Author/Authors :
Roxanne K. Kunz، نويسنده , , Shannon Rumfelt، نويسنده , , Ning Chen، نويسنده , , Dawei Zhang، نويسنده , , Andrew S. Tasker، نويسنده , , Roland Bürli، نويسنده , , Randall Hungate، نويسنده , , Violeta Yu، نويسنده , , Yen Nguyen، نويسنده , , Douglas A. Whittington، نويسنده , , Kristin L. Meagher، نويسنده , , Matthew Plant، نويسنده , , Yanyan Tudor، نويسنده , , Michael Schrag، نويسنده , , Yang Xu، نويسنده , , Gordon Y. Ng، نويسنده , , Essa Hu، نويسنده ,
Abstract :
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.
