In Vivo Radioimaging of Bradykinin Receptor B1, a Widely Overexpressed Molecule in Human Cancer

摘要: The bradykinin receptor B1R is overexpressed in many human cancers where it might be used as a general target for cancer imaging. In this study, we evaluated the feasibility of using radiolabeled kallidin derivatives to visualize expression preclinical model B1R-positive tumors. Three synthetic were vitro and vivo binding their ability tumors by PET. Enalaprilat phosphoramidon evaluate impact peptidases on tumor visualization. While found that peptides based native sequence ineffective at visualizing tumors, peptidase inhibition with greatly enhanced visualization . Two stabilized incorporating unnatural amino acids ( 68 Ga-SH01078 Ga-P03034) maintained receptor-binding affinities effective, allowing excellent visualization, minimal accumulation normal tissues, rapid renal clearance. Tumor uptake was blocked presence excess competitor, confirming specificity mediated. Our results offer proof concept noninvasive detection PET imaging tool cancers. Cancer Res; 75(2); 387–93. ©2014 AACR.