biostudies-literatureZavvar TSAustrian Science Fund FWF278https://www.ebi.ac.uk/biostudies/studies/S-EPMC9959130biostudies-literatureUnknown16(2)Different attempts have been made in the past two decades to develop radiolabeled peptide conjugates with enhanced pharmacokinetic properties in order to improve the application for tumor imaging and peptide receptor radionuclide therapy (PRRT), which targets the cholecystokinin-2 receptor (CCK2R). In this paper, the influence of different side chain and peptide bond modifications has been explored for the minigastrin analog DOTA-DGlu-Ala-Tyr-Gly-Trp-(<i>N</i>-Me)Nle-Asp-1Nal-NH₂ (DOTA-MGS5). Based on this lead structure, five new derivatives were synthesized for radiolabeling with trivalent radiometals. Different chemical and biological properties of the new derivatives were analyzed. Receptor interaction of the peptide derivatives and cell internalization of the radiolabeled pPharmaceuticals (Basel, Switzerland)Effects of Side Chain and Peptide Bond Modifications on the Targeting Properties of Stabilized Minigastrin Analogs.PMC9959130P 27844DOC 110Zavvar TSCastel HKlingler MHormann AARangger CDesrues LSummer DGandolfo Pvon Guggenberg EfalseEffects of Side Chain and Peptide Bond Modifications on the Targeting Properties of Stabilized Minigastrin Analogs.Different attempts have been made in the past two decades to develop radiolabeled peptide conjugates with enhanced pharmacokinetic properties in order to improve the application for tumor imaging and peptide receptor radionuclide therapy (PRRT), which targets the cholecystokinin-2 receptor (CCK2R). In this paper, the influence of different side chain and peptide bond modifications has been explored for the minigastrin analog DOTA-DGlu-Ala-Tyr-Gly-Trp-(<i>N</i>-Me)Nle-Asp-1Nal-NH₂ (DOTA-MGS5). Based on this lead structure, five new derivatives were synthesized for radiolabeling with trivalent radiometals. Different chemical and biological properties of the new derivatives were analyzed. Receptor interaction of the peptide derivatives and cell internalization of the radiolabeled p2023-01-01T00:00:00Z2023 Feb2025-08-12T03:05:02.688Z2025-08-12T03:05:02.688ZS-EPMC99591303705222610.3390/ph16020278