Preparation of F-18 Labeled Peptidic Gelatinase Inhibitor for PET Imaging

The growth, invasion, and metastasis of malignant tumor cells are a complicated process that includes cell division and proliferation, proteolytic degradation of the extracellular matrix, cell migration through basement membranes to reach the circulatory system, and remigration and growth of tumor cells at the metastatic sites. Clinical PET imaging with F-18 FDG has been widely applied for localization and staging of malignancies, however, it provides few information about the capability of distant metastases of the tumors. The initiation of migration and metastasis of tumor cells requires gelatinase proteolytic function of matrix metalloproteinase (MMP) to degrade the basement membrane and extracellular matrix. The overexpression of MMP, particularly MMP2 and MMP9, in many tumors makes that the distribution of MMP may become a valuable biomarker to evaluate the capability of distant metastasis of the tumor cells. A cyclic peptide, CTTHWGFTLC (CTT), was recently reported as an effective MPP gelatinase inhibitor for tumor therapy. The aims of this project are to develop a CTT-based NOTA-peptide conjugate for radiolabeling with F-18 using F-18-AlF approach, and to characterize of this new PET tracer in a MDA-MB-435 human breast tumor grafted mouse model.

Project ID:PC10202-1113
External Project ID:NSC102-2623-E182-002-NU