› 4v01

X-ray diffraction
2.33Å resolution

FGFR1 in complex with ponatinib (co-crystallisation).

Released:
DOI: 10.2210/pdb4v01/pdb
PDB entry 4v01 coloured by chain, front view.
PDB entry 4v01 coloured by chain, side view.
PDB entry 4v01 coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Structural insights into FGFR kinase isoform selectivity: diverse binding modes of AZD4547 and ponatinib in complex with FGFR1 and FGFR4.
Tucker JA, Klein T, Breed J, Breeze AL, Overman R, Phillips C, Norman RA
Structure 22 1764-1774 (2014)
PMID: 25465127

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
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

3 bound ligands:
Ligand SO4 6 x SO4
Ligand EDO 10 x EDO
Ligand 0LI 2 x 0LI
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: RIGAKU FR-E
Spacegroup: C2
Unit cell:
a: 207.255Å b: 58.09Å c: 65.231Å
α: 90° β: 107.38° γ: 90°
R-values:
R R work R free
0.191 0.189 0.238
Expression system: Escherichia coli

Quick links

Citations

11 review citations

Small molecules in targeted cancer therapy: advances, challenges, and future perspectives.
Zhong et al. (2021)
10 more

8 mentions without citation

FGFR-TKI resistance in cancer: current status and perspectives.
Yue et al. (2021)
7 more