4R6V

Crystal Structure of FGF Receptor (FGFR) 4 Kinase Harboring the V550L Gate-Keeper Mutation in Complex with FIIN-3, an Irreversible Tyrosine Kinase Inhibitor Capable of Overcoming FGFR kinase Gate-Keeper Mutations

Summary for 4R6V

• Entry DOI: 10.2210/pdb4r6v/pdb
• Related: 4QQ5 4QQC 4QQJ 4QQT 4QRC
• Descriptor: Fibroblast growth factor receptor 4, N-[4-({[(2,6-dichloro-3,5-dimethoxyphenyl)carbamoyl](6-{[4-(4-methylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl)amino}methyl)phenyl]propanamide, SULFATE ION, ... (4 entities in total)
• Functional Keywords: kinase domain fold, cell signaling, phosphotransferase, plasmamembrane, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• Biological source: Homo sapiens (human)
• Cellular location: Cell membrane; Single-pass type I membrane protein. Isoform 2: Secreted. Isoform 3: Cytoplasm : P22455
• Total number of polymer chains: 1
• Total formula weight: 37059.35

Authors

Huang, Z.,Mohammadi, M. (deposition date: 2014-08-26, release date: 2014-10-29, Last modification date: 2023-09-20)

• Primary citation: Tan, L.,Wang, J.,Tanizaki, J.,Huang, Z.,Aref, A.R.,Rusan, M.,Zhu, S.J.,Zhang, Y.,Ercan, D.,Liao, R.G.,Capelletti, M.,Zhou, W.,Hur, W.,Kim, N.,Sim, T.,Gaudet, S.,Barbie, D.A.,Yeh, J.R.,Yun, C.H.,Hammerman, P.S.,Mohammadi, M.,Janne, P.A.,Gray, N.S.; Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors.; Proc.Natl.Acad.Sci.USA, 111:E4869-E4877, 2014; PubMed: 25349422; DOI: 10.1073/pnas.1403438111

Experimental method

X-RAY DIFFRACTION (2.353 Å)