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 …

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

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

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

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) …

Targeted protein degradation has arisen as a powerful strategy for drug discovery allowing
the targeting of undruggable proteins for proteasomal degradation. This approach most …

Ligand-induced protein degradation has emerged as a compelling approach to promote the
targeted elimination of proteins from cells by directing these proteins to the ubiquitin …

Targeted protein degradation (TPD) has emerged as a powerful tool in drug discovery for
the perturbation of protein levels using heterobifunctional small molecules. E3 ligase …

BRD4, a bromodomain and extraterminal domain (BET) family member, is an attractive
target in multiple pathological settings, particularly cancer. While BRD4 inhibitors have …

As an emerging drug discovery paradigm, Proteolysis targeting chimeras (PROTACs)
facilitate ubiquitination and degradation of the targets by cellular endogenous proteasome …