4MR5

Crystal Structure of the second bromodomain of human BRD2 in complex with a quinazolinone ligand (RVX-OH)

4MR5 の概要

• エントリーDOI: 10.2210/pdb4mr5/pdb
• 関連するPDBエントリー: 4MR3 4mr4 4mr6
• 分子名称: Bromodomain-containing protein 2, 1,2-ETHANEDIOL, DIMETHYL SULFOXIDE, ... (5 entities in total)
• 機能のキーワード: brd2, ring3, small molecule inhibitor, rvx-oh, inhibitor complex, structural genomics consortium, sgc, transcription-transcription inhibitor complex, transcription/transcription inhibitor
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Nucleus (Probable): P25440
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 14072.21

構造登録者

Filippakopoulos, P.,Picaud, S.,Felletar, I.,Martin, S.,Fedorov, O.,von Delft, F.,Arrowsmith, C.H.,Edwards, A.M.,Weigelt, J.,Bountra, C.,Knapp, S.,Structural Genomics Consortium (SGC) (登録日: 2013-09-17, 公開日: 2013-11-27, 最終更新日: 2024-02-28)

• 主引用文献: Picaud, S.,Wells, C.,Felletar, I.,Brotherton, D.,Martin, S.,Savitsky, P.,Diez-Dacal, B.,Philpott, M.,Bountra, C.,Lingard, H.,Fedorov, O.,Muller, S.,Brennan, P.E.,Knapp, S.,Filippakopoulos, P.; RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain.; Proc.Natl.Acad.Sci.USA, 110:19754-19759, 2013; PubMed: 24248379; DOI: 10.1073/pnas.1310658110

実験手法

X-RAY DIFFRACTION (1.63 Å)