› 1t46

X-ray diffraction
1.6Å resolution

STRUCTURAL BASIS FOR THE AUTOINHIBITION AND STI-571 INHIBITION OF C-KIT TYROSINE KINASE

Released:
DOI: 10.2210/pdb1t46/pdb
PDB entry 1t46 coloured by chain, front view.
PDB entry 1t46 coloured by chain, side view.
PDB entry 1t46 coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Structural basis for the autoinhibition and STI-571 inhibition of c-Kit tyrosine kinase.
Mol CD, Dougan DR, Schneider TR, Skene RJ, Kraus ML, Scheibe DN, Snell GP, Zou H, Sang BC, Wilson KP
J Biol Chem 279 31655-63 (2004)
PMID: 15123710

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 domain:

Structure analysis Details

Assembly composition:
monomeric (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-145426 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Mast/stem cell growth factor receptor Kit Chain: A
Molecule details ›
Chain: A
Length: 313 amino acids
Theoretical weight: 35.39 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P10721 (Residues: 565-935; Coverage: 33%)
Gene names: KIT, SCFR
Sequence domains: Protein tyrosine and serine/threonine kinase
Structure domains:

Ligands and Environments

2 bound ligands:
Ligand PO4 2 x PO4
Ligand STI 1 x STI
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: ALS BEAMLINE 5.0.3
Spacegroup: P3221
Unit cell:
a: 70.089Å b: 70.089Å c: 127.88Å
α: 90° β: 90° γ: 120°
R-values:
R R work R free
0.19 0.188 0.213
Expression system: Spodoptera frugiperda

Quick links

Citations

84 review citations

Cell signaling by receptor tyrosine kinases.
Lemmon et al. (2010)
83 more

95 mentions without citation

Rational, biologically based treatment of EGFR-mutant non-small-cell lung cancer.
Pao et al. (2010)
94 more