Brand  (β version)

PDB ID: 5VND

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Ligands
Code Name Style Show Link
9ES N-{2-[(6-{[(2,6-dichloro-3,5-dimethoxyphenyl)carbamoyl](methyl)amino}pyrimidin-4-yl)amino]-5-(4-ethylpiperazin-1-yl)phenyl}propanamide PoSSuM
SO4 Sulfate ion PoSSuM
EDO 1,2-ethanediol PoSSuM
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Structure summary

Code : 5VND   PDBj   RCSB PDB   PDBe
Header : transferase/transferase inhibitor
Title : Crystal structure of FGFR1-Y563C (FGFR4 surrogate) covalently bound to H3B-6527
Release Data : 2017-05-24
Compound :
mol_id molecule chains synonym
1 Fibroblast growth factor receptor 1 A,B FGFR-1,Basic fibroblast growth factor receptor 1,bFGF-R-1,Fms-like tyrosine kinase 2,FLT-2,N-sam,Proto-oncogene c-Fgr
ec: 2.7.10.1
fragment: unp residues 458-765
mutation: C486A, Y561C, C582S
Source :
mol_id organism_scientific organism_common expression_system
1 Homo sapiens  (taxid:9606) Human Escherichia coli  (taxid:562)
gene: FGFR1, BFGFR, CEK, FGFBR, FLG, FLT2, HBGFR
expression_system_strain: DE3 star
Authors : Tsai, J.H.C., Reynolds, D., Fekkes, P., Smith, P., Larsen, N.A.
Keywords : FGFR4, H3B-56527, Covalent compound, transferase-transferase inhibitor complex
Exp. method : X-RAY DIFFRACTION ( 2.2 Å )
Citation :

H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma.

Joshi, J.J.,Coffey, H.,Corcoran, E.  et al.
(2017)  Cancer Res.  77 : 6999 - 7013

PubMed: 29247039
DOI: 10.1158/0008-5472.CAN-17-1865

Reaction

Chain : A, B
UniProt : P11362 (FGFR1_HUMAN)
Reaction: EC: Evidence:
Physiological Direction:
ATP + L-tyrosyl-[protein] = ADP + H(+) + O-phospho-L-tyrosyl- [protein] 2.7.10.1 PROSITE-ProRule:PRU10028, PubMed:1379697, PubMed:15117958, PubMed:18480409, PubMed:19224897, PubMed:19665973, PubMed:20133753, PubMed:8622701
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