Abstract
In cancer diagnosis and treatment, ‘accurate diagnosis’ and ‘targeted therapy’ are the primary focus and key goals of many research groups. Metal–organic frameworks (MOFs) have attracted considerable attention in cancer diagnosis and treatment owing to their structural diversity and multifunctionality. Starting in 2010, MOFs with targeting capabilities have been gradually developed and applied in the field of biomedicine. This Review provides readers with a simple guide to help design bioenabled MOFs for specific bioapplications. First, construction strategies of MOFs with targeting functions are classified, including non-covalent interaction, covalent interaction and coordinative interaction strategies. Then, the applications of MOFs modified by antibodies, peptides, aptamers, carbohydrates, cell membranes and other targeting strategies are discussed. Finally, the future challenges and prospects for constructing MOFs with targeting functionalities are outlined to provide guidelines for the next generation of MOFs capable of achieving accurate cancer diagnosis and treatment and to accelerate the development of MOFs in clinical applications.

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Acknowledgements
M.L. thanks the support of the National Natural Science Foundation of China (grant no. 2230822), Shenzhen University Third-Phase Project of Constructing High-Level University (grant no. 000001032104), the Research Team Cultivation Program of Shenzhen University (grant no. 2023QNT005) and Guangdong Province Key Areas Special Project for Regular Colleges and Universities (grant no. 2024ZDZX2018). The authors also thank the support from the Shenzhen University 2035 Program for Excellent Research (nos. 00000208 and 00000225) and the Shenzhen Science and Technology Program (grant no. RCBS20231211090515015). X.C. thanks the support of the Guangdong Basic and Applied Basic Research Foundation (2023B1515120001). P.T. thanks the support of the China Postdoctoral Science Foundation (grant no. 2025M771167). T.D.J. thanks the University of Bath and the Open Research Fund of the School of Chemistry and Chemical Engineering, Henan Normal University (2020ZD01) for their support.
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Tong, P., Wang, R., Zhou, Y. et al. Enhancing the targeting ability of metal–organic frameworks in cancer therapy and diagnosis. Nat Rev Chem (2026). https://doi.org/10.1038/s41570-026-00807-w
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DOI: https://doi.org/10.1038/s41570-026-00807-w


