Proteolysis-Targeting Chimeras in Cancer Therapy: Targeted Protein Degradation for Next-Generation Treatment

Proteolysis-targeting chimeras (PROTACs) are a promising advancement in cancer therapy, enabling targeted degradation of oncogenic proteins, including those previously considered "undruggable." They utilize the ubiquitin-proteasome system to selectively suppress disease-causing proteins with lower doses and reduced toxicity compared to traditional inhibitors. PROTACs have shown efficacy in treating various cancers, such as prostate and breast cancer, with candidates like ARV-110 and ARV-471 advancing in clinical trials. Despite challenges like optimizing pharmacokinetics and delivery, ongoing research is enhancing their potential as a next-generation platform for personalized cancer therapy. Additionally, GT20029 is in a Phase 1 clinical trial for androgenetic alopecia, targeting the androgen receptor through PROTAC-mediated degradation.