Development and Evaluation of [<sup>68</sup>Ga]Ga-DOTA-BT1718: A Novel Imaging Agent Targeting MT1-MMP for Malignant Tumor Diagnosis
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 [<sup>68</sup>Ga]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 [<sup>68</sup>Ga]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 (<i>p</i> < 0.05). Preliminary clinical translation results demonstrated that [<sup>68</sup>Ga]Ga-DOTA-BT1718 exhibited significant uptake in patients with pancreatic cancer and glioma, indicating its great potential for clinical application.
Authors
- Lin Qiu
- Yanggang Liu
- Qiang Wan (ORCID: https://orcid.org/0000-0002-8048-9816)
- Shijie Tang (ORCID: https://orcid.org/0000-0002-8022-0374)
- Lin Chen (ORCID: https://orcid.org/0000-0003-0108-4309)
- Yue Chen (ORCID: https://orcid.org/0000-0003-4088-7649)
- Jie Zeng
- Jing Yang (ORCID: https://orcid.org/0000-0002-5778-8578)
- Shuang Yan
- Yuqi Ai
Institutions
- Target (United States) (US)
- Southwest Medical University (CN)
- Affiliated Hospital of Southwest Medical University (CN)
- First Affiliated Hospital of Sichuan Medical University (CN)
- Institute of Nuclear Physics (UZ)
Publication Details
- Journal
- Journal of Medicinal Chemistry
- Published
- 2025-08-25
- DOI
- https://doi.org/10.1021/acs.jmedchem.5c01304
- Citations
- 1
- Primary Topic
- Peptidase Inhibition and Analysis
- Type
- article
- Field-Weighted Citation Impact
- 1.05
Funders
- Department of Science and Technology of Sichuan Province