Preparation and Characterization of Radiolabeled Peptidic Gelatinase Inhibitor

  • Wey, Shiaw-Pyng (PI)
  • Lin, Kun-Ju (CoPI)

Project: National Science and Technology CouncilNational Science and Technology Council Academic Grants

Project Details


Tumor growth, invasion, and metastasis are a complex process that includes cell division and proliferation, proteolytic digestion of the extracellular matrix, cell migration through basement membranes to reach the circulatory system, and remigration and growth of tumors at the metastatic sites. F-18 FDG PET has been widely used for clinical localization of tumor lesions, however, it provides few information about the capability of distant metastases of the malignancies. The migration and metastasis of tumor cells require gelatinase proteolytic function of MMP to degrade the basement membrane and extracellular matrix. The expression of MMP in many tumors is significant higher than normal. Therefore, 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 reported as an effective MPP gelatinase inhibitor for tumor therapy. The aims of this project are to develop a CTT-based DOTA-peptide conjugate labeled with Ga-68 for PET imaging, and to evaluate the characterization of this new tracer in tumor-bearing animal models. In year 2010, we have synthesized DOTA-CTT peptide conjugate and verified its quality with HPLC and mass spectroscopy. Ga-67-labeled DOTA-CTT peptide conjugate has been achieved with high radiochemical purity. In this project, the mouse models respectively bearing MDA-MB-231 and MDA-MB-435S cells, two human breast tumor cell lines expressing different levels of MMP, will be established. The in-vivo distribution of Ga-67/Ga-68-DOTA-CTT will be evaluated in both animal models by dissection and animal imaging.

Project IDs

Project ID:PB10101-3747
External Project ID:NSC101-2623-E182-001-NU
Effective start/end date01/01/1231/12/12


  • radiogallium-labeld tracer
  • peptidic gelatinase inhibitor
  • tumor imaging agent


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