Lessons learned in linking PROTACs from discovery to the clinic
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A Pike, ECY Lee, IN Michaelides, M Schade…
Nature Reviews …, 2025
nature.com
Targeted protein degradation has the potential to deliver greater efficacy than conventional receptor antagonists or enzyme inhibitors and address previously undruggable targets. This has driven a recent surge of interest in protein degradation modalities. Bifunctional degraders, specifically proteolysis targeting chimeras (PROTACs), have become a key modality in the protein degrader space, despite the physicochemical challenges they present in achieving oral bioavailability. In this Review, we discuss the lessons learned to …
