Does the radioligand [123I]I-HO-CGS 27023A allow for specific in vivo scintigraphic imaging of MMP activity in vascular lesions in apolipoprotein E-deficient mice?
In vivo scintigraphic imaging of matrix metalloproteinase activity is feasible using a radiolabeled MMP inhibitor in a mouse model of atherosclerosis.
BACKGROUND: Matrix metalloproteinases (MMPs) are enzymes involved in the proteolytic degradation of extracellular matrix. They play an important role in several disease processes, such as inflammation, cancer, and atherosclerosis. METHODS AND RESULTS: In this study, we have used the broad-spectrum MMP inhibitor CGS 27023A to develop the radioligand 123II-HO-CGS 27023A for in vivo imaging of MMP activity. Using this radioligand, we were able to specifically image MMP activity by scintigraphy in vivo in the MMP-rich vascular lesions that develop after carotid artery ligation and cholesterol-rich diet in apolipoprotein E-deficient mice. These results were confirmed by gamma counting of lesional tissue (counts per minute per milligram). CONCLUSIONS: Imaging of MMP activity in vivo is feasible using radiolabeled MMP inhibitors. Additional studies are needed to test the potential of this approach as a novel noninvasive clinical diagnostic tool for the management of human MMP-related diseases.
Schäfers et al. (Tue,) studied this question.