Evaluation of an Integrin α_vβ₃ and Aminopeptidase N Dual-Receptor Targeting Tracer for Breast Cancer Imaging.

ABSTRACT: Integrin α_vβ₃ and aminopeptidase N (APN, also known as CD13) are two important targets involved in the regulation of angiogenesis, tumor proliferation, invasion, and metastasis. In this study, we developed a heterodimeric tracer consisting of arginine-glycine-aspartic (RGD) and asparagine-glycine-arginine (NGR) peptides targeting α_vβ₃ and CD13, respectively, for PET imaging of breast cancer. The NGR peptide was first modified with N₃-NO^tB₂ and then conjugated to BCN-PEG₄-c(RGDyK) via copper-free click chemistry. The resulting precursor was purified and radiolabeled with gallium-68. Small-animal PET/CT imaging and post-imaging biodistribution studies were performed in mice bearing human breast cancer MCF

SUBMITTER: Gai Y 

PROVIDER: S-EPMC7486978 | biostudies-literature | 2020 Jan

REPOSITORIES: biostudies-literature