The investigational drugs E7820, indisulam and tasisulam (aryl-sulfonamides) promote the
degradation of the splicing factor RBM39 in a proteasome-dependent mechanism. While the …

Molecular-glue-mediated proximity-induced degradation now allows unprecedented
therapeutic targeting of previously undruggable proteins. Structures showing how aryl …

E7820 and indisulam are two examples of aryl sulfonamides that recruit RBM39 to Rbx-Cul4-
DDA1-DDB1-DCAF15 E3 ligase complex, leading to its ubiquitination and degradation by …

Molecular glues (MGs) are monovalent small molecules that induce an interaction between
proteins (native or non-native partners) by altering the protein–protein interaction (PPI) …

Small molecules that induce protein-protein interactions to exert proximity-driven
pharmacology such as targeted protein degradation are a powerful class of therapeutics 1 …

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

The anticancer agent indisulam inhibits cell proliferation by causing degradation of RBM39,
an essential mRNA splicing factor. Indisulam promotes an interaction between RBM39 and …

Molecular glue degraders (MGDs) are small molecules that degrade proteins of interest via
the ubiquitin–proteasome system. While MGDs were historically discovered serendipitously …

Targeted protein degradation (TPD) is a new pharmacology based on small-molecule
degraders that induce proximity between a protein of interest (POI) and an E3 ubiquitin …

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 …