Selectivity profiling and off-target identification of clinically relevant kinase inhibitors for gastrointestinal tumors

Targeted inhibition of protein kinases by small molecule drugs has evolved into a viable approach for anticancer therapy. These inhibitors are widely used in signal transduction therapy, although the true selectivity of them has remained unclear. Recently several kinase inhibitors have been used for Gastrointestinal tumors. We have developed a chemical derivatization based affinity chromatography technology for selectivity profiling and off-target identification of kinase inhibitors. The strategic relevance of the KinaTor™ technology in lead optimization is twofold. Firstly, it provides the selectivity panel for…