› 4uwc

X-ray diffraction
1.96Å resolution

Fibroblast growth factor receptor 1 kinase in complex with JK-P3

Released:
DOI: 10.2210/pdb4uwc/pdb
PDB entry 4uwc coloured by chain, front view.
PDB entry 4uwc coloured by chain, side view.
PDB entry 4uwc coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Validation of ion mobility spectrometry - mass spectrometry as a screening tool to identify type II kinase inhibitors of FGFR1 kinase.
Beeston HS, Klein T, Norman RA, Tucker JA, Anderson M, Ashcroft AE, Holdgate GA
Rapid Commun Mass Spectrom e9130 (2021)
PMID: 34038603

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: 309 amino acids
Theoretical weight: 35.14 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

4 bound ligands:
Ligand EDO 12 x EDO
Ligand 4Y0 2 x 4Y0
Ligand PPI 3 x PPI
Ligand SO4 6 x SO4
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: DIAMOND BEAMLINE I02
Spacegroup: C2
Unit cell:
a: 207.464Å b: 58.422Å c: 65.946Å
α: 90° β: 107.38° γ: 90°
R-values:
R R work R free
0.179 0.177 0.206
Expression system: Escherichia coli BL21(DE3)

Quick links

Citations

1 citations in other articles

Exploring the Conformational Landscape and Stability of Aurora A Using Ion-Mobility Mass Spectrometry and Molecular Modeling.
Tomlinson et al. (2022)

2 mentions without citation

Design and Synthesis of Novel Nordihydroguaiaretic Acid (NDGA) Analogues as Potential FGFR1 Kinase Inhibitors With Anti-Gastric Activity and Chemosensitizing Effect.
Chen et al. (2020)
1 more