2QU5

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

Summary for 2QU5

• Entry DOI: 10.2210/pdb2qu5/pdb
• Related: 2QU6
• Descriptor: Vascular endothelial growth factor receptor 2, 4-[[2-[[4-chloro-3-(trifluoromethyl)phenyl]amino]-3H-benzimidazol-5-yl]oxy]-N-methyl-pyridine-2-carboxamide (3 entities in total)
• Functional Keywords: receptor tyrosinse kinase, kdr, 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: 1
• Total formula weight: 36746.41

Authors

Whittington, D.A.,Kim, J.L.,Long, A.M.,Rose, P.,Gu, Y.,Zhao, H. (deposition date: 2007-08-03, release date: 2007-09-25, Last modification date: 2023-11-15)

• Primary citation: Potashman, M.H.,Bready, J.,Coxon, A.,Demelfi, T.M.,Dipietro, L.,Doerr, N.,Elbaum, D.,Estrada, J.,Gallant, P.,Germain, J.,Gu, Y.,Harmange, J.C.,Kaufman, S.A.,Kendall, R.,Kim, J.L.,Kumar, G.N.,Long, A.M.,Neervannan, S.,Patel, V.F.,Polverino, A.,Rose, P.,Plas, S.V.,Whittington, D.,Zanon, R.,Zhao, H.; Design, Synthesis, and Evaluation of Orally Active Benzimidazoles and Benzoxazoles as Vascular Endothelial Growth Factor-2 Receptor Tyrosine Kinase Inhibitors.; J.Med.Chem., 50:4351-4373, 2007; PubMed: 17696416; DOI: 10.1021/jm070034i

Experimental method

X-RAY DIFFRACTION (2.95 Å)