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5KTU

Crystal structure of the bromodomain of human CREBBP bound to pyrazolopiperidine scaffold

Summary for 5KTU
Entry DOI10.2210/pdb5ktu/pdb
DescriptorCREB-binding protein, 1-(3-phenylazanyl-1,4,6,7-tetrahydropyrazolo[4,3-c]pyridin-5-yl)ethanone, DIMETHYL SULFOXIDE, ... (4 entities in total)
Functional Keywordsbromodomain, inhibitor, epigenetics, transferase
Biological sourceHomo sapiens (Human)
Cellular locationCytoplasm: Q92793
Total number of polymer chains2
Total formula weight28318.46
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 citationCrawford, 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: 27682507
DOI: 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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