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Updated: Jul 2, 2026
High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines
Published on: November 9, 2020
Mechanisms that matter: unbiased cellular screening for degraders
Helen E Burston1, Elizabeth M Rosethorne2, Francesca Cavallo2
1Sygnature Discovery, Saint-Laurent, QC, Canada.
None:
Recent discoveries have highlighted that small monovalent molecules can leverage a variety of cellular mechanisms to induce degradation of a specific target protein. This perspective exemplifies and contextualizes these mechanisms within drug discovery, with a focus on identification of novel monovalent degraders via cell-based high-throughput screening (HTS) methodologies. Considerations for screening strategies, assay technologies and mechanistic deconvolution are discussed, with emphasis on identification of degrader compounds from diverse compound collections.
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