5KTU
Crystal structure of the bromodomain of human CREBBP bound to pyrazolopiperidine scaffold
Summary for 5KTU
Entry DOI | 10.2210/pdb5ktu/pdb |
Descriptor | CREB-binding protein, 1-(3-phenylazanyl-1,4,6,7-tetrahydropyrazolo[4,3-c]pyridin-5-yl)ethanone, DIMETHYL SULFOXIDE, ... (4 entities in total) |
Functional Keywords | bromodomain, inhibitor, epigenetics, transferase |
Biological source | Homo sapiens (Human) |
Cellular location | Cytoplasm: Q92793 |
Total number of polymer chains | 2 |
Total formula weight | 28318.46 |
Authors | Jayaram, H.,Poy, F.,Setser, J.W.,Bellon, S.F. (deposition date: 2016-07-12, release date: 2016-11-02, Last modification date: 2023-10-04) |
Primary citation | Crawford, T.D.,Romero, F.A.,Lai, K.W.,Tsui, V.,Taylor, A.M.,de Leon Boenig, G.,Noland, C.L.,Murray, J.,Ly, J.,Choo, E.F.,Hunsaker, T.L.,Chan, E.W.,Merchant, M.,Kharbanda, S.,Gascoigne, K.E.,Kaufman, S.,Beresini, M.H.,Liao, J.,Liu, W.,Chen, K.X.,Chen, Z.,Conery, A.R.,Cote, A.,Jayaram, H.,Jiang, Y.,Kiefer, J.R.,Kleinheinz, T.,Li, Y.,Maher, J.,Pardo, E.,Poy, F.,Spillane, K.L.,Wang, F.,Wang, J.,Wei, X.,Xu, Z.,Xu, Z.,Yen, I.,Zawadzke, L.,Zhu, X.,Bellon, S.,Cummings, R.,Cochran, A.G.,Albrecht, B.K.,Magnuson, S. Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300. J. Med. Chem., 59:10549-10563, 2016 Cited by PubMed: 27682507DOI: 10.1021/acs.jmedchem.6b01022 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (1.38 Å) |
Structure validation
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