机构：[1]Department of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25 Taiping Street, Jiangyang District, Luzhou, Sichuan 646000, People's Republic of China.[2]Nuclear Medicine and Molecular Imaging Key Laboratory of Sichuan Province, Luzhou Sichuan 646000, People's Republic of China.[3]Laboratory for Targeted Radiopharmaceuticals Creation, Luzhou, Sichuan 646000, People's Republic of China.[4]Institute of Nuclear Medicine, Southwest Medical University, Luzhou, Sichuan 646000, People's Republic of China.
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.
基金：
the Science and
Technology Department of Sichuan Province (Project No.
2023YFS0091) and the scientific and technological project of
the Health Commission of Sichuan Province (Project No.
24QNMP093) and Sichuan Provincial Science and Technology
Plan Joint Innovation Special Project (Project No.
2022YFS0608−B2.)
语种：
外文
PubmedID：
中科院(CAS)分区：
出版当年[2025]版：
大类|1 区医学
小类|1 区药物化学
最新[2025]版：
大类|1 区医学
小类|1 区药物化学
第一作者：
第一作者机构：[1]Department of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25 Taiping Street, Jiangyang District, Luzhou, Sichuan 646000, People's Republic of China.[2]Nuclear Medicine and Molecular Imaging Key Laboratory of Sichuan Province, Luzhou Sichuan 646000, People's Republic of China.[3]Laboratory for Targeted Radiopharmaceuticals Creation, Luzhou, Sichuan 646000, People's Republic of China.[4]Institute of Nuclear Medicine, Southwest Medical University, Luzhou, Sichuan 646000, People's Republic of China.
共同第一作者：
通讯作者：
通讯机构：[1]Department of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25 Taiping Street, Jiangyang District, Luzhou, Sichuan 646000, People's Republic of China.[2]Nuclear Medicine and Molecular Imaging Key Laboratory of Sichuan Province, Luzhou Sichuan 646000, People's Republic of China.[3]Laboratory for Targeted Radiopharmaceuticals Creation, Luzhou, Sichuan 646000, People's Republic of China.[4]Institute of Nuclear Medicine, Southwest Medical University, Luzhou, Sichuan 646000, People's Republic of China.
推荐引用方式(GB/T 7714)：
Yang Jing,Liu Yanggang,Tang Shijie,et al.Development and Evaluation of [68Ga]Ga-DOTA-BT1718: A Novel Imaging Agent Targeting MT1-MMP for Malignant Tumor Diagnosis[J].Journal Of Medicinal Chemistry.2025,68(17):18519-18529.doi:10.1021/acs.jmedchem.5c01304.
APA：
Yang Jing,Liu Yanggang,Tang Shijie,Ai Yiheng,Yan Shuang...&Qiu Lin.(2025).Development and Evaluation of [68Ga]Ga-DOTA-BT1718: A Novel Imaging Agent Targeting MT1-MMP for Malignant Tumor Diagnosis.Journal Of Medicinal Chemistry,68,(17)
MLA：
Yang Jing,et al."Development and Evaluation of [68Ga]Ga-DOTA-BT1718: A Novel Imaging Agent Targeting MT1-MMP for Malignant Tumor Diagnosis".Journal Of Medicinal Chemistry 68..17(2025):18519-18529
医学