Ethan S Toriki, James W Papatzimas, Kaila Nishikawa, Dustin Dovala, Andreas O Frank, Matthew J Hesse, Daniela Dankova, Jae-Geun Song, Megan Bruce-Smythe, Heidi Struble, Francisco J Garcia, Scott M Brittain, Andrew C Kile, Lynn M McGregor, Jeffrey M McKenna, John A Tallarico, Markus Schirle, Daniel K Nomura
Targeted protein degradation with molecular glue degraders has arisen as a powerful therapeutic modality for eliminating classically undruggable disease-causing proteins through proteasome-mediated degradation. However, we currently lack rational chemical design principles for converting protein-targeting ligands into molecular glue degraders. To overcome this challenge, we sought to identify a transposable chemical handle that would convert protein-targeting ligands into molecular degraders of their corresponding targets...
May 24, 2023: ACS Central Science