(1101-B) The use of SureFire Ultra assays to demonstrate PROTAC mediated degradation and the effects on signalling pathways.

Abstract: The SureFire Ultra assay is a sensitive, rapid, homogeneous bead-based method that is suitable for small scale use but is also amenable to automation and high throughput screening. The SureFire Ultra technology has been developed to provide exceptional assay sensitivity and enhanced signal windows for kinase screening programs. Endogenous cellular phosphorylation can be measured in all types of cellular extracts including cultured cells, tissue lysates and samples containing high to low antibody titers. The assays have low background which allows at the same time for the measurement of low levels of pathway activation. The portfolio covers a wide range of signalling pathways including PI3K/AKT/MAPK signaling, cell cycle regulation, neuroscience and autophagy.
SureFire Ultra offers a broad range of kits targeted to phospho proteins but there has been a more recent focus on Total assay development. These Total assays can be used to demonstrate targeted degradation by PROTAC compounds in a cellular context. PROTAC compounds have gained a lot of recent attention as a strategy to target disease related proteins for degradation in a manner that is specific, with lower toxicity than traditional drugs as well as targeting proteins that were previously considered undruggable.
This study will highlight the use of SureFire Ultra assays to demonstrate the efficacy of PROTAC compounds and their effect on downstream signalling events.