Targeting of MMP2 activity in malignant tumors with a Ga-68-labeled gelatinase inhibitor cyclic peptide

摘要

Introduction: Elevated levels of gelatinases (matrix metalloproteinases 2/9, i.e., MMP2 and MMP9) are associated with tumor progression, invasion and metastasis, so these enzymes are potential targets for tumor imaging. The peptide c(KAHWGFTLD)NH2 (herein, C6) is a selective gelatinase inhibitor. Cy5.5-C6 has been visualized in many tumor models in vivo. However, the sensitivity and penetrance of optical imaging are poor. It is well known that positron emission tomography (PET) has a high detection sensitivity and Gallium-68 (Ga-68) is an optimal PET radioisotope. Thus, in the present study, we developed a novel ligand, Ga-68-NOTA-C6, to image MMP2 activity in tumors.