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Investigation of the structure-activity relationship at the N-terminal part of minigastrin analogs.

Nadine HolzleitnerThomas GüntherAmira Daoud-GadiehConstantin LapaHans-Jürgen Wester
Published in: EJNMMI research (2023)
We 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.
Keyphrases
  • structure activity relationship
  • molecular docking
  • pet ct
  • drug delivery
  • pet imaging
  • molecular dynamics simulations