期刊
JOURNAL OF NUCLEAR MEDICINE
卷 52, 期 6, 页码 986-993出版社
SOC NUCLEAR MEDICINE INC
DOI: 10.2967/jnumed.110.085613
关键词
PET; tumor microenvironment; chemokine; stem cells; molecular imaging; colon cancer; brain cancer; metastasis
资金
- American Brain Tumor Association
- Maryland Stem Cell Research Fund
- Elsa U. Pardee Foundation
- National Cancer Institute [U24 CA92871]
The chemokine receptor 4 (CXCR4) is overexpressed in several cancers and metastases and as such presents an enticing target for molecular imaging of metastases and metastatic potential of the primary tumor. CXCR4-based imaging agents could also be useful for diagnosis, staging, and therapeutic monitoring. Here we evaluated a positron-emitting monocyclam analog, Cu-64-{N-[1,4,8,11-tetraazacyclotetradecanyl-1,4-phenylenebis(methylene)]-2-(aminomethyl)pyridine} (Cu-64-AMD3465), in subcutaneous U87 brain tumors and U87 tumors stably expressing CXCR4 (U87-stb-CXCR4) and in colon tumors (HT-29) using dynamic and whole-body PET supported by ex vivo biodistribution studies. Both dynamic and whole-body PET/CT studies show specific accumulation of radioactivity in U87-stb-CXCR4 tumors, with the percentage injected dose per gram reaching a maximum of 102.70 +/- 20.80 at 60 min and tumor-to-muscle ratios reaching a maximum of 362.56 +/- 153.51 at 90 min after injection of the radiotracer. Similar specificity was also observed in the HT-29 colon tumor model. Treatment with AMD3465 inhibited uptake of radioactivity by the tumors in both models. Our results show that Cu-64-AMD3465 is capable of detecting lesions in a CXCR4-dependent fashion, with high target selectivity, and may offer a scaffold for the synthesis of clinically translatable agents.
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