Development of a homotrimeric PSMA radioligand based on the NOTI chelating platform
Trimerization of the Glu-CO-Lys binding motif for conjugate 9 resulted in a ~ threefold higher binding affinity and cellular uptake as well as in an altered biodistribution profile compared to the control [<sup>68</sup>Ga]Ga-PSMA-11 due to its intrinsic high binding to serum proteins. To fully elucidate its biodistribution, future studies in combination with long-lived radionuclides, such as <sup>64</sup>Cu, are warranted. Its prolonged biological half-life and favorable tumor-to-kidney ratio make this homotrimeric conjugate also a potential candidate for future radiotherapeutic applications in combination with therapeutic radionuclides such as <sup>67</sup>Cu.
Authors
- Caroline Burgard (ORCID: https://orcid.org/0000-0003-1522-8860)
- Sebastian Martin (ORCID: https://orcid.org/0000-0002-7875-3737)
- Samer Ezziddin (ORCID: https://orcid.org/0000-0003-4110-3375)
- Stephan Maus (ORCID: https://orcid.org/0000-0003-1679-8080)
- Tobias Stemler
- Mark Bartholomä (ORCID: https://orcid.org/0000-0002-0361-2833)
- Andrea Schaefer-Schuler (ORCID: https://orcid.org/0000-0002-2439-5786)
- Florian Rosar (ORCID: https://orcid.org/0000-0002-2985-4099)
- Moritz-Valentin Schreck
Institutions
- Saarland University (DE)
- University of Lausanne (CH)
Publication Details
- Journal
- EJNMMI Radiopharmacy and Chemistry
- Published
- 2024-12-11
- DOI
- https://doi.org/10.1186/s41181-024-00314-7
- Citations
- 4
- Primary Topic
- Peptidase Inhibition and Analysis
- Type
- article
- Field-Weighted Citation Impact
- 1.13
Funders
- Deutsche Forschungsgemeinschaft
- Dr. Rolf M. Schwiete Stiftung