3U6J

Crystal structure of the VEGFR2 kinase domain in complex with a pyrazolone inhibitor

3U6J の概要

• エントリーDOI: 10.2210/pdb3u6j/pdb
• 関連するPDBエントリー: 3U6H 3U6I
• 分子名称: Vascular endothelial growth factor receptor 2, N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]-3-fluorophenyl}-1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (3 entities in total)
• 機能のキーワード: kdr, flk-1, angiogenesis, phosphotransferase, cancer, vascular endothelial growth factor, transferase/transferase inhibitor, transferase-transferase inhibitor complex
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Isoform 1: Cell membrane; Single-pass type I membrane protein. Isoform 2: Secreted (Probable). Isoform 3: Secreted: P35968
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 36685.23

構造登録者

Whittington, D.A.,Long, A.,Rose, P.,Gu, Y.,Zhao, H. (登録日: 2011-10-12, 公開日: 2012-02-22, 最終更新日: 2024-02-28)

• 主引用文献: Norman, M.H.,Liu, L.,Lee, M.,Xi, N.,Fellows, I.,D'Angelo, N.D.,Dominguez, C.,Rex, K.,Bellon, S.F.,Kim, T.S.,Dussault, I.; Structure-based design of novel class II c-Met inhibitors: 1. Identification of pyrazolone-based derivatives.; J.Med.Chem., 55:1858-1867, 2012; PubMed: 22320343; DOI: 10.1021/jm201330u

実験手法

X-RAY DIFFRACTION (2.15 Å)