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Optical Control of Small Molecule-Induced Protein Degradation.


ABSTRACT: 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.

SUBMITTER: Naro Y 

PROVIDER: S-EPMC7229639 | biostudies-literature | 2020 Feb

REPOSITORIES: biostudies-literature

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Optical Control of Small Molecule-Induced Protein Degradation.

Naro Yuta Y   Darrah Kristie K   Deiters Alexander A  

Journal of the American Chemical Society 20200123 5


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 cere  ...[more]

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