4OGI

Crystal Structure of the first bromodomain of human BRD4 in complex with the inhibitor BI-2536

4OGI の概要

• エントリーDOI: 10.2210/pdb4ogi/pdb
• 関連するPDBエントリー: 4OGJ
• 分子名称: Bromodomain-containing protein 4, 1,2-ETHANEDIOL, 4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl]amino}-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide, ... (4 entities in total)
• 機能のキーワード: bromodomain, bromodomain containing protein 4, plk1 kinase inhibitor, structural genomics, structural genomics consortium, sgc, transcription-inhibitor complex, transcription/inhibitor
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Nucleus: O60885
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 31366.20

構造登録者

Filippakopoulos, P.,Picaud, S.,Jose, B.,Martin, S.,Fedorov, O.,von Delft, F.,Arrowsmith, C.H.,Edwards, A.M.,Bountra, C.,Knapp, S.,Structural Genomics Consortium (SGC) (登録日: 2014-01-16, 公開日: 2014-02-26, 最終更新日: 2023-09-20)

• 主引用文献: Ciceri, P.,Muller, S.,O'Mahony, A.,Fedorov, O.,Filippakopoulos, P.,Hunt, J.P.,Lasater, E.A.,Pallares, G.,Picaud, S.,Wells, C.,Martin, S.,Wodicka, L.M.,Shah, N.P.,Treiber, D.K.,Knapp, S.; Dual kinase-bromodomain inhibitors for rationally designed polypharmacology.; Nat.Chem.Biol., 10:305-312, 2014; PubMed: 24584101; DOI: 10.1038/nchembio.1471

実験手法

X-RAY DIFFRACTION (1.73 Å)