PDGFR TK assay for screening inhibitory compound-libararies

Introduction: Changes in the expression of platelet-derived growth factor receptor (PDGFR) have been described in gastrointestinal tumors, and correlated with more aggressive behaviour. This finding suggests that blockade of PDGF-dependent growth pathways may be an effective strategy to inhibit growth of these tumors. Our Aim was to set-up and characterize a non-radioactive TK assay platform to screen potential drug-candidate compound libraries designed against the ATP binding site of PDGF receptor, representing a uniform functional target. Methods: An assay based on detection of phosphorylated substrate was est…