Proteolysis targeting chimeras (PROTACs) technology is a novel and promising therapeutic
strategy using small molecules to induce ubiquitin-dependent degradation of proteins. It has …

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

Carbon–heteroatom bonds, most often amide and ester bonds, are the standard method to
link together two complex fragments because carboxylic acids, amines, and alcohols are …

Compared with traditional therapies, targeted therapy has merits in selectivity, efficacy, and
tolerability. Small molecule inhibitors are one of the primary targeted therapies for cancer …

Proteolysis-targeting chimeras (PROTACs) as an emerging drug discovery modality has
been extensively concerned in recent years. Over 20 years development, accumulated …

Exploring the response of malignant cells to intracellular metabolic stress is critical for
understanding pathologic processes and developing anticancer therapies. Herein, we …

Despite significant progress in clinical management, drug resistance remains a major
obstacle. Recent research based on protein degradation to restrain drug resistance has …

Proteolysis targeting chimera (PROTAC) degradation of pathogenic proteins by hijacking of
the ubiquitin-proteasome-system has become a promising strategy in drug design. The …

Over the last two decades, proteolysis targeting chimeras (PROTACs) have been
revolutionary in drug development rendering targeted protein degradation (TPD) as an …

Targeted protein degraders such as PROTACs and molecular glues are a rapidly emerging
therapeutic modality within industry and academia. Degraders possess unique mechanisms …