Tumor angiogenesis imaging agent: biodistribution of131I-YG5 and 131I-Boc-YG5

RADIOCHEMISTRY, RADIOPHARMACEUTICALS AND NUCLEAR MEDICINE

Tumor angiogenesis imaging agent: biodistribution of¹³¹I-YG5 and ¹³¹I-Boc-YG5

SUN Xin，

CHU Taiwei，

WANG Xiangyun

Nuclear Science and Techniques

Vol.21, No.5

pp.302-305

Published in print 20 Oct 2010

DOI：10.13538/j.1001-8042/nst.21.302-305

28800

The cyclic peptide YG5 and the t-butyloxycarbonyl (Boc)-modified analog (Boc-YG5) were labeled with radioiodine. The radiochemical purity of ¹³¹I-YG5 or ¹³¹I-Boc-YG5 was almost 100% after purification by RP-HPLC. Biodistribution in BALB/C nude mice bearing MCF-7 tumor was measured. After t-butyloxycarbonyl (Boc)-modification, the ¹³¹I-Boc-YG5 was quite resistant to deiodination in vivo, resulting in negligible radioactivity accumulation in thyroid. The radiotracer clearance in tumor became faster, the absolute tumor uptake decreased for ¹³¹I-Boc-YG5, but the tumor-to-tissue uptake ratios increased. The uptake ratios of tumor to muscle, blood, heart, and lung at 1 h post injection reached 4.73, 1.70, 4.09 and 1.70, respectively. It is demonstrated that Boc-group is an effective prosthetic one to prevent deiodination in vivo and improve tumor imaging for radioiodinated NGR.

RadioiodinationAngiogenesisBiodistributionNGRDeiodinationt-butyloxycarbonyl

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