ArticleEuropean journal of nuclear medicine and molecular imaging2015
Targeted radionuclide therapy with RAFT-RGD radiolabelled with (90)Y or (177)Lu in a mouse model of αvβ3-expressing tumours.
Article in European journal of nuclear medicine and molecular imaging, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 22 citations in OpenAlex.
- Safety, pharmacokinetics, and dosimetry ofActa pharmaceutica Sinica. B · 2025Article
- Integrin Targeting and Beyond: Enhancing Cancer Treatment with Dual-Targeting RGD (Arginine-Glycine-Aspartate) Strategies.Pharmaceuticals (Basel, Switzerland) · 2024Review
- EGFR- and Integrin αInternational journal of molecular sciences · 2024Review
- Elevating theranostics: The emergence and promise of radiopharmaceutical cell-targeting heterodimers in human cancers.iRadiology · 2024Article
- Multimeric RGD-Based Strategies for Selective Drug Delivery to Tumor Tissues.Pharmaceutics · 2023Review
- Comparison of integrin αEuropean journal of hybrid imaging · 2023Article
- Article
- Non-oncological applications of RGD-based single-photon emission tomography and positron emission tomography agents.European journal of nuclear medicine and molecular imaging · 2021Review
- [Molecular imaging and biology · 2019Article
- Comparison and evaluation of two RGD peptides labelled withOncotarget · 2018Article
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Authors and funding
14 authors at 5 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeThe αvβ3 integrin plays an important role in tumour-induced angiogenesis, tumour proliferation, survival and metastasis. The tetrameric RGD-based peptide, regioselectively addressable functionalized template-(cyclo-[RGDfK])4 (RAFT-RGD), specifically targets the αvβ3 integrin in vitro and in vivo. The aim of this study was to evaluate the therapeutic potential of RAFT-RGD radiolabelled with β(-) emitters in a nude mouse model of αvβ3 integrin-expressing tumours.
methodsBiodistribution and SPECT/CT imaging studies were performed after injection of (90)Y-RAFT-RGD or (177)Lu-RAFT-RGD in nude mice subcutaneously xenografted with αvβ3 integrin-expressing U-87 MG cells. Experimental targeted radionuclide therapy with (90)Y-RAFT-RGD or (177)Lu-RAFT-RGD and (90)Y-RAFT-RAD or (177)Lu-RAFT-RAD (nonspecific controls) was evaluated by intravenous injection of the radionuclides into mice bearing αvβ3 integrin-expressing U-87 MG tumours of different sizes (small or large) or bearing TS/A-pc tumours that do not express αvβ3. Tumour volume doubling time was used to evaluate the efficacy of each treatment.
resultsInjection of 37 MBq of (90)Y-RAFT-RGD into mice with large αvβ3-positive tumours or 37 MBq of (177)Lu-RAFT-RGD into mice with small αvβ3-positive tumours caused significant growth delays compared to mice treated with 37 MBq of (90)Y-RAFT-RAD or 37 MBq of (177)Lu-RAFT-RAD or untreated mice. In contrast, injection of 30 MBq of (90)Y-RAFT-RGD had no effect on the growth of αvβ3-negative tumours.
conclusion(90)Y-RAFT-RGD and (177)Lu-RAFT-RGD are potent agents targeting αvβ3-expressing tumours for internal targeted radiotherapy.
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