ArticleEJNMMI radiopharmacy and chemistry2024
Unnatural amino acid substitutions to improve in vivo stability and tumor uptake of
Article in EJNMMI radiopharmacy and chemistry, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.
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Who cites it
5 citing papers in PubMed.
- A Comprehensive Review on Non-natural Amino Acid-based Modifications in Antibacterial Peptides.Mini reviews in medicinal chemistry · 2026Review
- Studies on the impact of modifications at the Gln-Trp site in RM2-based GRPR ligands.EJNMMI research · 2025Article
- NovelPharmaceuticals (Basel, Switzerland) · 2025Article
- Synthesis and Evaluation ofPharmaceuticals (Basel, Switzerland) · 2025Article
- Synthesis and Evaluation of NovelPharmaceuticals (Basel, Switzerland) · 2024Article
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Authors and funding
10 authors.
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Abstract
backgroundOverexpressed in various solid tumors, gastrin-releasing peptide receptor (GRPR) is a promising cancer imaging marker and therapeutic target. Although antagonists are preferable for the development of GRPR-targeted radiopharmaceuticals due to potentially fewer side effects, internalization of agonists may lead to longer tumor retention and better treatment efficacy. In this study, we systematically investigated unnatural amino acid substitutions to improve in vivo stability and tumor uptake of a previously reported GRPR-targeted agonist tracer, [
resultsUnnatural amino acid substitutions were conducted for Gln
conclusionsUnnatural amino acid substitution is an effective strategy to improve in vivo stability and tumor uptake of peptide-based radiopharmaceuticals. With excellent tumor uptake and tumor-to-background contrast, [
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