Advancing Design Strategy of PROTACs for Cancer Therapy

    June 2025 in “ MedComm
    Hang Luo, Yuan Tian, Razack Abdullah, Bao‐Ting Zhang, Yuan Ma, Ge Zhang
    Proteolysis targeting chimeras (PROTACs) are a promising class of anticancer therapeutics that utilize the ubiquitin-proteasome system to degrade targeted proteins. Despite their potential, designing effective PROTACs remains challenging. This review provides an overview of the components involved in PROTAC design, including POI ligands, E3 ligands, and linkers, and highlights the role of artificial intelligence in optimizing these elements. The review also discusses the current applications and challenges of PROTACs in cancer therapy and suggests future directions for their development by integrating multidisciplinary technologies.
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