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 developed 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. 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.