ArticleEJNMMI research2018
Synthesis and in vitro and in vivo evaluation of urea-based PSMA inhibitors with increased lipophilicity.
Article in EJNMMI research, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 35 citations in OpenAlex.
- [European journal of nuclear medicine and molecular imaging · 2026Article
- Enhancing Cytosolic Internalization of [International journal of molecular sciences · 2025Article
- Predicting the effect of different folate doses on [EJNMMI research · 2023Article
- Preclinical Evaluation of a PSMA-Targeting Homodimer with an Optimized Linker for Imaging of Prostate Cancer.Molecules (Basel, Switzerland) · 2023Article
- [Molecules (Basel, Switzerland) · 2022Article
- Synthesis and Preclinical Evaluation ofJournal of nuclear medicine : official publication, Society of Nuclear Medicine · 2022Article
- [Nan fang yi ke da xue xue bao = Journal of Southern Medical University · 2022Article
- Metamorphosis of prostate specific membrane antigen (PSMA) inhibitors.Biophysical reviews · 2022Review
- Strain-Promoted Azide-Alkyne Cycloaddition-Based PSMA-Targeting Ligands for Multimodal Intraoperative Tumor Detection of Prostate Cancer.Bioconjugate chemistry · 2022Article
- Interactions of Urea-Based Inhibitors with Prostate-Specific Membrane Antigen for Boron Neutron Capture Therapy.ACS omega · 2021Article
- Targeted delivery of cytotoxic proteins to prostate cancer via conjugation to small molecule urea-based PSMA inhibitors.Scientific reports · 2021Article
- Evaluation of radioiodinated protein conjugates and their potential metabolites containing lysine-urea-glutamate (LuG), PEG and closo-decaborate(2-) as models for targeting astatine-211 to metastatic prostate cancer.Nuclear medicine and biology · 2021Article
- Design, Synthesis, Computational, and Preclinical Evaluation ofMolecules (Basel, Switzerland) · 2020Article
- Hybrid Tracers Based on Cyanine Backbones Targeting Prostate-Specific Membrane Antigen: Tuning Pharmacokinetic Properties and Exploring Dye-Protein Interaction.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2020Article
- Development of an Albumin-Based PSMA Probe With Prolonged Half-Life.Frontiers in molecular biosciences · 2020Article
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
Abstract
backgroundSeveral radiolabeled prostate-specific membrane antigen (PSMA) inhibitors based on the lysine-urea-glutamate (KuE) motif as the pharmacophore proved to be suitable tools for PET/SPECT imaging of the PSMA expression in prostate cancer patients. PSMA I&T, a theranostic tracer developed in our group, was optimized through alteration of the peptidic structure in order to increase the affinity to PSMA and internalization in PSMA-expressing tumor cells. However, further structural modifications held promise to improve the pharmacokinetic profile.
resultsAmong the investigated compounds 1-9, the PSMA inhibitors 5 and 6 showed the highest PSMA affinity (lowest IC
conclusionsHigher lipophilicity of the novel PSMA ligands 10 and 11 proved to be beneficial in terms of affinity and internalization and resulted in higher tumor uptake compared to the parent compound. Additional combination with para-iodo-phenylalanine in the spacer of ligand 11 elevated the plasma protein binding and enabled sustained tumor accumulation over 24 h, increasing the tumor uptake almost fourfold compared to
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