Extrapolating Lessons from Targeted Protein Degradation to Other Proximity-Inducing Drugs
Georg E. Winter
Abstract:Targeted protein
degradation (TPD) is an emerging pharmacologic
strategy. It relies on small-molecule “degraders” that
induce proximity of a component of an E3 ubiquitin ligase complex
and a target protein to induce target ubiquitination and subsequent
proteasomal degradation. Essentially, degraders thus expand the function
of E3 ligases, allowing them to degrade proteins they would not recognize
in the absence of the small molecule. Over the past decade, insights
gained from identifying, designing, and charac… Show more
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