Optical Control of Small Molecule-Induced Protein Degradation
As an emerging approach to protein perturbation, small molecule-induced protein degradation has gained significant attention as both a chemical tool and a potential therapeutic. To enable discrete control over its function, we have developed a broadly applicable approach for the optical activation o...
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Veröffentlicht in: | Journal of the American Chemical Society 2020-02, Vol.142 (5), p.2193-2197 |
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creator | Naro, Yuta Darrah, Kristie Deiters, Alexander |
description | As an emerging approach to protein perturbation, small molecule-induced protein degradation has gained significant attention as both a chemical tool and a potential therapeutic. To enable discrete control over its function, we have developed a broadly applicable approach for the optical activation of small molecule-induced protein degradation. By installing two different photolabile protecting groups, so-called caging groups, onto two different ligands recruiting Von Hippel–Lindau (VHL) and cereblon (CRBN) E3 ubiquitin ligases, our strategy enables light-triggered protein degradation for any small molecule warhead. |
doi_str_mv | 10.1021/jacs.9b12718 |
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subjects | Ligands protein degradation Proteolysis Small Molecule Libraries - chemistry therapeutics ubiquitin-protein ligase Ubiquitin-Protein Ligases - metabolism Ubiquitination |
title | Optical Control of Small Molecule-Induced Protein Degradation |
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