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5KJ2

The novel p300/CBP inhibitor A-485 uncovers a unique mechanism of action to target AR in castrate resistant prostate cancer

Summary for 5KJ2
Entry DOI10.2210/pdb5kj2/pdb
DescriptorHistone acetyltransferase p300, N-[(4-fluorophenyl)methyl]-2-{(1R)-5-[(methylcarbamoyl)amino]-2',4'-dioxo-2,3-dihydro-3'H-spiro[indene-1,5'-[1,3]oxazolidin]-3'-yl}-N-[(2S)-1,1,1-trifluoropropan-2-yl]acetamide, SODIUM ION, ... (4 entities in total)
Functional Keywordshistone acetyltransferase, transferase-transferase inhibitor complex, transferase/transferase inhibitor
Biological sourceHomo sapiens (Human)
Total number of polymer chains1
Total formula weight40820.46
Authors
Jakob, C.G.,Qiu, W.,Edalji, R.P.,Sun, C. (deposition date: 2016-06-17, release date: 2017-09-27, Last modification date: 2023-09-27)
Primary citationLasko, L.M.,Jakob, C.G.,Edalji, R.P.,Qiu, W.,Montgomery, D.,Digiammarino, E.L.,Hansen, T.M.,Risi, R.M.,Frey, R.,Manaves, V.,Shaw, B.,Algire, M.,Hessler, P.,Lam, L.T.,Uziel, T.,Faivre, E.,Ferguson, D.,Buchanan, F.G.,Martin, R.L.,Torrent, M.,Chiang, G.G.,Karukurichi, K.,Langston, J.W.,Weinert, B.T.,Choudhary, C.,de Vries, P.,Van Drie, J.H.,McElligott, D.,Kesicki, E.,Marmorstein, R.,Sun, C.,Cole, P.A.,Rosenberg, S.H.,Michaelides, M.R.,Lai, A.,Bromberg, K.D.
Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours.
Nature, 550:128-132, 2017
Cited by
PubMed: 28953875
DOI: 10.1038/nature24028
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (1.95 Å)
Structure validation

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