ArticleNuclear medicine and biology2014
Radiolabeling and in vitro evaluation of (67)Ga-NOTA-modular nanotransporter--a potential Auger electron emitting EGFR-targeted radiotherapeutic.
Article in Nuclear medicine and biology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 43 citations in OpenAlex.
- Prospects of Using Protein Engineering for Selective Drug Delivery into a Specific Compartment of Target Cells.Pharmaceutics · 2023Review
- In situ lymphoma imaging in a spontaneous mouse model using the Cerenkov Luminescence of F-18 and Ga-67 isotopes.Scientific reports · 2021Article
- Quantification of EGFR and EGFR-overexpressed cancer cells based on carbon dots@bimetallic CuCo Prussian blue analogue.RSC advances · 2020Article
- Targeted Delivery ofFrontiers in pharmacology · 2020Article
- Stabilization of Modular Nanotransporters by Embedding Hemin in Them in a New Strain with Heme Receptor Expression.Doklady. Biochemistry and biophysics · 2020Article
- Subcellular Targeting of Theranostic Radionuclides.Frontiers in pharmacology · 2018Review
- Targeted Intracellular Delivery of Antibodies: The State of the Art.Frontiers in pharmacology · 2018Review
- Antitumor Activity of Auger Electron EmitterFrontiers in pharmacology · 2018Article
- Modular Nanotransporters for Nuclear-Targeted Delivery of Auger Electron Emitters.Frontiers in pharmacology · 2018Review
- A model for optimizing delivery of targeted radionuclide therapies into resection cavity margins for the treatment of primary brain cancers.Biomedical physics & engineering express · 2017Article
- Antitumor efficacy of Auger electron emitterDoklady. Biochemistry and biophysics · 2017Article
- Preparation, cytotoxicity, and in vivo antitumor efficacy ofInternational journal of nanomedicine · 2017Article
- Development and evaluation of a new modular nanotransporter for drug delivery into nuclei of pathological cells expressing folate receptors.Drug design, development and therapy · 2017Article
- Modular nanotransporters for targeted intracellular delivery of drugs: folate receptors as potential targets.Current pharmaceutical design · 2015Review
- Validation of the plasmid study to relate DNA damaging effects of radionuclides to those from external beam radiotherapy.Nuclear medicine and biologyArticle
- Auger: The future of precision medicine.Nuclear medicine and biologyReview
- In vitro cytotoxicity of Auger electron-emitting [Nuclear medicine and biologyArticle
- Production and radiochemistry of antimony-120m: Efforts toward Auger electron therapy withNuclear medicine and biologyArticle
- Article
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Authors and funding
7 authors at 4 institutions in 2 countries.
Funding
Abstract
introductionModular nanotransporters (MNTs) are vehicles designed to transport drugs from the cell surface via receptor-mediated endocytosis and endosomal escape to nucleus. Hence their conjugation to Auger electron emitters, can cause severe cell killing, by nuclear localization. Herein we evaluate the use of MNT as a platform for targeted radiotherapy with (67)Ga.
methodsEGF was the targeting ligand on the MNT, and NOTA was selected for its radiolabeling with (67)Ga. In the radiolabeling study we dealt with the precipitation of MNT (pI 5.7) at the labeling pH (4.5-5.5) of (67)Ga. Cellular and nuclei uptake of (67)Ga-NOTA-MNT by the A431 cell line was determined. Its specific cytotoxicity was compared to that of (67)Ga-EDTA, (67)Ga-NOTA-BSA and (67)Ga-NOTA-hEGF, in A431 and U87MGWTT, cell lines, by clonogenic assay. Dosimetry studies were also performed.
results(67)Ga-NOTA-MNT was produced with 90% yield and specific activity of 25.6mCi/mg. The in vitro kinetics revealed an increased uptake over 24h. 55% of the internalized radioactivity was detected in the nuclei at 1h. The cytotoxicity of (67)Ga-NOTA-MNT on A431 cell line was 17 and 385-fold higher when compared to non-specific (67)Ga-NOTA-BSA and (67)Ga-EDTA. While its cytotoxic potency was 13 and 72-fold higher when compared to (67)Ga-NOTA-hEGF in the A431 and the U87MGWTT cell lines, respectively, validating its nuclear localization. The absorbed dose, for 63% cell killing, was 8Gy, confirming the high specific index of (67)Ga.
conclusionThese results demonstrate the feasibility of using MNT as a platform for single cell kill targeted radiotherapy by Auger electron emitters.
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