› 4nks

X-ray diffraction
2.5Å resolution

Crystal structure of human fibroblast growth factor receptor 1 kinase domain in complex with pyrazolaminopyrimidine 3

Released:
DOI: 10.2210/pdb4nks/pdb
PDB entry 4nks coloured by chain, front view.
PDB entry 4nks coloured by chain, side view.
PDB entry 4nks coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
FGFR1 Kinase Inhibitors: Close Regioisomers Adopt Divergent Binding Modes and Display Distinct Biophysical Signatures.
Klein T, Tucker J, Holdgate GA, Norman RA, Breeze AL
ACS Med Chem Lett 5 166-71 (2014)
PMID: 24900792

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)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Fibroblast growth factor receptor 1 Chains: A, B
Molecule details ›
Chains: A, B
Length: 309 amino acids
Theoretical weight: 35.14 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
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 2M2 2 x 2M2
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: ESRF BEAMLINE ID14-4
Spacegroup: C2
Unit cell:
a: 208.058Å b: 56.918Å c: 66.242Å
α: 90° β: 107.73° γ: 90°
R-values:
R R work R free
0.223 0.22 0.278
Expression system: Escherichia coli

Quick links

Citations

1 review citation

Functional proteomics of the epigenetic regulators ASXL1, ASXL2 and ASXL3: a convergence of proteomics and epigenetics for translational medicine.
Katoh M. (2015)
4 other articles

1 mention without citation

Landscape of activating cancer mutations in FGFR kinases and their differential responses to inhibitors in clinical use.
Patani et al. (2016)