National Center for
3DTW: Crystal Structure Of The Vegfr2 Kinase Domain In Complex With A Benzisoxazole Inhibitor
Bioorg. Med. Chem. Lett. (2008) 18 p.5115-5117
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.