ArticleEuropean journal of nuclear medicine and molecular imaging2011
Renal uptake of different radiolabelled peptides is mediated by megalin: SPECT and biodistribution studies in megalin-deficient mice.
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 69 papers.
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69 citing papers in PubMed, 137 citations in OpenAlex.
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- Radiolabeled 15-mer peptide internalization is mediated by megalin (LRP2 receptor) in a CRISPR/Cas9-based LRP2 knockout human kidney cell model.EJNMMI radiopharmacy and chemistry · 2024Article
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- Amide-to-Triazole Switch in Somatostatin-14-Based Radioligands: Impact on Receptor Affinity and In Vivo Stability.Pharmaceutics · 2024Article
- Somatostatin Receptor Subtype-2 Targeting System for Specific Delivery of Temozolomide.Journal of medicinal chemistry · 2024Article
- Towards the Magic Radioactive Bullet: Improving Targeted Radionuclide Therapy by Reducing the Renal Retention of Radioligands.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Navigating the landscape of PD-1/PD-L1 imaging tracers: from challenges to opportunities.Frontiers in medicine · 2024Review
- Targeted radiopharmaceuticals: an underexplored strategy for ovarian cancer.Theranostics · 2024Review
- Reducing kidney uptake of radiolabelled exendin-4 using variants of the renally cleavable linker MVK.EJNMMI radiopharmacy and chemistry · 2023Article
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- New Radiolabeled Exendin Analogues Show Reduced Renal Retention.Molecular pharmaceutics · 2023Article
9 more citing papers are in PubMed but not listed here.
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9 authors at 3 institutions in 1 country.
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No grant is acknowledged in the PubMed record.
Abstract
purposeRadiolabelled peptides used for peptide receptor radionuclide therapy are excreted mainly via the kidneys and are partly reabsorbed and retained in the proximal tubular cells. The resulting high renal radiation dose can cause nephrotoxicity, limiting the maximum activity dose and the effectiveness of peptide receptor radionuclide therapy. The mechanisms of kidney reabsorption of these peptides are incompletely understood, but the scavenger receptor megalin has been shown to play a role in the reabsorption of (111)In-octreotide. In this study, the role of megalin in the renal reabsorption of various relevant radiolabelled peptides was investigated.
methodsGroups of kidney-specific megalin-deficient mice and wild-type mice were injected with (111)In-labelled somatostatin, exendin, neurotensin or minigastrin analogues. Single photon emission computed tomographic (SPECT) images of the kidneys were acquired and analysed quantitatively, or the animals were killed 3 h after injection and the activity concentration in the kidneys was measured.
resultsMegalin-deficient mice showed significantly lower uptake of all studied radiolabelled peptides in the kidneys, ranging from 22% ((111)In-octreotide) to 65% ((111)In-exendin) of uptake in wild-type kidneys. Quantitative analysis of renal uptake by SPECT and ex vivo measurements showed a very good correlation.
conclusionMegalin is involved in the renal reabsorption of radiolabelled octreotide, octreotate, exendin, neurotensin and minigastrin. This knowledge may help in the design of strategies to reduce this reabsorption and the resulting nephrotoxicity in peptide receptor radionuclide therapy, enabling more effective therapy. Small-animal SPECT is an accurate tool, allowing in vivo quantification of renal uptake and serial measurements in individual mice.
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