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5CGP

Selective pharmacological inhibition of the CREB binding protein bromodomain regulates inflammatory cytokines in macrophages and RGS4 in neurons

Summary for 5CGP
Entry DOI10.2210/pdb5cgp/pdb
Related5CFW
DescriptorCREB-binding protein, 5-(3,5-dimethyl-1,2-oxazol-4-yl)-2-[2-(4-methoxyphenyl)ethyl]-1-[2-(morpholin-4-yl)ethyl]-1H-benzimidazole (3 entities in total)
Functional Keywordsinhibitor, complex, transcription-inhibitor complex, transcription/inhibitor
Biological sourceHomo sapiens (Human)
Cellular locationCytoplasm: Q92793
Total number of polymer chains1
Total formula weight14683.92
Authors
Chekler, E.L.,Jones, L.H. (deposition date: 2015-07-09, release date: 2016-04-20, Last modification date: 2023-09-27)
Primary citationChekler, E.L.,Pellegrino, J.A.,Lanz, T.A.,Denny, R.A.,Flick, A.C.,Coe, J.,Langille, J.,Basak, A.,Liu, S.,Stock, I.A.,Sahasrabudhe, P.,Bonin, P.D.,Lee, K.,Pletcher, M.T.,Jones, L.H.
Transcriptional Profiling of a Selective CREB Binding Protein Bromodomain Inhibitor Highlights Therapeutic Opportunities.
Chem.Biol., 22:1588-1596, 2015
Cited by
PubMed: 26670081
DOI: 10.1016/j.chembiol.2015.10.013
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (1.96 Å)
Structure validation

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