Development of a novel ¹⁸F-labeled radiotracer targeting granzyme B for imaging early tumor responses to immunotherapy.

ABSTRACT:

Background

Immunotherapy has emerged as a promising avenue for malignant tumors treatment, but methods to validate its in vivo antitumor activity remain limited. Granzyme B, a key mediator of immune-mediated cell death, is a potential biomarker for assessing immunotherapy efficacy. This study aimed to develop a radiotracer with high sensitivity and specificity for in vivo imaging of granzyme B.

Methods

10 granzyme B targeting inhibitors were synthesized and evaluated to improve binding affinity. The most promising compound was conjugated with 1,4,7-triazacyclononane-N,N',N"-triacetic acid chelator and radiolabeled with Al¹⁸F to generate radiotracer ¹⁸F-G1. Its imaging and pharmacokinetic properties were compared with those of the recently developed radi

SUBMITTER: Xu H 

PROVIDER: S-EPMC12645622 | biostudies-literature | 2025 Nov

REPOSITORIES: biostudies-literature