Radiolabeled R954 Derivatives for Imaging Bradykinin B1 Receptor Expression with Positron Emission Tomography.

摘要: Peptide receptors have emerged as promising targets for diagnosis and therapy. The aberrant overexpression of these in different cancer subtypes allows the adoption new treatment strategies that complement conventional chemotherapies. Bradykinin B1 receptor (B1R) is a G protein-coupled overexpressed many cancers, with limited expression healthy tissues. Previously, we developed 68Ga- 18F-labeled derivatives B1R antagonist peptides B9858 B9958, successfully targeted B1R-expressing tumor xenografts vivo. R954 (Ac-Orn-Arg-Oic-Pro-Gly-αMePhe-Ser-d-2-Nal-Ile), potent antagonist, reportedly more stable than against peptidase degradation. We evaluated two radiolabeled (68Ga-HTK01083 18F-HTK01146) PET imaging. Peptides were synthesized via solid phase strategy. Nonradioactive standards obtain by reacting GaCl3 DOTA-dPEG2-R954 clicking N-propargyl-N,N-dimethylammoniomethyl-trifluoroborate ...