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Development and Evaluation of [<sup>68</sup>Ga]Ga-DOTA-BT1718: A Novel Imaging Agent Targeting MT1-MMP for Malignant Tumor Diagnosis

Jing YangDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25 Taiping Street, Jiangyang District, Luzhou, Sichuan 646000, People’s Republic of ChinaYanggang LiuDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25 Taiping Street, Jiangyang District, Luzhou, Sichuan 646000, People’s Republic of ChinaShijie TangDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25 Taiping Street, Jiangyang District, Luzhou, Sichuan 646000, People’s Republic of ChinaYuqi AiDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25 Taiping Street, Jiangyang District, Luzhou, Sichuan 646000, People’s Republic of ChinaShuang YanDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25 Taiping Street, Jiangyang District, Luzhou, Sichuan 646000, People’s Republic of ChinaJie ZengDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25 Taiping Street, Jiangyang District, Luzhou, Sichuan 646000, People’s Republic of ChinaQiang WanDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25 Taiping Street, Jiangyang District, Luzhou, Sichuan 646000, People’s Republic of ChinaLin ChenDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25 Taiping Street, Jiangyang District, Luzhou, Sichuan 646000, People’s Republic of ChinaYue ChenDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25 Taiping Street, Jiangyang District, Luzhou, Sichuan 646000, People’s Republic of ChinaLin QiuDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25 Taiping Street, Jiangyang District, Luzhou, Sichuan 646000, People’s Republic of China

Journal of Medicinal Chemistryjournal2025en

ABI

Аннотация

Membrane-type 1 matrix metalloproteinase (MT1-MMP) is highly expressed in various malignant tumors. Therefore, evaluating the expression level of MT1-MMP in tumors is crucial. We designed and synthesized [68Ga]Ga-DOTA-BT1718, which targets MT1-MMP, to monitor MT1-MMP expression levels in malignant tumors via positron emission tomography/computed tomography. The results demonstrated that [68Ga]Ga-DOTA-BT1718 exhibited a high uptake in HT1080, Capan2, and U87MG tumors with high MT1-MMP expression. In contrast, it demonstrated low uptake in A549 tumors with low MT1-MMP expression. Notably, this difference was significant (p < 0.05). Preliminary clinical translation results demonstrated that [68Ga]Ga-DOTA-BT1718 exhibited significant uptake in patients with pancreatic cancer and glioma, indicating its great potential for clinical application.

Мавзулар

Peptidase Inhibition and Analysis Protease and Inhibitor Mechanisms Cell Adhesion Molecules Research

Идентификаторлар

DOI: 10.1021/acs.jmedchem.5c01304

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