5HBE

CDK8-CYCC IN COMPLEX WITH 8-[3-Chloro-5-(1-methyl-2,2-dioxo-2, 3-dihydro-1H-2l6-benzo[c]isothiazol-5-yl)-pyridin- 4-yl]-1-oxa-3,8-diaza-spiro[4.5]decan-2-one

5HBE の概要

• エントリーDOI: 10.2210/pdb5hbe/pdb
• 分子名称: Cyclin-dependent kinase 8, Cyclin-C, 8-[3-chloranyl-5-[1-methyl-2,2-bis(oxidanylidene)-3~{H}-2,1-benzothiazol-5-yl]pyridin-4-yl]-1-oxa-3,8-diazaspiro[4.5]decan-2-one, ... (7 entities in total)
• 機能のキーワード: cdk8 kinase / cyclin c, transferase
• 由来する生物種: Homo sapiens (Human); 詳細
• 細胞内の位置: Nucleus : P49336 P24863
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 74866.56

構造登録者

Musil, D.,Blagg, J.,Mallinger, A. (登録日: 2015-12-31, 公開日: 2016-02-03, 最終更新日: 2016-02-24)

• 主引用文献: Mallinger, A.,Schiemann, K.,Rink, C.,Stieber, F.,Calderini, M.,Crumpler, S.,Stubbs, M.,Adeniji-Popoola, O.,Poeschke, O.,Busch, M.,Czodrowski, P.,Musil, D.,Schwarz, D.,Ortiz-Ruiz, M.J.,Schneider, R.,Thai, C.,Valenti, M.,de Haven Brandon, A.,Burke, R.,Workman, P.,Dale, T.,Wienke, D.,Clarke, P.A.,Esdar, C.,Raynaud, F.I.,Eccles, S.A.,Rohdich, F.,Blagg, J.; Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.; J.Med.Chem., 59:1078-1101, 2016; PubMed: 26796641; DOI: 10.1021/acs.jmedchem.5b01685

実験手法

X-RAY DIFFRACTION (2.38 Å)