Evaluation of the Gly-Phe-Lys Linker to Reduce the Renal Radioactivity of a [⁶⁴Cu]Cu-Labeled Multimeric cRGD Peptide.

ABSTRACT: Radiometal-labeled peptide-based radiopharmaceuticals (RLPB-radiopharmaceuticals) are promising for cancer imaging and targeted radiotherapy; however, their effectiveness is often compromised by the high retention of nonspecific radioactivity in the kidneys due to renal excretion pathways. Current strategies to address this issue have limitations, highlighting the need for innovative approaches to improve targeting specificity and therapeutic efficacy. We aimed to evaluate the applicability of the Gly-Phe-Lys (GFK) tripeptide, a renal brush border (RBB) enzyme-cleavable linkage, to reduce renal radioactivity in RLPB-radiopharmaceuticals using the integrin-targeting radiopeptide [⁶⁴Cu]Cu-cyclam-RAFT-c(-RGDfK-)₄ ([⁶⁴Cu]Cu-cyclam-RaftRGD). We designed and synt

SUBMITTER: Jin ZH 

PROVIDER: S-EPMC11799997 | biostudies-literature | 2025 Feb

REPOSITORIES: biostudies-literature