TL;DR
This chapter presents a protocol for the best practice use of UPS-targeting tool compounds to further understand their molecular mechanism of action within the CRBN- and VHL-mediated degradation pathways in human cells.
Summary. Targeted protein degradation (TPD) is a modern strategy for developing new therapeutic agents that requires not only detection of decreased target abundance but also stepwise validation of the compound’s mechanism of action. In this approach, the disappearance of the target protein is necessary but insufficien...
Breast cancer is one of the most significant health issues in the world, and resistance to treatment and a lack of targets that can be addressed with drugs limit the effectiveness of the existing treatment options. The development of proteolysis-targeting chimeras (PROTACs) has shifted the concept of occupancy-based in...
The biological functions of the 19S regulatory particle, its role in cancer pathogenesis, and emerging therapeutic strategies targeting 19S-associated proteins to improve outcomes in hematologic malignancies are discussed.
This review summarizes the development of classical small-molecule E3 ligase ligands and highlights emerging biological recruitment strategies involving antibodies, nanobodies, aptamers, peptides, and engineered proteins that provide greater programmability and selectivity.
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