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

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

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 …

Cyclin-dependent kinase 6 (CDK6) is an important regulator of the cell cycle. Together with
CDK4, it phosphorylates and inactivates retinoblastoma (Rb) protein. In tumour cells, CDK6 …

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

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

A focused PROTAC library hijacking cancer therapeutic target CDK6 was developed. A
design principle as “match/mismatch” was proposed for understanding the degradation …

Inhibitors of CDK4 and CDK6 have emerged as important FDA-approved treatment options
for breast cancer patients. The properties and pharmacology of CDK4/6 inhibitor medicines …

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