3RHX

Crystal structure of the catalytic domain of FGFR1 kinase in complex with ARQ 069

Summary for 3RHX

Entry DOI	10.2210/pdb3rhx/pdb
Descriptor	Basic fibroblast growth factor receptor 1, (6S)-6-phenyl-5,6-dihydrobenzo[h]quinazolin-2-amine, SULFATE ION, ... (5 entities in total)
Functional Keywords	fgfr1 kinase, fgfr2 kinase, inactive conformation, kinase-inhibitor complex, transferase-transferase inhibitor complex, transferase/transferase inhibitor
Biological source	Homo sapiens (human)
Cellular location	Membrane; Single-pass type I membrane protein: P11362
Total number of polymer chains	2
Total formula weight	70769.22
Authors	Eathiraj, S.,Palma, R.,Hirschi, M.,Volckova, E.,Nakuci, E.,Castro, J.,Chen, C.R.,Chan, T.C.,France, D.S.,Ashwell, M.A. (deposition date: 2011-04-12, release date: 2011-05-04, Last modification date: 2024-02-28)
Primary citation	Eathiraj, S.,Palma, R.,Hirschi, M.,Volckova, E.,Nakuci, E.,Castro, J.,Chen, C.R.,Chan, T.C.,France, D.S.,Ashwell, M.A. A novel mode of protein kinase inhibition exploiting hydrophobic motifs of autoinhibited kinases: discovery of ATP-independent inhibitors of fibroblast growth factor receptor. J.Biol.Chem., 286:20677-20687, 2011 Cited by PubMed: 21454610 DOI: 10.1074/jbc.M110.213736 PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (2.01 Å)

Structure validation