Studies on the impact of modifications at the Gln-Trp site in RM2-based GRPR ligands
Substitution of the Gln-Trp site in RM2 by artificial amino acids had a distinct impact on overall pharmacokinetics. While Hse (instead of Gln) and Bta (instead of Trp) led to a decreased, α-Me-Trp (instead of Trp) led to an increased in vivo stability, which resulted in improved pharmacokinetics over time in case of the latter. However, at 1 h post-injection both [<sup>68</sup>Ga]Ga-[Hse<sup>7</sup>]RM2 and [<sup>68</sup>Ga]Ga-[Bta<sup>8</sup>]RM2 displayed slightly higher tumor-to-pancreas and tumor-to-intestine ratios, rendering homoserine and β-(3-benzothienyl)alanine potential options for the modification of GRPR ligands with regard to imaging properties.
Authors
- Thomas Günther
- Sebastian Fischer (ORCID: https://orcid.org/0009-0000-8061-7091)
- Roswitha Beck
- Hans‐Jürgen Wester (ORCID: https://orcid.org/0000-0002-6655-4183)
- Lena Koller
- Sandra Dominelli
Institutions
- Stanford Medicine (US)
- Technical University of Munich (DE)
- Stanford University (US)
Publication Details
- Journal
- EJNMMI Research
- Published
- 2025-09-01
- DOI
- https://doi.org/10.1186/s13550-025-01241-7
- Citations
- 1
- Primary Topic
- Radiopharmaceutical Chemistry and Applications
- Type
- article
- Field-Weighted Citation Impact
- 1.36
Funders
- Deutsche Forschungsgemeinschaft
- Technische Universität München