![]() Our lead compounds display little or no activity in the dark but can be reversibly activated with different wavelengths of light. We demonstrate this concept by using PHOTACs that target either BET family proteins (BRD2,3,4) or FKBP12. ![]() These trifunctional molecules, which we named PHOTACs (PHOtochemically TArgeting Chimeras), consist of a ligand for an E3 ligase, a photoswitch, and a ligand for a protein of interest. ![]() We now introduce photoswitchable PROTACs that can be activated with the spatiotemporal precision that light provides. They have emerged as powerful tools to control the levels of specific cellular proteins. PROTACs (PROteolysis TArgeting Chimeras) are bifunctional molecules that target proteins for ubiquitylation by an E3 ligase complex and subsequent degradation by the proteasome.
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