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

Targeted protein degradation (TPD) holds immense promise for drug discovery, but
mechanisms of acquired resistance to degraders remain to be fully identified. Here, we used …

Target-protein degradation is an emerging field in drug discovery and development. In
particular, the substrate-receptor proteins of the cullin–ubiquitin ligase system play a key …

Ligand-dependent protein degradation has emerged as a compelling strategy to
pharmacologically control the protein content of cells. So far, however, only a limited number …

Indisulam and related sulfonamides recruit the splicing factor RBM39 to the CRL4-DCAF15
E3 ubiquitin ligase, resulting in RBM39 ubiquitination and degradation. Here, we used a …

Targeted protein degradation relies on small molecules that induce new protein–protein
interactions between targets and the cellular protein degradation machinery. Most of these …

Small-molecule-induced protein depletion technologies, also called inducible degrons,
allow degradation of genetically engineered target proteins within cells and animals. Here …

Heterobifunctional small-molecule degraders that induce protein degradation through ligase-
mediated ubiquitination have shown considerable promise as a new pharmacological …

Targeted protein degradation (TPD) by PROTACs is a promising strategy to control disease-
causing protein levels within the cell. While TPD is emerging as an innovative drug …

Engineered destruction of target proteins by recruitment to the cell's degradation machinery
has emerged as a promising strategy in drug discovery. The majority of molecules that …