Precision peptide theranostics: developing N- to C-terminus optimized theranostics targeting cholecystokinin-2 receptor.

ABSTRACT: Peptides are ideal for theranostic development as they afford rapid target accumulation, fast clearance from background tissue, and exhibit good tissue penetration. Previously, we developed a novel series of peptides that presented discreet folding propensity leading to an optimal candidate [⁶⁸Ga]Ga-DOTA-GA1 ([D-Glu]₆-Ala-Tyr-NMeGly-Trp-NMeNle-Asp-Nal-NH₂) with 50 pM binding affinity against cholecystokinin-2 receptors (CCK₂R). However, we were confronted with challenges of unfavorably high renal uptake. Methods: A structure activity relationship study was undertaken of the lead theranostic candidate. Prudent structural modifications were made to the peptide scaffold to evaluate the contributions of specific N-t

SUBMITTER: Rahimi MN 

PROVIDER: S-EPMC10945332 | biostudies-literature | 2024

REPOSITORIES: biostudies-literature