› 4rwj

X-ray diffraction
2.49Å resolution

Crystal Structure of FGFR1 (C488A, C584S) in complex with AZD4547 (N-{3-[2-(3,5-DIMETHOXYPHENYL)ETHYL]-1H-PYRAZOL-5-YL}-4-[(3R,5S)-3,5-DIMETHYLPIPERAZIN-1-YL]BENZAMIDE)

Released:
DOI: 10.2210/pdb4rwj/pdb
PDB entry 4rwj coloured by chain, front view.
PDB entry 4rwj coloured by chain, side view.
PDB entry 4rwj coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Illuminating the molecular mechanisms of tyrosine kinase inhibitor resistance for the FGFR1 gatekeeper mutation: the Achilles' heel of targeted therapy.
Sohl CD, Ryan MR, Luo B, Frey KM, Anderson KS
ACS Chem Biol 10 1319-29 (2015)
PMID: 25686244

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: 317 amino acids
Theoretical weight: 36.23 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli BL21(DE3)
UniProt:
  • Canonical: P11362 (Residues: 458-765; Coverage: 39%)
Gene names: BFGFR, CEK, FGFBR, FGFR1, FLG, FLT2, HBGFR
Sequence domains: Protein tyrosine and serine/threonine kinase
Structure domains:

Ligands and Environments

1 bound ligand:
Ligand 66T 2 x 66T
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: NSLS BEAMLINE X29A
Spacegroup: C2
Unit cell:
a: 211.674Å b: 50.148Å c: 66.85Å
α: 90° β: 107.41° γ: 90°
R-values:
R R work R free
0.204 0.2 0.25
Expression system: Escherichia coli BL21(DE3)

Quick links

Citations

16 review citations

FGF/FGFR signaling in health and disease.
Xie et al. (2020)
15 more

4 mentions without citation

Illuminating the molecular mechanisms of tyrosine kinase inhibitor resistance for the FGFR1 gatekeeper mutation: the Achilles' heel of targeted therapy.
Sohl et al. (2015)
3 more