4KNB

C-Met in complex with OSI ligand

4KNB の概要

• エントリーDOI: 10.2210/pdb4knb/pdb
• 分子名称: Hepatocyte growth factor receptor, 7-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-3-[1-(piperidin-4-yl)-1H-pyrazol-4-yl]furo[3,2-c]pyridin-6-amine, GAMMA-BUTYROLACTONE, ... (4 entities in total)
• 機能のキーワード: protein kinase, transferase
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Membrane; Single-pass type I membrane protein. Isoform 3: Secreted: P08581
• タンパク質・核酸の鎖数: 4
• 化学式量合計: 132419.11

構造登録者

Wang, J.,Steinig, A.G.,Li, A.H.,Chen, X.,Dong, H.,Ferraro, C.,Jin, M.,Kadalbajoo, M.,Kleinberg, A.,Stolz, K.M.,Tavares-Greco, P.A.,Wang, T.,Albertella, M.R.,Peng, Y.,Crew, L.,Kahler, J. (登録日: 2013-05-09, 公開日: 2014-04-30, 最終更新日: 2024-02-28)

主引用文献

Steinig, A.G.,Li, A.H.,Wang, J.,Chen, X.,Dong, H.,Ferraro, C.,Jin, M.,Kadalbajoo, M.,Kleinberg, A.,Stolz, K.M.,Tavares-Greco, P.A.,Wang, T.,Albertella, M.R.,Peng, Y.,Crew, L.,Kahler, J.,Kan, J.,Schulz, R.,Cooke, A.,Bittner, M.,Turton, R.W.,Franklin, M.,Gokhale, P.,Landfair, D.,Mantis, C.,Workman, J.,Wild, R.,Pachter, J.,Epstein, D.,Mulvihill, M.J.
Novel 6-aminofuro[3,2-c]pyridines as potent, orally efficacious inhibitors of cMET and RON kinases.
Bioorg.Med.Chem.Lett., 23:4381-4387, 2013

PubMed Abstract: A series of novel 6-aminofuro[3,2-c]pyridines as kinase inhibitors is described, most notably, OSI-296 (6). We discuss our exploration of structure-activity relationships and optimization leading to OSI-296 and disclose its pharmacological activity against cMET and RON in cellular assays. OSI-296 is a potent and selective inhibitor of cMET and RON kinases that shows in vivo efficacy in tumor xenografts models upon oral dosing and is well tolerated.

PubMed: 23773865
DOI: 10.1016/j.bmcl.2013.05.074

実験手法

X-RAY DIFFRACTION (2.4 Å)