Molecular Evolution of Multivalent OncoFAP Derivatives with Enhanced Tumor Uptake and Prolonged Tumor Retention
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View abstract on PubMed
Summary
This summary is machine-generated.Researchers developed novel compact OncoFAP multimers with enhanced affinity for fibroblast activation protein (FAP). These new ligands demonstrate increased tumor retention for improved cancer radiotherapy efficacy.
Area Of Science
- Oncology
- Radiochemistry
- Molecular Imaging
Background
- Fibroblast activation protein (FAP) is a key biomarker in many epithelial cancers.
- Current FAP-targeted radioligands have short tumor half-lives, limiting therapeutic potential.
- Prolonged tumor retention is crucial for effective FAP-targeted radioligand therapeutics.
Purpose Of The Study
- To develop novel compact OncoFAP multimers with improved FAP affinity.
- To enhance tumor-residence time for therapeutic applications.
- To evaluate the in vitro and in vivo performance of new FAP ligands.
Main Methods
- Design and synthesis of compact OncoFAP multimers.
- In silico analysis of multimer-FAP interactions.
- In vitro affinity assays (IC50 determination).
- In vivo biodistribution studies in tumor-bearing mice.
Main Results
- Developed multimers with low picomolar IC50s, indicating high FAP affinity.
- In silico analysis revealed favorable binding pocket interactions.
- TriOncoFAP-DOTAGA showed excellent in vitro profile and superior in vivo biodistribution.
Conclusions
- Compact OncoFAP multimers offer enhanced FAP affinity and improved tumor retention.
- TriOncoFAP-DOTAGA is a promising candidate for FAP-targeted cancer therapy.
- These findings support the development of next-generation FAP-targeted radiotherapeutics.
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