ArticleJournal of medicinal chemistry2016
Structure-Activity Relationship of (18)F-Labeled Phosphoramidate Peptidomimetic Prostate-Specific Membrane Antigen (PSMA)-Targeted Inhibitor Analogues for PET Imaging of Prostate Cancer.
Article in Journal of medicinal chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
What it found
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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.
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Who cites it
20 citing papers in PubMed.
- Prostate-Specific Membrane Antigen (PSMA)-Directed Dendrimer-Camptothecin Conjugate for Targeted Treatment of Prostate Cancer.ACS applied nano materials · 2025Article
- Prodrugs Targeting Prostate-Specific Membrane Antigen against Prostate Cancer.Journal of medicinal chemistry · 2025Review
- PSMA-Targeted 2-Deoxyglucose-Based Dendrimer Nanomedicine for the Treatment of Prostate Cancer.Biomacromolecules · 2024Article
- A PSMA-targeted doxorubicin small-molecule drug conjugate.Bioorganic & medicinal chemistry letters · 2024Article
- PSMA-targeted dendrimer as an efficient anticancer drug delivery vehicle for prostate cancer.Nanoscale · 2024Article
- Repurposing of PSMA-targeted diagnostic and therapeutic agents for the detection and treatment of giant cell tumors of bone.Frontiers in oncology · 2024Article
- Recent Developments in PET and SPECT Radiotracers as Radiopharmaceuticals for Hypoxia Tumors.Pharmaceutics · 2023Review
- Recent Advances ofInternational journal of molecular sciences · 2023Review
- Modular Smart Molecules for PSMA-Targeted Chemotherapy.Molecular cancer therapeutics · 2022Article
- Fluorine-18 Labeled Urea-Based Ligands Targeting Prostate-Specific Membrane Antigen (PSMA) with Increased Tumor and Decreased Renal Uptake.Pharmaceuticals (Basel, Switzerland) · 2022Article
- Metamorphosis of prostate specific membrane antigen (PSMA) inhibitors.Biophysical reviews · 2022Review
- Prostate-Specific Membrane Antigen-Targeted Turn-on Probe for Imaging Cargo Release in Prostate Cancer Cells.Bioconjugate chemistry · 2021Article
- PSMA-Targeting Radiopharmaceuticals for Prostate Cancer Therapy: Recent Developments and Future Perspectives.Cancers · 2021Review
- Molecular Imaging of Prostate Cancer Targeting CD46 Using ImmunoPET.Clinical cancer research : an official journal of the American Association for Cancer Research · 2021Article
- From Plant to Patient: Thapsigargin, a Tool for Understanding Natural Product Chemistry, Total Syntheses, Biosynthesis, Taxonomy, ATPases, Cell Death, and Drug Development.Progress in the chemistry of organic natural products · 2021Article
- Radiolabelled Peptides for Positron Emission Tomography and Endoradiotherapy in Oncology.Pharmaceuticals (Basel, Switzerland) · 2020Review
- Toward the Discovery and Development of PSMA Targeted Inhibitors for Nuclear Medicine Applications.Current radiopharmaceuticals · 2020Review
- Identification, Characterization, and Optimization of Integrin αMolecules (Basel, Switzerland) · 2019Article
- Exploring Metabolism In Vivo Using EndogenousSeminars in nuclear medicine · 2017Review
- Article
Corrections and comments
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Authors and funding
17 authors.
Funding
Abstract
A series of phosphoramidate-based prostate specific membrane antigen (PSMA) inhibitors of increasing lipophilicity were synthesized (4, 5, and 6), and their fluorine-18 analogs were evaluated for use as positron emission tomography (PET) imaging agents for prostate cancer. To gain insight into their modes of binding, they were also cocrystallized with the extracellular domain of PSMA. All analogs exhibited irreversible binding to PSMA with IC50 values ranging from 0.4 to 1.3 nM. In vitro assays showed binding and rapid internalization (80-95%, 2 h) of the radiolabeled ligands in PSMA(+) cells. In vivo distribution demonstrated significant uptake in CWR22Rv1 (PSMA(+)) tumor, with tumor to blood ratios of 25.6:1, 63.6:1, and 69.6:1 for [(18)F]4, [(18)F]5, and [(18)F]6, respectively, at 2 h postinjection. Installation of aminohexanoic acid (AH) linkers in the phosphoramidate scaffold improved their PSMA binding and inhibition and was critical for achieving suitable in vivo imaging properties, positioning [(18)F]5 and [(18)F]6 as favorable candidates for future prostate cancer imaging clinical trials.
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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.