3DTW: Crystal Structure Of The Vegfr2 Kinase Domain In Complex With A Benzisoxazole Inhibitor

Deregulation of the receptor tyrosine kinase c-Kit is associated with an increasing number of human diseases, including certain cancers and mast cell diseases. Interference of c-Kit signaling with multi-kinase inhibitors has been shown clinically to successfully treat gastrointestinal stromal tumors and mastocytosis. Targeted therapy of c-Kit activity may provide therapeutic advantages against off-target effects for non-oncology applications. A new structural class of c-Kit inhibitors is described, including in vitro c-Kit potency, kinase selectivity, and the observed binding mode.
PDB ID: 3DTWDownload
MMDB ID: 66643
PDB Deposition Date: 2008/7/16
Updated in MMDB: 2008/10
Experimental Method:
x-ray diffraction
Resolution: 2.9  Å
Source Organism:
Similar Structures:
Biological Unit for 3DTW: monomeric; determined by author and by software (PISA)
Molecular Components in 3DTW
Label Count Molecule
Protein (1 molecule)
Vascular Endothelial Growth Factor Receptor 2(Gene symbol: KDR)
Molecule annotation
Chemical (1 molecule)
* Click molecule labels to explore molecular sequence information.

Citing MMDB