Bifunctional Molecules beyond PROTACs.

Heterobifunctional molecules, which recruit E3 ligases to ubiquitinate a target protein of interest, have found wide application as both biological tools and molecules with the potential to have clinical effects. In their recent paper, Yamazoe et al. report a heterobifunctional molecule that recruits the phosphatase PP1 to promote the dephosphorylation of pAKT to give AKT. This Viewpoint seeks to place this work in the wider context of heterobifunctional molecules and looks ahead to new possibilities presented by these results.