ArticlePharmaceuticals (Basel, Switzerland)2022
A New Class of PSMA-617-Based Hybrid Molecules for Preoperative Imaging and Intraoperative Fluorescence Navigation of Prostate Cancer.
Article in Pharmaceuticals (Basel, Switzerland), 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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The trial behind it
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Who cites it
10 citing papers in PubMed.
- Sarcosine-Based Pharmacokinetic Optimization and Fluorescent Dye Library Evaluation of Dual-Labeled PSMA Inhibitors for Fluorescence-Guided Surgery.Pharmaceuticals (Basel, Switzerland) · 2026Article
- Bimodal Fluorescent Conjugate Based on Prostate-Specific Membrane Antigen Ligands with the Chelating Agent DOTA and SulfoCy5 Dye: Synthesis, Radiolabeling, and Biological Activity.International journal of molecular sciences · 2026Article
- Focusing on Prostate-Specific Membrane Antigen in Precision Diagnosis and Treatment of Prostate Cancer.Biomedicines · 2026Review
- PSMA-targeting hybrid molecule PSMA-914 for preoperative imaging and intraoperative fluorescence-guidance: A first-in-human experience.Theranostics · 2026Article
- Advancements in Intraoperative Imaging for Enhanced Surgical Precision.Recent results in cancer research. Fortschritte der Krebsforschung. Progres dans les recherches sur le cancer · 2026Review
- Fluorescent PSMA-Targeted Radiotheranostic Compounds for Multiscale Imaging.Bioconjugate chemistry · 2025Article
- Prodrugs Targeting Prostate-Specific Membrane Antigen against Prostate Cancer.Journal of medicinal chemistry · 2025Review
- Dual-Labeled Small Peptides in Cancer Imaging and Fluorescence-Guided Surgery: Progress and Future Perspectives.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Effect of Linker Entities on Pharmacokinetics ofACS pharmacology & translational science · 2024Article
- Prostate-specific membrane antigen-targeted surgery in prostate cancer: Accurate identification, real-time diagnosis, and precise resection.Theranostics · 2024Review
Corrections and comments
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Authors and funding
11 authors.
Funding
Abstract
The development of PSMA-targeting low-molecular-weight hybrid molecules aims at advancing preoperative imaging and accurate intraoperative fluorescence guidance for improved diagnosis and therapy of prostate cancer. In hybrid probe design, the major challenge is the introduction of a bulky dye to peptidomimetic core structures without affecting tumor-targeting properties and pharmacokinetic profiles. This study developed a novel class of PSMA-targeting hybrid molecules based on the clinically established theranostic agent PSMA-617. The fluorescent dye-bearing candidates of the strategically designed molecule library were evaluated in in vitro assays based on their PSMA-binding affinity and internalization properties to identify the most favorable hybrid molecule composition for the installation of a bulky dye. The library's best candidate was realized with IRDye800CW providing the lead compound. Glu-urea-Lys-2-Nal-Chx-Lys(IRDye800CW)-DOTA (PSMA-927) was investigated in an in vivo proof-of-concept study, with compelling performance in organ distribution studies, PET/MRI and optical imaging, and with a strong PSMA-specific tumor uptake comparable to that of PSMA-617. This study provides valuable insights about the design of PSMA-targeting low-molecular-weight hybrid molecules, which enable further advances in the field of peptidomimetic hybrid molecule development.
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Registered trials
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