Targeted protein degradation (TPD) has emerged as a transformative approach in drug discovery, offering a novel strategy to modulate protein levels for therapeutic benefit. Within this paradigm, molecular glues (MG) and proteolysis-targeting chimeras (PROTACs) have gained prominence for their ability to induce the degradation of specific target proteins. However, challenges persist in characterization and rank-ordering of degradation compounds in live cells given the differences in dynamics of protein loss and recovery among compounds. Furthermore, live-cell, kinetic characterizations of TPD induced by PROTACs and MGs have been lacking. Here, we present a suite of luminescence technologies that enable real-time measurement of TPD in live cells. Using bromodomain-containing protein 4 (BRD4) as the model system, we demonstrate the use of HiBiT and NanoBRET® technologies to assess degradation rates, compound permeability, and kinetics for ternary complex formation and ubiquitination. We also present the ViaScript LgBiT mRNA Delivery System and the GloMax® Galaxy Bioluminescent Imager, our next-generation tools to support live-cell kinetic analysis. Together, these assays provide a comprehensive platform for the characterization and optimization of new degrader compounds.
2026 Spring Convention