3B8Q

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

Summary for 3B8Q

• Entry DOI: 10.2210/pdb3b8q/pdb
• Related: 3B8R
• Descriptor: Vascular endothelial growth factor receptor 2, N-(4-chlorophenyl)-6-[(6,7-dimethoxyquinolin-4-yl)oxy]naphthalene-1-carboxamide (3 entities in total)
• Functional Keywords: receptor tyrosine kinase, angiogenesis, atp-binding, developmental protein, differentiation, glycoprotein, host-virus interaction, immunoglobulin domain, membrane, nucleotide-binding, phosphorylation, polymorphism, transferase, transmembrane, tyrosine-protein kinase
• Biological source: Homo sapiens (human); More
• Cellular location: Cell junction . Isoform 1: Cell membrane; Single-pass type I membrane protein. Isoform 2: Secreted . Isoform 3: Secreted: P35968
• Total number of polymer chains: 2
• Total formula weight: 73539.03

Authors

Whittington, D.A.,Long, A.M.,Gu, Y.,Zhao, H. (deposition date: 2007-11-01, release date: 2008-04-01, Last modification date: 2023-11-15)

• Primary citation: Harmange, J.C.,Weiss, M.M.,Germain, J.,Polverino, A.J.,Borg, G.,Bready, J.,Chen, D.,Choquette, D.,Coxon, A.,DeMelfi, T.,DiPietro, L.,Doerr, N.,Estrada, J.,Flynn, J.,Graceffa, R.F.,Harriman, S.P.,Kaufman, S.,La, D.S.,Long, A.,Martin, M.W.,Neervannan, S.,Patel, V.F.,Potashman, M.,Regal, K.,Roveto, P.M.,Schrag, M.L.,Starnes, C.,Tasker, A.,Teffera, Y.,Wang, L.,White, R.D.,Whittington, D.A.,Zanon, R.; Naphthamides as Novel and Potent Vascular Endothelial Growth Factor Receptor Tyrosine Kinase Inhibitors: Design, Synthesis and Evaluation; J.Med.Chem., 51:1649-1667, 2008; PubMed: 18324761; DOI: 10.1021/jm701097z

Experimental method

X-RAY DIFFRACTION (2.75 Å)