Stick it to E3s

The limited availability of small-molecule ligands for E3 ubiquitin ligases stymies the development of next-generation degraders. Two recent papers report the identification of novel, covalent and PROTAC-compatible ligands that hijack the previously untargeted ligases RNF114 and DCAF16.

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Fig. 1: Out of around 600 E3 ligases, only a small subset is amenable for targeted protein degradation.


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Correspondence to Georg E. Winter.

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Brand, M., Winter, G.E. Stick it to E3s. Nat Chem Biol 15, 655–656 (2019).

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