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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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Structural Investigation of Technetium-Diphosphonate Complex 99mTc-MDP

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Chinese Journal of Chemical Physics 2011年第3期24卷 295-304,I0003页

作者：邱玲林建国居学海贡雪东罗世能江苏省原子医学研究所卫生部核医学重点实验室江苏省分子核医学重点实验室无锡214063 南京理工大学化工学院分子与材料计算研究所南京210094

Density functional theory method has been employed to investigate the structures of the prototypical technetium-labeled diphosphonate complex 99mTc-MDP, where MDP represents methylenediphosphonic acid. A total of 14 trial structures were generated by allowing for the geometric, conformational, charge, and spin isomerism. Based on the optimized structures and calculated energies at the B3LYP/LANL2DZ level, two stable isomers were determined for the title complex. And they were further studied systematically in comparison with the experimental structure. The basis sets 6-31G＊（LANL2DZ for Tc）, 6-31G＊（cc-pVDZ-pp for Tc）, and DGDZVP have also been employed in combination with the B3LYP functional to study the basis set effect on the geometries of isomers. The optimized structures agree well with the available experimental data, and the bond lengths are more sensitive to the basis set than the bond angles. The charge distributions were studied by the Mulliken population analysis and natural bond orbital analysis. The results reflect a significant ligand-to-metal electron donation.

关键词： radiopharmaceutical 99mTc-methylenediphosphonate Structural prediction Density functional theory Basis set effect

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Bone-targeted therapies to reduce skeletal morbidity in prostate cancer

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Asian Journal of Andrology 2018年第3期20卷 215-220页

作者： Tanya B Dorff Neeraj Agarwal USC Keck School of Medicine USC Norris Comprehensive Cancer Center Genitourinary Oncology Los Angeles CA 90033 USA Hunts Man Cancer Institute Universityof Utah 2000 Circle of Hope Salt Lake City UT 84112 USA

Bone metastases are the main driver of morbidity and mortality in advanced prostate cancer. Targeting the bone microenvironment, a key player in the pathogenesis of bone metastasis, has become one of the mainstays of therapy in men with advanced prostate cancer. This review will evaluate the data supporting the use of bone-targeted therapy, including （1） bisphosphonates such as zoledronic acid, which directly target osteoclasts, （2） denosumab, a receptor activator of nuclear factor-kappa B （RANK） ligand inhibitor, which targets a key component of bone stromal interaction, and （3） radium-223, an alpha-emitting calcium mimetic, which hones to the metabolically active areas of osteoblastic metastasis and induces double-strand breaks in the DNA. Denosumab has shown enhanced delay in skeletal-related events compared to zoledronic acid in patients with metastatic castration-resistant prostate cancer （mCRPC）. Data are mixed with regard to pain control as a primary measure of efficacy. New data call into question dosing frequency, with quarterly dosing strategy potentially achieving similar effect compared to monthly dosing for zoledronic acid. In the case of radium-223, there are data for both pain palliation and improved overall survival in mCRPC. Further studies are needed to optimize timing and combination strategies for bone-targeted therapies. Ongoing studies will explore the impact of combining bone-targeted therapy with investigational therapeutic agents such as immunotherapy, for advanced prostate cancer. Future studies should strive to develop biomarkers of response, in order to improve efficacy and cost-effectiveness of these agents.

关键词： bisphosphonate bone metastases prostate cancer radiopharmaceutical receptor activator of nuclear factor-kappa B-ligand

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A PET probe targeting polyamine transport system for precise tumor diagnosis and therapy

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Asian Journal of Pharmaceutical Sciences 2024年第3期19卷 146-159页

作者： Ming Zhou Xiaoqin Yin Bei Chen Shuo Hu Wenhu Zhou Department of Nuclear Medicine Xiangya HospitalCentral South UniversityChangsha 410008China Xiangya School of Pharmaceutical Sciences Central South UniversityChangsha 410013China Key Laboratory of Biological Nanotechnology of National Health Commission Changsha 410008China National Clinical Research Center for Geriatric Disorders(Xiangya) Changsha 410008China

Polyamine metabolism dysregulation is a hallmark of many cancers,offering a promising avenue for early tumor *** study presents the development of a nuclear probe derived from spermidine(SPM)for dual-purpose tumor PET imaging and internal radiation *** probe,radiolabeled with either[68Ga]Ga for diagnostic applications or[177Lu]Lu for therapeutic use,was synthesized with exceptional purity,stability,and specific *** testing involving 12 different tumor cell lines revealed remarkable specificity towards B16 melanoma cells,showcasing outstanding tumor localization and target-to-non-target *** investigations employing polyamines,non-labeled precursor,and polyamine transport system(PTS)inhibitor,consistently affirmed the probe?s targetability through recognition of the ***,while previous reports indicated PTS upregulation in various tumor types for targeted therapy,this study observed no positive signals,highlighting a concentration-dependent discrepancy between targeting for therapy and ***,when labeled with[177Lu],the probe demonstrated its therapeutic potential by effectively controlling tumor growth and extending mouse *** into biodistribution,excretion,and biosafety in healthy humans laid a robust foundation for clinical *** study introduces a versatile SPM-based nuclear probe with applications in precise tumor theranostics,offering promising prospects for clinical implementation.

关键词： PET imaging Polyamine metabolism Spermine radiopharmaceutical Melanoma

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Comparison between Two Ethanolic Solutions for 3’-Deoxy-3’-[18F]Fluorothymidine Elution

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Advances in Chemical Engineering and Science 2017年第1期7卷 23-33页

作者： Leonardo T. C. Nascimento Marina B. Silveira Soraya M. Z. M. D. Ferreira Juliana B. Silva Centro de Desenvolvimento da Tecnologia Nuclear CDTN Belo Horizonte Brasil

3’-Deoxy-3’-[18F]Fluorothymidine—[18F]FLT is a Positron Emission Tomography (PET) tracer which has been used for noninvasive assessment of proliferation activity in several types of cancer. During the past few years, some novel approaches for [18F]FLT synthesis have been developed, mainly focused on optimization of reaction conditions and purification methods. The present study reports the use of two different eluents in the final step of [18F]FLT production and the evaluation of its effect on radiochemical yield and product quality. The first eluent evaluated was water: ethanol (90:10, v/v), commercially available, and the second was NaCl 0.9% (saline): ethanol (92:8, v/v). The mean of the corrected radiochemical yields corresponded to 27% ± 7% for elution with water and ethanol and to 23% ± 3% for elution with saline and ethanol, which could indicate that the eluent solutions have similar elution strength. Besides, quality control results were in accordance with the requirements and demonstrated that there was no significant difference between both formulations. Considering that pharmaceutical preparations containing ethanol should be preferentially diluted with saline to avoid hemolysis, the eluent saline:ethanol (92:8, v/v) was chosen for [18F]FLT extraction and final formulation.

关键词： [18F]FLT Synthesis Quality Control Formulation Elution radiopharmaceutical

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What Is Exactly the Scope of Nuclear Chemistry and Its Educational Position between Other Chemistry Branches

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Advances in Chemical Engineering and Science 2017年第1期7卷 60-75页

作者： Turan ünak Nuclear Chemistry Ege University Izmir Turkey üNAK’lar Company Izmir Turkey

The undergraduate chemistry programs of different universities across the world show clearly that nuclear chemistry education doesn’t have a permanent status in chemistry curricula like classical sub-branches of chemistry which means like organic, inorganic, analytical, physical, and biochemistry. Before starting the evaluation of the status of nuclear chemistry education, first of all, nuclear chemistry should correctly be defined and its position in chemistry education programs should correctly be determined. In addition, a confusion of terminology or at least, a terminological turbulence exists in this branch of chemistry about the use of terms such as nuclear chemistry, radiochemistry, nuclear and radiochemistry. Also, the scopes of the expressions used in this field such as radiochemistry, radiation chemistry, radiopharmaceutical chemistry, etc. should be exactly defined and the realtions between them should be clearly understood. Breifly, nuclear chemistry may be difined as a large umbrella which covers all chemical studies related to radioactive materials and nuclear radiation including the fine sub-branches such as radiochemistry, radiation chemistry, radioanalytical chemistry, radiopharmaceutical chemistry, environmental radiochemistry. If these are not done, the educational problems in nuclear chemistry could not be correctly investigated and the remedies could not be correctly determined.

关键词： Nuclear Chemistry Radiochemistry Radiation Chemistry radiopharmaceutical Chemistry Undergraduate Education Universities

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Synthesis and Radiation Dosimetry of [68Ga]-Ga-Lys1, Lys3-DOTA-Bombesin (1,14) Antagonist for PET-Imaging, as a Potential Theragnostic Tracer in Oncology

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Journal of Encapsulation and Adsorption Sciences 2020年第2期10卷 29-41页

作者： Juan C. Manrique-Arias Quetzali Pitalua-Cortes Roberto Pedrero-Piedras Géiser Rodríguez-Mena Tessy López Cristian Cabezas-Ortiz Osvaldo García-Pérez Departamento de Medicina Nuclear Ciclotrón y Radiofarmacia Instituto Nacional de Cancerología México City México Cancer Center Cyclotron Department Doctors Hospital Monterrey México Departamento de Atención a la Salud Universidad Autónoma Metropolitana-Xochimilco México City México

This Bombesin (BBN), a tetradecapeptide analog of human gastrin-releasing peptide (GRP) with a high binding affinity for GRP receptors (GRPR), is over- expressed in early stages of androgen-dependent prostate carcinomas, but not in advanced stages. Therefore, there is a need to develop effective tracers for the accurate and specific detection of this disease. The objective of this study was to evaluate Lys1, Lys3-DOTA-BBN (1,14) analog with the radiolabeled positron emitter [68Ga]-Ga-BBN for receptor imaging with PET, and to determine its biodistribution and radiation dosimetry using whole-body (WB) PET scans in healthy volunteers. The highest uptake was in the pancreas, followed by urinary bladder. The critical organ was pancreas with a mean absorbed dose of 206 ± 0.7, 210 ± 0.7, 120 ± 0.9, 390.23 ± 0.6 μGy/MBq and the effective doses were estimated as 73.2 ± 0.6, 49.8 ± 0.3 μGy/MBq (women and men, respectively).

关键词： Radiation Dosimetry Biodistribution PET Imaging radiopharmaceutical Lys1 Lys3-DOTA-BBN (1 14) Bombesin Analogs

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