PT - JOURNAL ARTICLE AU - Jiyuan Li AU - Yuxiang Han AU - Hui Liu AU - Zhibo Liu TI - A boron derived tyrosine mimic identifies cancer with positron emission tomography DP - 2018 May 01 TA - Journal of Nuclear Medicine PG - 1259--1259 VI - 59 IP - supplement 1 4099 - http://jnm.snmjournals.org/content/59/supplement_1/1259.short 4100 - http://jnm.snmjournals.org/content/59/supplement_1/1259.full SO - J Nucl Med2018 May 01; 59 AB - 1259Objectives: Non-invasive diagnosis of cancer is a enormous challenge in clinics due to the rising number of patients. A biopsy or surgery is often required to justify the malignancy of certain types of cancer. Previously, positron emission tomography (PET) with 18F-FDG is the standard non-invasive technique for cancer imaging. However, FDG highlights any tissue with high energy consumption and is not tumor-specific. FDG accumulation may be observed in a variety of healthy tissues and ones affected by various non-neoplastic pathologic conditions, such as acute and chronic inflammations and infections. Herein we report a 18F-labeled boron-derived tyrosine derivative (B-Tyr) to target cancer with high specificity in living systems. METHOD A boron-derived tyrosine derivative was synthesized to mimic Tyr, of which the transportation depends on L-type amino acid transporter (LAT). 18F-19F isotope exchange reaction was conducted for radiolabeling and quality control was performed by both HPLC and radioTLC. The metabolic stability of 18F-B-Tyr was assessed both in vitro and in vivo. PET imaging and bio-distribution studies were performed in mice bearing A549 and BGC823 xenografts on the shoulder. RESULT The intracellular uptake of B-Tyr was highly selective and competed effectively with natural Tyr. Remarkably, 18F-B-Tyr is highly metabolically stable, which is a unique advantage because metabolism of imaging probe often results in low tumor-specificity with high background uptake. As expected, 18F-B-Tyr showed high accumulation in A549 tumor (6.28 ± 1.6 %ID/g) and BGC823 tumor (8.63 ± 1.7 %ID/g) and low uptake in the rest of the body. The tracer had predominant renal clearance but with low kidney retention. CONCLUSION A boron-derived Tyr derivative was developed and evaluated for targeting LAT-1 expression with PET. Administration of 18F-B-Tyr allowed for clear visualization of tumor xenografts in mice, suggesting a unique advantage over 18F-FDG, which is currently the gold standard PET tracer for clinical diagnosis. Furthermore, B-Tyr can serve as a potential boron delivery agent for boron neutron capture therapy. <!--EndFragment-->