Synthesis and Evaluation of Radiogallium-Labeled Peptide Probes for In Vivo Imaging of Legumain Activity.

ABSTRACT: Legumain (LGMN), a lysosomal cysteine protease, is crucial for tumor progression, invasion, and metastasis, making it a promising target for cancer imaging and therapy. This study developed novel ⁶⁷Ga-labeled 1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA)-conjugated LGMN-cleavable peptide probes ([⁶⁷Ga]Ga-NOTA-LCPs) composed of polyarginine and polyglutamic acid sequences linked by LGMN-cleavable sites for nuclear medicine imaging of LGMN activity. The probes were synthesized via fluorenylmethoxycarbonyl solid-phase peptide synthesis and radiolabeled in high radiochemical yields. In vitro assays with HCT116 cells showed significantly higher uptake of [⁶⁷Ga]Ga-NOTA-LCPs compared to non-cleavable controls, confirming efficient cleavage and cellular uptak

SUBMITTER: Fuchigami T 

PROVIDER: S-EPMC12693633 | biostudies-literature | 2025 Nov

REPOSITORIES: biostudies-literature