Novel MRI and fluorescent probes responsive to the Factor XIII transglutaminase activity

作者：Tei Lorenzo; Mazooz Galit; Shellef Yael; Avni Reut; Vandoorne Katrien; Barge Alessandro; Kalchenko Vyacheslav; Dewhirst Mark W; Chaabane Linda; Miragoli Luigi; Longo Dario; Neeman Michal^*; Aime Silvio

来源：Contrast Media and Molecular Imaging, 2010, 5(4): 213-222.

DOI：10.1002/cmmi.392

• molecular imaging, magnetic resonance imaging, near infrared imaging
• transglutaminase activity, responsive contract agents, blood clotting, tumor imaging

Transglutaminases, including factor XIII and tissue transglutaminase, participate in multiple extracellular processes associated with remodeling of the extracellular matrix during wound repair, blood clotting, tumor progression and fibrosis of ischemic injuries. The aim of this work was to evaluate a novel substrate analog for transglutaminase optimized by molecular modeling calculations (DCCP16), which can serve for molecular imaging of transglutaminase activity by magnetic resonance imaging and by near-infrared imaging. Experimental data showed covalent binding of Gd-DCCP16 and DCCP16-IRIS Blue to human clots, to basement membrane components and to casein in purified systems as well as in three-dimensional multicellular spheroids. In vivo, DCCP16 showed enhancement with a prolonged retention in clots and tumors, demonstrating the ability to detect both factor XIII and tissue transglutaminase mediated covalent binding of the contrast material.

• 出版日期2010-8