Work

Preclinical Evaluation of 68Ga-Labeled CSPG4-Targeting Peptides for PET/CT Imaging in Pancreatic and Gastric Carcinoma

Year: 2025

Type: article

Abstract: Chondroitin sulfate proteoglycan 4 (CSPG4) is highly expressed in various solid tumors and promotes tumor progression and migration. Targeting CSPG4 therapy, such as monoclonal antibodies 9.2.27 and CAR-M, has already been in clinical trials. Database analysis further correlated elevated levels of CSPG4 with reduced overall survival in both cancers. Achieving real-time visualization of aberrant CSPG4 expression in various solid tumors remains a critical issue that needs to be addressed. To address this, we pioneered the preparation of three 68Ga-labeled PET probes targeting CSPG4, [68Ga]Ga-DOTA-LS10, [68Ga]Ga-DOTA-SH11, and [68Ga]Ga-DOTA-TH10. In pancreatic (ASPC1) and gastric (MKN45) carcinoma models, [68Ga]Ga-DOTA-TH10 showed prominent tumor uptake (ASPC1:1.63 ± 0.15%ID/g at 60 min), validated by Western blot and immunohistochemistry confirming CSPG4 overexpression. This study conducted the first PET imaging on CSPG4 expression in pancreatic cancer and gastric cancer models using 68Ga-labeled peptides, aiming to provide guidance for clinical real-time monitoring of its expression.

Source: Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.5c02187

Authors: Zerong Wang, Xiaoyu Pan, Ye Li, Fengsheng Zhang, Linjie Bian, Jindian Li

Institutions: Fudan University, Fudan University Shanghai Cancer Center, Institute of Modern Physics, Shanghai Medical College of Fudan University

Language: English

Topic: Radiopharmaceutical Chemistry and Applications

Subfield: Radiology, Nuclear Medicine and Imaging

Field: Medicine

Domain: Health Sciences

SDG: Good health and well-being

Open Access status: hybrid

Estimated APC paid: $4,500