ArticleEuropean journal of nuclear medicine and molecular imaging2011
Preliminary evaluation of (177)Lu-labeled knottin peptides for integrin receptor-targeted radionuclide therapy.
Article in European journal of nuclear medicine and molecular imaging, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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12 citing papers in PubMed.
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- Cyclotides: Overview and Biotechnological Applications.Chembiochem : a European journal of chemical biology · 2017Review
- Radiolabeled nanobodies as theranostic tools in targeted radionuclide therapy of cancer.Expert opinion on drug delivery · 2014Review
- A radiofluorinated divalent cystine knot peptide for tumor PET imaging.Molecular pharmaceutics · 2014Article
- 99mTc-labeled cystine knot peptide targeting integrin αvβ6 for tumor SPECT imaging.Molecular pharmaceutics · 2014Article
- Article
- PET of EGFR expression with an 18F-labeled affibody molecule.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2012Article
- 111In-labeled cystine-knot peptides based on the Agouti-related protein for targeting tumor angiogenesis.Journal of biomedicine & biotechnology · 2012Article
- Stroma targeting nuclear imaging and radiopharmaceuticals.International journal of molecular imaging · 2012Article
- Diagnosis and therapy are walking together on radiopeptides' avenue.European journal of nuclear medicine and molecular imaging · 2011Article
- Integrin targeted delivery of radiotherapeutics.Theranostics · 2011Article
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Abstract
purposeCystine knot peptides (knottins) 2.5D and 2.5F were recently engineered to bind integrin receptors with high affinity and specificity. These receptors are overexpressed on the surface of a variety of malignant human tumor cells and tumor neovasculature. In this study, 2.5D and 2.5F were labeled with a therapeutic radionuclide, (177)Lu, and the resulting radiopeptides were then evaluated as potential radiotherapeutic agents in a murine model of human glioma xenografts.
methodsKnottins 2.5D and 2.5F were synthesized using solid phase peptide synthesis, folded in vitro, and site-specifically coupled with 1,4,7,10-tetraazacyclododecane-N,N',N'',N'''-tetraacetic acid (DOTA) at their N terminus for (177)Lu radiolabeling. The stability of the radiopeptides (177)Lu-DOTA-2.5D and (177)Lu-DOTA-2.5F was tested in both phosphate-buffered saline (PBS) and mouse serum. Cell uptake assays of the radiolabeled peptides were performed in U87MG integrin-expressing human glioma cells. The biodistribution studies of both (177)Lu-DOTA-2.5D and (177)Lu-DOTA-2.5F were examined in U87MG tumor-bearing athymic nu/nu mice. Radiation absorbed doses for the major tissues of a human adult male were calculated based on the mouse biodistribution results.
resultsDOTA-2.5D and DOTA-2.5F were labeled with (177)Lu at over 55% efficiency. High radiochemical purity for both radiocomplexes (> 95%) could be achieved after high performance liquid chromatography (HPLC) purification. Both radiopeptides were stable in PBS and mouse serum. Compared to (177)Lu-DOTA-2.5D (0.39 and 0.26 %ID/g at 2 and 24 h, respectively), (177)Lu-DOTA-2.5F showed much higher tumor uptake (2.16 and 0.78 %ID/g at 2 and 24 h, respectively). It also displayed higher tumor to blood ratios than that of (177)Lu-DOTA-2.5D (31.8 vs 18.7 at 24 h and 52.6 vs 20.6 at 72 h). Calculation of radiodosimetry for (177)Lu-DOTA-2.5D and (177)Lu-DOTA-2.5F suggested that tumor and kidney were tissues with the highest radiation absorbed doses. Moreover, (177)Lu-DOTA-2.5F had a higher tumor to kidney radiation absorbed dose ratio than that of (177)Lu-DOTA-2.5D.
conclusionCystine knot peptides can be successfully radiolabeled with (177)Lu for potential therapeutic applications. Knottin 2.5F labeled with (177)Lu exhibits favorable distribution in murine U87MG xenograft model; thus, it is a promising agent for radionuclide therapy of integrin-positive tumors.
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