Abstract

Correlation of Kinetic Inhibitory Ligand Binding with 3D Tumor Invasion for the Evaluation of anti-Metastatic Effects of CXCR4 Inhibitors

Peter Banks, Scientific Director, BioTek Instruments Inc

Here we examine the drug-target residence time of various CXCR4 inhibitors using a direct, homogeneous ligand binding assay and CXCR4 expressing cell line. This inhibitor panel was further tested in a 3D tumor invasion assay to determine whether there is a correlation between the molecule’s CXCR4 residence time and inhibition of the phenotypic effect of tumor invasion. Results indicated that drug-target residence times longer than the cognate CXCR4 ligand demonstrate highest inhibition in the 3D tumor invasion assay.