Development of high-throughput CETSA target engagement assays

National Center For Advancing Translational Sciences

Investigators

Linked publications, trials & patents

Abstract

Demonstrating binding of a small molecule to a target within a cellular environment is valuable for confirming on-target activity. During this period, the collaborative team has continued to develop a real-time CETSA (RT-CETSA) method that can be used to capture kinetic melting profiles of target proteins using a thermally stable NanoLuciferase variant and prototype device to capture luminescence in conjunction with heating. Several new target proteins related to lysosomal function were selected for testing in the RT-CETSA method. The team is continuing to develop the technology to further streamline workflow and improve data acquisition to allow for rapid testing of CETSA for lead optimization and high-throughput screening.