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Locally unlocks prodrugs by radiopharmaceutical in tumor for cancer therapy

Science Bulletin 2024年第17期69卷 2745-2755页

作者： Changlun Wang Mengxin Xu Zihang Zhang Senhai Zeng Siyong Shen Zexuan Ding Junyi Chen Xi-Yang Cui Zhibo Liu Beijing National Laboratory for Molecular Sciences Radiochemistry and Radiation Chemistry Key Laboratory of Fundamental ScienceKey Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of EducationCollege of Chemistry and Molecular EngineeringPeking UniversityBeijing 100871China Peking University-Tsinghua University Center for Life Sciences Peking UniversityBeijing 100871China Changping Laboratory Beijing 102206China Key Laboratory of Carcinogenesis and Translational Research of Ministry of Education Key Laboratory for Research and Evaluation of Radiopharmaceuticals of National Medical Products AdministrationDepartment of Nuclear MedicinePeking University Cancer HospitalBeijing 100142China

Chemotherapy is the first-line treatment for cancer, but its systemic toxicity can be severe. Tumorselective prodrug activation offers promising opportunities to reduce systemic toxicity. Here, we present a strategy for activating prodrugs using radiopharmaceuticals. This strategy enables the targeted release of chemotherapeutic agents due to the high tumor-targeting capability of radiopharmaceuticals. [^(18)F]FDG(2-[^(18)F]-fluoro-2-deoxy-D-glucose), one of the most widely used radiopharmaceuticals in clinics, can trigger Pt(IV) complex for controlled release of axial ligands in tumors, it might be mediated by hydrated electrons generated by water radiolysis resulting from the decay of radionuclide18F. Its application offers the controlled release of fluorogenic probes and prodrugs in living cells and tumor-bearing mice. Of note,an OxaliPt(IV) linker is designed to construct an [^(18)F]FDG-activated antibody-drug conjugate(Pt-ADC).Sequential injection of Pt-ADC and [^(18)F]FDG efficiently releases the toxin in the tumor and remarkably suppresses the tumor growth. Radiotherapy is booming as a perturbing tool for prodrug activation,and we find that [^(18)F]FDG is capable of deprotecting various radiotherapy-removable protecting groups(RPGs). Our results suggest that tumor-selective radiopharmaceutical may function as a trigger, for developing innovative prodrug activation strategies with enhanced tumor selectivity.

关键词： prodrugactivation Radiopharmaceutical Radiochemistry [^(18)F]FDG Platinum(IV)prodrug

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