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Updated: Dec 31, 2025

High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines
Published on: November 9, 2020
Targeted Protein Degradation by Chimeric Small Molecules, PROTACs and SNIPERs
Mikihiko Naito1, Nobumichi Ohoka1, Norihito Shibata1
1Laboratory Molecular Target and Gene Therapy Products, National Institute of Health Sciences, Kawasaki, Japan.
Abstract:
Technologies that induce targeted protein degradation by small molecules have been developed recently. Chimeric small molecules such as Proteolysis Targeting Chimeras (PROTACs) and Specific and Non-genetic IAP-dependent Protein Erasers (SNIPERs), and E3 modulators such as thalidomides, hijack the cellular machinery for ubiquitylation, and the ubiquitylated proteins are subjected to proteasomal degradation. This has motivated drug development in industry and academia because "undruggable targets" can now be degraded by targeted protein degradation.
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