Synthesis and Evaluation of CREKA-Tris(Gd-DOTA)3 for MR Molecular Imaging of Breast Cancer

Zhuxian Zhou¹, Zhen Ye¹, Xueming Wu¹, Zheng-Rong Lu¹

MRI is a powerful medical imaging modality to display anatomical structures of body, especially useful for the detection and characterization of diseased soft tissues such as solid tumors. Various targeted contrast agents have been prepared for cancer molecular imaging with MRI. However, MRI is not effective for molecular imaging because of its low sensitivity. Most of these agents could not generate sufficient contrast enhancement because of low concentration of biomarkers on cancer cell surface. CREKA is a tumor-homing pentapeptide (Cys-Arg-Glu-Lys-Ala) specifically homes to tumors by binding to fibrin and fibronectin associated plasma protein clots in tumor stroma. Thus, we synthesized and evaluated a new tumor-targeted contrast agent CREKA-Tris(Gd-DOTA)3 for MR molecular imaging of breast cancer