Cross-coupling reactions have played a critical role enabling the rapid expansion of
structure–activity relationships (SAR) during the drug discovery phase to identify a clinical …

Molecularly targeted cancer therapies substantially improve patient outcomes, although the
durability of their effectiveness can be limited. Resistance to these therapies is often related …

Proteolysis targeting chimera (PROTAC), hijacking protein of interest (POI) and recruiting E3
ligase for target degradation via the ubiquitin-proteasome pathway, is a novel drug …

Protein degradation technology has progressed dramatically since 2001 when proteolysis
targeting chimera (PROTAC) was first reported. Various of distinctive degradation …

In the past two decades, we have witnessed the discovery and development of many potent
and efficacious proteolysis-targeting chimera (PROTAC) degraders, with several in phase I/II …

Targeted protein degradation (TPD), the ability to control a proteins fate by triggering its
degradation in a highly selective and effective manner, has created tremendous excitement …

Hetero-bifunctional PROteolysis TArgeting Chimeras (PROTACs) represent a new emerging
class of small molecules designed to induce polyubiquitylation and proteasomal-dependent …

Highlights•AR is a clinically fully validated target for treatment of human prostate
cancer.•PROTAC AR degraders overcome common resistance mechanisms developed …

The key proteins involved in transcriptional regulation play convergent roles in cellular
homeostasis, and their dysfunction mediates aberrant gene expressions that underline the …

Ferroptosis is an iron-dependent, non-apoptotic form of cell death involving in various
disease processes. Mechanistically, glutathione peroxidase 4 (GPX4) which belongs to the …