PROTAC-biomacromolecule conjugates for precise protein degradation in cancer therapy: A review

Proteolysis targeting chimera (PROTAC) technology is a promising new mode of targeted protein degradation with significant transformative implications for the clinical treatment of different diseases. Nevertheless, while this technology offers numerous advantages, on-target off-tumour toxicity in he...

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Bibliographic Details
Published in:International journal of biological macromolecules 2024-03, Vol.261 (Pt 2), p.129864-129864, Article 129864
Main Authors: Wang, Chao, Zhang, Yujing, Yu, Wanpeng, Xu, Jiazhen, Xing, Dongming
Format: Article
Language:English
Subjects:
Biomacromolecule
Cancer therapy
PBCs
PROTACs
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Summary:Proteolysis targeting chimera (PROTAC) technology is a promising new mode of targeted protein degradation with significant transformative implications for the clinical treatment of different diseases. Nevertheless, while this technology offers numerous advantages, on-target off-tumour toxicity in healthy cells remains a major challenge for clinical application in cancer therapy. Strategies are presently being explored to optimize degradation activity with cellular selectivity to minimize undesirable side effects. PROTAC-antibody conjugates and PROTAC-aptamer conjugates are unique innovations that combine PROTACs and biomacromolecules. These novel PROTAC-biomacromolecule conjugates (PBCs) can enhance the targetability of PROTACs and reduce their off-target side-effects. The combination of potent PROTACs and highly safe biomacromolecules will pioneer an emerging trend in targeted protein degradation. In our review, we have summarized recent advances in PBCs, discussed current challenges, and outlooked opportunities for future research in the field.
ISSN:0141-8130
1879-0003
DOI:10.1016/j.ijbiomac.2024.129864