Molecular glue compounds induce protein–protein interactions that, in the context of a
ubiquitin ligase, lead to protein degradation. Unlike traditional enzyme inhibitors, these …

Targeted protein degradation is a new therapeutic modality based on drugs that destabilize
proteins by inducing their proximity to E3 ubiquitin ligases. Of particular interest are …

Molecular glue degraders are an effective therapeutic modality, but their design principles
are not well understood. Recently, several unexpectedly diverse compounds were reported …

Molecular-glue degraders mediate interactions between target proteins and components of
the ubiquitin-proteasome system to cause selective protein degradation. Here, we report a …

The design of selective small molecules is often stymied by similar ligand binding pockets.
Here, we report BSJ-03-123, a phthalimide-based degrader that exploits protein-interface …

Protein ubiquitination is a common form of post-translational modification that regulates a
broad spectrum of protein substrates in diverse cellular pathways. Through a three-enzyme …

Targeted protein degradation with molecular glue degraders has arisen as a powerful
therapeutic modality for eliminating classically undruggable disease-causing proteins …

Abstract Cyclin-dependent kinase 2 (CDK2) complex is significantly over-activated in many
cancers. While it makes CDK2 an attractive target for cancer therapy, most inhibitors against …

D-type cyclins are central regulators of the cell division cycle and are among the most
frequently deregulated therapeutic targets in human cancer, but the mechanisms that …

Molecular glue degraders are small, drug-like compounds that induce interactions between
an E3 ubiquitin ligase and a target, which result in ubiquitination and subsequent …