ArticleEJNMMI research2023
Investigation of the structure-activity relationship at the N-terminal part of minigastrin analogs.
Article in EJNMMI research, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.
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Who cites it
3 citing papers in PubMed, 8 citations in OpenAlex.
- Advances in radiopharmaceuticals for cancer radiotheranostics: CCK2R targeting as a paradigm for translational innovation.Cancer communications (London, England) · 2025Review
- Development of INER-PP-F11N as the Peptide-Radionuclide Conjugate Drug Against CCK2 Receptor-Overexpressing Tumors.International journal of molecular sciences · 2025Article
- Significant reduction of activity retention in the kidneys via optimized linker sequences in radiohybrid-based minigastrin analogs.EJNMMI research · 2024Article
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
Abstract
backgroundOver the last years, several strategies have been reported to improve the metabolic stability of minigastrin analogs. However, currently applied compounds still reveal limited in vitro and in vivo stability. We thus performed a glycine scan at the N-terminus of DOTA-MGS5 (DOTA-D-Glu-Ala-Tyr-Gly-Trp-(N-Me)Nle-Asp-1-Nal) to systematically analyze the peptide structure. We substituted N-terminal amino acids by simple PEG spacers and investigated in vitro stability in human serum. Furthermore, we evaluated different modifications on its tetrapeptide binding sequence (H-Trp-(N-Me)Nle-Asp-1-Nal-NH
resultsAffinity data of all glycine scan peptides were found to be in a low nanomolar range (4.2-8.5 nM). However, a truncated compound lacking the D-γ-Glu-Ala-Tyr sequence revealed a significant loss in CCK-2R affinity. Substitution of the D-γ-Glu-Ala-Tyr-Gly sequence of DOTA-γ-MGS5 (DOTA- D-γ-Glu-Ala-Tyr-Gly-Trp-(N-Me)Nle-Asp-1-Nal-NH
conclusionWe could demonstrate that a substitution of D-γ-Glu-Ala-Tyr-Gly by PEG spacers simplified the peptide structure of DOTA-MGS5 while high CCK-2R affinity and favorable lipophilicity were maintained. Nevertheless, further optimization with regard to metabolic stability must be carried out for these minigastrin analogs.
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