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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 YangNuclear Medicine and Molecular Imaging Key Laboratory of Sichuan ProvinceYanggang LiuSouthwest Medical UniversityShijie TangDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25 Taiping Street, Jiangyang District, Luzhou, Sichuan 646000, People’s Republic of ChinaYuqi AiInstitute of Nuclear MedicineShuang YanSouthwest Medical UniversityJie ZengLaboratory for Targeted Radiopharmaceuticals CreationQiang WanInstitute of Nuclear MedicineLin ChenInstitute of Nuclear MedicineYue ChenNuclear Medicine and Molecular Imaging Key Laboratory of Sichuan ProvinceLin QiuSouthwest Medical University

Journal of Medicinal Chemistryjournal2025en

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ABI

Annotatsiya

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.

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Mavzular

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

Identifikatorlar

DOI: 10.1021/acs.jmedchem.5c01304

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