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"Automated Profiling Of PROTAC-Induced Cereblon Neosubstrate Degradation Using Simple Western"

This application note from Bio-Techne discusses the application of PROTAC (PROteolysis TArgeting Chimeras) Degraders, a class of heterobifunctional small molecules that selectively degrade target proteins within cells via the ubiquitin-proteasome system, thus expanding the druggable proteome.

These Degraders are modular in design, including an E3 ubiquitin ligase ligand, a chemical linker, and a “warhead ligand” for a target protein, and are particularly effective when applied to cereblon, an E3 ligase often used in PROTAC Degrader development programs.

To determine the efficiency of Degraders, the paper highlights the use of the Simple Western platform, which allows for rapid and quantitative characterization of degradation constant values. This automated immunoassay platform generates highly reproducible and quantifiable data, producing up to 96 data points in a single overnight run and thus making it an ideal solution for studying Degraders. The paper presents data demonstrating the power of this platform in screening panels of Degrader and IMiD compounds to quantify degradation activity.

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