ArticlePharmaceutics2022
Design, Synthesis, and Evaluation of Linker-Optimised PSMA-Targeting Radioligands.
Article in Pharmaceutics, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 27 citations in OpenAlex.
- A Review of Approaches to the Synthesis of DCL-Based Prostate-Specific Membrane Antigen Ligands.International journal of molecular sciences · 2026Review
- Optimizing PSMA-617-based inhibitors through charged linker modifications: Insights into structure-activity relationships.Theranostics · 2026Article
- Kidney-targeted nanoplatforms: Strategies and applications.Theranostics · 2026Review
- A New Labeling Method ofWorld journal of nuclear medicine · 2025Article
- Reduction of Negative Charge in Mercaptoacetyl-Based Chelators Influences the Biodistribution of Prostate-Specific Membrane Antigen-Targeting Pseudopeptides Labeled with Technetium-99m.ACS pharmacology & translational science · 2025Article
- Paving the way for future PSMA inhibitors: insights from comparative preclinical evaluations of structure modifications.EJNMMI radiopharmacy and chemistry · 2025Article
- Clinical evaluation of [RSC advances · 2025Article
- Single-Photon Emission Computer Tomography Imaging of Prostate-Specific Membrane Antigen (PSMA) Expression in Prostate Cancer Patients Using a Novel Peptide-Based Probe [ACS pharmacology & translational science · 2025Article
- Structure-Activity Relationships and Biological Insights into PSMA-617 and Its Derivatives with Modified Lipophilic Linker Regions.ACS omega · 2025Article
- The [18F] F-PSMA Probe: Chemical Perspectives.Current medicinal chemistry · 2025Review
- Value of [Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2024Article
- Synthesis and Preclinical Evaluation of Urea-Based Prostate-Specific Membrane Antigen-Targeted Conjugates Labeled withACS pharmacology & translational science · 2024Article
- Preclinical Evaluation of a Novel High-Affinity Radioligand [International journal of molecular sciences · 2023Article
- Synthesis,International journal of molecular sciences · 2023Article
- Article
- Article
- Prostate specific membrane antigen binding radiopharmaceuticals: Current data and new concepts.Frontiers in medicine · 2022Review
Corrections and comments
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
Abstract
Prostate-specific membrane antigen (PSMA) is overexpressed in the majority of prostate cancer cells and is considered to be an important target for the molecular imaging and therapy of prostate cancer. Herein, we present the design, synthesis, and evaluation of 11 PSMA-binding radioligands with modified linker structures, focusing on the relationship between molecular structure and targeting properties. The linker design was based on 2-naphthyl-L-alanine-tranexamic acid, the linker structure of PSMA-617. X-ray crystal-structure analysis of PSMA and structure-based design were used to generate the linker modifications, suggesting that substitution of tranexamic acid could lead to interactions with Phe546, Trp541, and Arg43 within the binding cavity. After synthesis through SPPS, analogues were labelled with indium-111 and evaluated in vitro for their specific binding, affinity, and cellular retention. Selected compounds were further evaluated in vivo in PSMA-expressing tumour-bearing mice. Based on the results, 2-naphthyl-L-alanine appears to be crucial for good targeting properties, whereas tranexamic acid could be replaced by other substituents. [
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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.