ArticleNuclear medicine and biology
Brush border enzyme-cleavable linkers: Evaluation for reducing renal uptake of radiolabeled prostate-specific membrane antigen inhibitors.
Article in Nuclear medicine and biology. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
18 citing papers in PubMed, 31 citations in OpenAlex.
- Linker Chemistry in Radiopharmaceutical Design.Bioconjugate chemistry · 2026Review
- Sex-dependent PRRT toxicity in patients with metastatic somatostatin receptor-avid neuroendocrine tumors treated withHormones (Athens, Greece) · 2026Article
- Biodistribution-Driven Discovery Identifies a Glycosidase-Cleavable Linker to Reprogram Radiotheranostics.bioRxiv : the preprint server for biology · 2025Article
- Trends in nanobody radiotheranostics.European journal of nuclear medicine and molecular imaging · 2025Review
- EphA2-targeted alpha-particle theranostics for enhancing PDAC treatment.Theranostics · 2025Article
- Astatine-211 and actinium-225: two promising nuclides in targeted alpha therapy.Acta biochimica et biophysica Sinica · 2024Review
- New tactics in the design of theranostic radiotracers.Npj imaging · 2024Review
- Towards the Magic Radioactive Bullet: Improving Targeted Radionuclide Therapy by Reducing the Renal Retention of Radioligands.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Reducing kidney uptake of radiolabelled exendin-4 using variants of the renally cleavable linker MVK.EJNMMI radiopharmacy and chemistry · 2023Article
- New Long-Acting [Journal of medicinal chemistry · 2023Article
- Preclinical Evaluation of 225Ac-Labeled Single-Domain Antibody for the Treatment of HER2pos Cancer.Molecular cancer therapeutics · 2022Article
- A Preclinical Study of anPharmaceuticals (Basel, Switzerland) · 2022Article
- Application of Cleavable Linkers to Improve Therapeutic Index of Radioligand Therapies.Molecules (Basel, Switzerland) · 2022Review
- Reducing the Kidney Uptake of High Contrast CXCR4 PET Imaging Agents via Linker Modifications.Pharmaceutics · 2022Article
- Introduction to Antibody-Drug Conjugates.Antibodies (Basel, Switzerland) · 2021Review
- PSMA-Targeting Radiopharmaceuticals for Prostate Cancer Therapy: Recent Developments and Future Perspectives.Cancers · 2021Review
- Evaluation of Met-Val-Lys as a Renal Brush Border Enzyme-Cleavable Linker to Reduce Kidney Uptake ofMolecules (Basel, Switzerland) · 2020Article
- Enhancing the therapeutic index of [Nuclear medicine and biologyArticle
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
7 authors at 3 institutions in 1 country.
Funding
Abstract
introductionRadiolabeled, low-molecular-weight prostate-specific membrane antigen (PSMA) inhibitors based on the Glu-ureido pharmacophore show promise for the detection and treatment of castration-resistant prostate cancer; however, high renal retention of activity, related in part to overexpression of PSMA in kidneys can be problematic. The goal of the current study was to investigate the use of brush border enzyme-cleavable linkers as a strategy for reducing kidney activity levels from radiolabeled PSMA inhibitors.
methodsPSMA-769 (6), a derivative of the prototypical PSMA inhibitor (((S)‑1‑carboxy‑5‑(4‑iodobenzamido)pentyl)carbamoyl)glutamate (12) modified to contain a Gly-Tyr linker, and its protected tin precursor (11) were synthesized starting from the basic pharmacophore molecule Lys-urea-Glu. An analogue of 6 containing d‑tyrosine in lieu of l‑tyrosine (PSMA-769-d-tyrosine) and the corresponding tin precursor (d-11) also were synthesized. Both radioiodinated and
resultsCompounds [
conclusionUse of this brush border enzyme-cleavable linker reduced kidney uptake and resulted in improved tumor:kidney uptake ratios. Although further structural improvements are needed, this linker approach might be useful as a component in strategies for reducing renal uptake of radiolabeled PSMA inhibitors.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.