A peptide targeted contrast agent specific to fibrin-fibronectin complexes for cancer molecular imaging with MRI

F Ye, EK Jeong, Z Jia, T Yang, D Parker… - Bioconjugate …, 2008 - ACS Publications
F Ye, EK Jeong, Z Jia, T Yang, D Parker, ZR Lu
Bioconjugate Chemistry, 2008ACS Publications
A peptide targeted contrast agent, CLT1-(Gd-DTPA), was synthesized for molecular imaging
of fibronectin− fibrin complexes in tumor tissue with magnetic resonance imaging (MRI). The
T 1 and T 2 relaxivities of CLT1-(Gd-DTPA) were 4.22 and 4.45 mM− 1 s− 1 at 3 T,
respectively. The targeted contrast agent specifically bound to tumor tissue and resulted in
significant tumor contrast enhancement at a dose of 0.1 mmol Gd/kg for at least 60 min in
mice bearing HT-29 human colon carcinoma xenografts as shown in dynamic MR images. In …
A peptide targeted contrast agent, CLT1-(Gd-DTPA), was synthesized for molecular imaging of fibronectin−fibrin complexes in tumor tissue with magnetic resonance imaging (MRI). The T1 and T2 relaxivities of CLT1-(Gd-DTPA) were 4.22 and 4.45 mM−1 s−1 at 3 T, respectively. The targeted contrast agent specifically bound to tumor tissue and resulted in significant tumor contrast enhancement at a dose of 0.1 mmol Gd/kg for at least 60 min in mice bearing HT-29 human colon carcinoma xenografts as shown in dynamic MR images. In contrast, a control nontargeted contrast agent, Gd(DTPA-BMA), was cleared rapidly with little tumor enhancement 60 min postinjection. Tumor enhancement with CLT1-(Gd-DTPA) was significantly reduced after coinjection with a 3-fold excess of free CLT1 peptide. The preliminary study has shown that CLT1-(Gd-DTPA) can specifically bind to the fibrin−fibronectin complexes in tumor tissues, resulting in significant tumor enhancement. The targeted contrast agent has a potential for cancer molecular imaging with MRI.
ACS Publications