5U2E

BRD4 first bromodomain (BD1) in complex with dual PI3 kinase (PI3K) inhibitor SF2535

Summary for 5U2E

Entry DOI	10.2210/pdb5u2e/pdb
Related	5U28 5U2C 5U2F
Descriptor	Bromodomain-containing protein 4, ethyl 4-[5-(morpholin-4-yl)-7-oxo-7H-thieno[3,2-b]pyran-3-yl]benzoate (3 entities in total)
Functional Keywords	bromodomain, transcription, inhibitor, epigenetics, transcription regulator-inhibitor complex, transcription regulator/inhibitor
Biological source	Homo sapiens (Human)
Cellular location	Nucleus: O60885
Total number of polymer chains	2
Total formula weight	33596.64
Authors	Andrews, F.H.,Kutateladze, T.G. (deposition date: 2016-11-30, release date: 2017-02-08, Last modification date: 2024-03-06)
Primary citation	Andrews, F.H.,Singh, A.R.,Joshi, S.,Smith, C.A.,Morales, G.A.,Garlich, J.R.,Durden, D.L.,Kutateladze, T.G. Dual-activity PI3K-BRD4 inhibitor for the orthogonal inhibition of MYC to block tumor growth and metastasis. Proc. Natl. Acad. Sci. U.S.A., 114:E1072-E1080, 2017 Cited by PubMed: 28137841 DOI: 10.1073/pnas.1613091114 PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (1.991 Å)

Structure validation