Work

Optical Control of Small Molecule-Induced Protein Degradation

Year: 2020

Type: article

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.

Source: Journal of the American Chemical Society

DOI: 10.1021/jacs.9b12718

Authors: Yuta Naro, Kristie Darrah, Alexander Deiters

Institution: University of Pittsburgh

Language: English

Topic: Protein Degradation and Inhibitors

Subfield: Molecular Biology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

Open Access status: green

Funders: University of Pittsburgh, National Cancer Institute, National Institute of General Medical Sciences, National Institute of Allergy and Infectious Diseases

Awards: G1275542470, Conditional Control of Drug Function Through α-Boryl Ether Oxidation, G741073515