5KJ2

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

5KJ2 の概要

• エントリーDOI: 10.2210/pdb5kj2/pdb
• 分子名称: 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)
• 機能のキーワード: histone acetyltransferase, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• 由来する生物種: Homo sapiens (Human)
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 40820.46

構造登録者

Jakob, C.G.,Qiu, W.,Edalji, R.P.,Sun, C. (登録日: 2016-06-17, 公開日: 2017-09-27, 最終更新日: 2023-09-27)

• 主引用文献: 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; PubMed: 28953875; DOI: 10.1038/nature24028

実験手法

X-RAY DIFFRACTION (1.95 Å)