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Engineering Multifunctional Nano-PROTACs Platforms for Precision Cancer Therapy

Authors: NING Yingyi; WU Yuanhao; SU Linzhu; LIU Jianfeng; HUANG Fan

DOI: 10.1007/s40843-026-4383-8Status: Verified Translated Edition
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Key Findings in This Report

• • PROTACs exhibit high molecular weight and poor bioavailability, which limit passive tumor accumulation; nanoencapsulation addresses these by improving solubility and stability, potentially increasing intratumoral drug exposure by orders of magnitude compared to free PROTACs. • • Nanocarriers enable spatiotemporally controlled release via passive (EPR effect) or active targeting, reducing systemic toxicity; this is critical because off-tumor PROTAC activity can degrade healthy tissue proteins, leading to dose-limiting toxicities. • • The integration of PROTACs with nanotechnology facilitates synergistic combination therapies, e.g., with radiotherapy or immunotherapy, potentially overcoming acquired resistance mechanisms such as target mutation and pathway rewiring. • • Clinical translation of nano-PROTACs faces scalability and manufacturing challenges, including batch-to-batch reproducibility and long-term stability; however, the platform's modularity supports personalized targeting ligands, aligning with precision oncology paradigms.