› 4xuf

X-ray diffraction
3.2Å resolution

Crystal structure of the FLT3 kinase domain bound to the inhibitor quizartinib (AC220)

Released:
DOI: 10.2210/pdb4xuf/pdb
PDB entry 4xuf coloured by chain, front view.
PDB entry 4xuf coloured by chain, side view.
PDB entry 4xuf coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Crystal structure of the FLT3 kinase domain bound to the inhibitor Quizartinib (AC220).
Zorn JA, Wang Q, Fujimura E, Barros T, Kuriyan J
PLoS One 10 e0121177 (2015)
PMID: 25837374

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-153242 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Receptor-type tyrosine-protein kinase FLT3 Chains: A, B
Molecule details ›
Chains: A, B
Length: 297 amino acids
Theoretical weight: 33.98 KDa
Source organism: Homo sapiens
Expression system: unidentified baculovirus
UniProt:
  • Canonical: P36888 (Residues: 600-947; Coverage: 31%)
Gene names: CD135, FLK2, FLT3, STK1
Sequence domains: Protein tyrosine and serine/threonine kinase
Structure domains:

Ligands and Environments

1 bound ligand:
Ligand P30 2 x P30
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: ALS BEAMLINE 8.2.2
Spacegroup: P212121
Unit cell:
a: 48.726Å b: 75.492Å c: 153.968Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.299 0.297 0.32
Expression system: unidentified baculovirus

Quick links

Citations

9 review citations

Gilteritinib: potent targeting of FLT3 mutations in AML.
Levis et al. (2020)
8 more

31 mentions without citation

An overview of kinase downregulators and recent advances in discovery approaches.
Wang et al. (2021)
30 more