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First targeted protein degrader hits the clinic

New therapeutics that harness cellular machinery to degrade targets are entering clinical trials, led by a PROTAC anticancer candidate developed by Arvinas.

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A targeted degrader (multicoloured) binds a target (green) and an E3 ligase (blue), to drive ubiquitylation (purple) and degradation by the proteasome (orange). Credit: Arvinas.

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Nature Reviews Drug Discovery 18, 237-239 (2019)

doi: 10.1038/d41573-019-00043-6

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