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Title
Japanese: 
English:Development of an oxygen-sensitive degradable peptide probe for the imaging of hypoxia-inducible factor-1-active regions in tumors. 
Author
Japanese: Ueda Masashi, Ogawa Kei, Miyano Azusa, Ono Masahiro, 近藤科江, Saji Hideo.  
English: Ueda Masashi, Ogawa Kei, Miyano Azusa, Ono Masahiro, Kizaka-Kondoh Shinae, Saji Hideo.  
Language English 
Journal/Book name
Japanese: 
English:Molecular imaging and biology 
Volume, Number, Page Vol. 15    No. 6   
Published date Apr. 2013 
Publisher
Japanese: 
English: 
Conference name
Japanese: 
English: 
Conference site
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English: 
Abstract [Purpose]We aimed to develop a radiolabeled peptide probe for the imaging of hypoxia-inducible factor-1 (HIF-1)-active tumors. [Procedures]We synthesized the peptide probes that contain or lack an essential sequence of the oxygen-dependent degradation of HIF-1α in proteasomes ([123/125]I-DKOP30 or [125]I-mDKOP, respectively). The degradation of probes was evaluated in vitro using cell lysates containing proteasomes. In vivo biodistribution study, planar imaging, autoradiography, and comparison between probe accumulation and HIF-1 transcriptional activity were also performed. [Results]The [125]I-DKOP30 underwent degradation in a proteasome-dependent manner, while [125]I-mDKOP was not degraded. Biodistribution analysis showed [125]I-DKOP30 accumulation in tumors. The tumors were clearly visualized by in vivo imaging, and intratumoral distribution of [125]I-DKOP30 coincided with the HIF-1α-positive hypoxic regions. Tumoral accumulation of 125I-DKOP30 was significantly correlated with HIF-1-dependent luciferase bioluminescence, while that of [125]I-mDKOP was not. [Conclusion] [123]I-DKOP30 is a useful peptide probe for the imaging of HIF-1-active tumors.

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