5E1S

The Crystal structure of INSR Tyrosine Kinase in complex with the Inhibitor BI 885578

5E1S の概要

• エントリーDOI: 10.2210/pdb5e1s/pdb
• 分子名称: Insulin receptor, (5R)-N-(1-{2-[4-(2-methoxyethyl)piperazin-1-yl]ethyl}-1H-pyrazol-3-yl)-5,8-dimethyl-9-phenyl-6,8-dihydro-5H-pyrazolo[3,4-h]quinazolin-2-amine (3 entities in total)
• 機能のキーワード: kinase, insr, igf-1r, inhibitor, transferase
• 由来する生物種: Homo sapiens (Human)
• 細胞内の位置: Cell membrane; Single-pass type I membrane protein: P06213
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 35479.61

構造登録者

Kessler, D.,Zahn, S.,Sanderson, M.,Wolkerstorfer, B. (登録日: 2015-09-30, 公開日: 2015-10-14, 最終更新日: 2024-01-10)

• 主引用文献: Sanderson, M.P.,Apgar, J.,Garin-Chesa, P.,Hofmann, M.H.,Kessler, D.,Quant, J.,Savchenko, A.,Schaaf, O.,Treu, M.,Tye, H.,Zahn, S.K.,Zoephel, A.,Haaksma, E.,Adolf, G.R.,Kraut, N.; BI 885578, a Novel IGF1R/INSR Tyrosine Kinase Inhibitor with Pharmacokinetic Properties That Dissociate Antitumor Efficacy and Perturbation of Glucose Homeostasis.; Mol.Cancer Ther., 14:2762-2772, 2015; PubMed: 26438154; DOI: 10.1158/1535-7163.MCT-15-0539

実験手法

X-RAY DIFFRACTION (2.264 Å)