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 DOI | 10.2210/pdb5kj2/pdb |
Descriptor | Histone 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 Keywords | histone acetyltransferase, transferase-transferase inhibitor complex, transferase/transferase inhibitor |
Biological source | Homo sapiens (Human) |
Total number of polymer chains | 1 |
Total formula weight | 40820.46 |
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 citation | Lasko, 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: 28953875DOI: 10.1038/nature24028 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (1.95 Å) |
Structure validation
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