Synthesis and Preclinical Evaluation of [⁶⁸Ga]SP94 for Micro-PET Imaging of GRP78 Expression in Hepatocellular Carcinoma.

ABSTRACT: Glucose-regulated protein 78 (GRP78) is overexpressed in a wide variety of solid tumors, serving as a well-characterized target for tumor imaging or therapy. In this work, we developed a GRP78-responsive radiotracer (DOTA-⁶⁸Ga)-Gly-Gly-Gly-Ser-Phe-Ser-Ile-Ile-His-Thr-Pro-Ile-Leu-Pro-Leu-Gly-Gly-Cys ([⁶⁸Ga]SP94) for hepatocellular carcinoma (HCC) micro-PET imaging. DOTA-SP94 was synthesized by solid phase synthesis and then radiolabeled with ⁶⁸GaCl₃ with >99% radiochemical purity. The expression levels of GRP78 in HepG₂ cells were confirmed by Western blotting. In vitro and in vivo study of [⁶⁸Ga]SP94 showed high stability and high uptake in GRP78-overexpressing HepG₂ cells and tumor, fast clearance, and low nontar

SUBMITTER: Xu Y 

PROVIDER: S-EPMC8521616 | biostudies-literature | 2021 Oct

REPOSITORIES: biostudies-literature