5KTU

Crystal structure of the bromodomain of human CREBBP bound to pyrazolopiperidine scaffold

5KTU の概要

• エントリーDOI: 10.2210/pdb5ktu/pdb
• 分子名称: CREB-binding protein, 1-(3-phenylazanyl-1,4,6,7-tetrahydropyrazolo[4,3-c]pyridin-5-yl)ethanone, DIMETHYL SULFOXIDE, ... (4 entities in total)
• 機能のキーワード: bromodomain, inhibitor, epigenetics, transferase
• 由来する生物種: Homo sapiens (Human)
• 細胞内の位置: Cytoplasm: Q92793
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 28318.46

構造登録者

Jayaram, H.,Poy, F.,Setser, J.W.,Bellon, S.F. (登録日: 2016-07-12, 公開日: 2016-11-02, 最終更新日: 2023-10-04)

• 主引用文献: Crawford, T.D.,Romero, F.A.,Lai, K.W.,Tsui, V.,Taylor, A.M.,de Leon Boenig, G.,Noland, C.L.,Murray, J.,Ly, J.,Choo, E.F.,Hunsaker, T.L.,Chan, E.W.,Merchant, M.,Kharbanda, S.,Gascoigne, K.E.,Kaufman, S.,Beresini, M.H.,Liao, J.,Liu, W.,Chen, K.X.,Chen, Z.,Conery, A.R.,Cote, A.,Jayaram, H.,Jiang, Y.,Kiefer, J.R.,Kleinheinz, T.,Li, Y.,Maher, J.,Pardo, E.,Poy, F.,Spillane, K.L.,Wang, F.,Wang, J.,Wei, X.,Xu, Z.,Xu, Z.,Yen, I.,Zawadzke, L.,Zhu, X.,Bellon, S.,Cummings, R.,Cochran, A.G.,Albrecht, B.K.,Magnuson, S.; Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300.; J. Med. Chem., 59:10549-10563, 2016; PubMed: 27682507; DOI: 10.1021/acs.jmedchem.6b01022

実験手法

X-RAY DIFFRACTION (1.38 Å)