› 3rhx

X-ray diffraction
2.01Å resolution

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

Released:
DOI: 10.2210/pdb3rhx/pdb
PDB entry 3rhx coloured by chain, front view.
PDB entry 3rhx coloured by chain, side view.
PDB entry 3rhx coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
A novel mode of protein kinase inhibition exploiting hydrophobic motifs of autoinhibited kinases: discovery of ATP-independent inhibitors of fibroblast growth factor receptor.
Eathiraj S, Palma R, Hirschi M, Volckova E, Nakuci E, Castro J, Chen CR, Chan TC, France DS, Ashwell MA
J Biol Chem 286 20677-87 (2011)
PMID: 21454610

Function and Biology Details

Reaction catalysed: 
ATP + a [protein]-L-tyrosine = ADP + a [protein]-L-tyrosine phosphate
Biochemical function:
Biological process:
Cellular component:
  • not assigned
Sequence domains:

Structure analysis Details

Assembly composition:
monomeric (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-145801 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Fibroblast growth factor receptor 1 Chains: A, B
Molecule details ›
Chains: A, B
Length: 306 amino acids
Theoretical weight: 34.91 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli BL21
UniProt:
  • Canonical: P11362 (Residues: 461-765; Coverage: 38%)
Gene names: BFGFR, CEK, FGFBR, FGFR1, FLG, FLT2, HBGFR
Sequence domains: Protein tyrosine and serine/threonine kinase
Structure domains:

Ligands and Environments

3 bound ligands:
Ligand 3RH 2 x 3RH
Ligand SO4 1 x SO4
Ligand EDO 5 x EDO
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: NSLS BEAMLINE X29A
Spacegroup: C2
Unit cell:
a: 208.43Å b: 57.865Å c: 65.686Å
α: 90° β: 107.22° γ: 90°
R-values:
R R work R free
0.205 0.201 0.262
Expression system: Escherichia coli BL21

Quick links

Citations

3 review citations

Small-molecule inhibitors of the receptor tyrosine kinases: promising tools for targeted cancer therapies.
Hojjat-Farsangi M. (2014)
2 more

5 mentions without citation

Screening of mutations affecting protein stability and dynamics of FGFR1-A simulation analysis.
Doss et al. (2012)
4 more