Design, Synthesis, and Biological Evaluation of a Novel [¹⁸F]AlF-H₃RESCA-FAPI Radiotracer Targeting Fibroblast Activation Protein.

ABSTRACT: Background: Cancer-associated fibroblasts (CAFs) are key contributors to the tumorigenic process, with fibroblast activation protein (FAP) overexpressed on CAFs in numerous epithelial carcinomas. FAP represents a promising target for tumor imaging and therapy. We aimed to develop a novel [¹⁸F]AlF-H₃RESCA-FAPI radiotracer with a high labeling yield at room temperature for positron emission tomography (PET) imaging of FAP-expressing tumors. Methods: The H₃RESCA-FAPI chelator was synthesized and radiolabeled with [¹⁸F]AlF. Its radiotracer binding affinity to FAP was assessed using surface plasmon resonance (SPR). Its in vitro stability, plasma clearance, and biodistribution were evaluated. PET imaging was performed in U87MG tumor-beari

SUBMITTER: Zhang Q 

PROVIDER: S-EPMC11859916 | biostudies-literature | 2025 Feb

REPOSITORIES: biostudies-literature