qHTS to Identify Substrates of P-glycoprotein (P-gp) and Collateral Sensitivity agents of P-gp-expressing Cancer Cells

National Center For Advancing Translational Sciences

Investigators

Abstract

ETB is aiming to identify P-gp substrates within its libraries to provide early filters of P-gp transport potential, as well as developing compounds capable of selectivity killing P-gp expressing cells (as anticancer agents). During this period, the project team cherry-picked 161 hits and evaluated them in both shift assay (two sets of cell lines) and matrix assay. 93 hits were confirmed in both assays. We also checked the activity of these compounds in human ABCG2 substrates in zebrafish homologs. We found that there are 30 potentials substrates of zebrafish homologs. Currently we are completing the project for publication.