27)
Primary citationTaylor, A.M.,Cote, A.,Hewitt, M.C.,Pastor, R.,Leblanc, Y.,Nasveschuk, C.G.,Romero, F.A.,Crawford, T.D.,Cantone, N.,Jayaram, H.,Setser, J.,Murray, J.,Beresini, M.H.,de Leon Boenig, G.,Chen, Z.,Conery, A.R.,Cummings, R.T.,Dakin, L.A.,Flynn, E.M.,Huang, O.W.,Kaufman, S.,Keller, P.J.,Kiefer, J.R.,Lai, T.,Li, Y.,Liao, J.,Liu, W.,Lu, H.,Pardo, E.,Tsui, V.,Wang, J.,Wang, Y.,Xu, Z.,Yan, F.,Yu, D.,Zawadzke, L.,Zhu, X.,Zhu, X.,Sims, R.J.,Cochran, A.G.,Bellon, S.,Audia, J.E.,Magnuson, S.,Albrecht, B.K.
Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637).
Acs Med.Chem.Lett., 7:531-536, 2016
Cited by
PubMed: 27190605
DOI: 10.1021/acsmedchemlett.6b00075
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (1.05 Å)
Structure validation

217705

数据于2024-03-27公开中

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