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タイトル: | Development of an oxygen-sensitive degradable peptide probe for the imaging of hypoxia-inducible factor-1-active regions in tumors. |
著者: | Ueda, Masashi Ogawa, Kei Miyano, Azusa Ono, Masahiro https://orcid.org/0000-0002-2497-039X (unconfirmed) Kizaka-Kondoh, Shinae Saji, Hideo |
著者名の別形: | 上田, 真史 佐治, 英郎 |
キーワード: | Tumor hypoxia Hypoxia-inducible factor-1 Oxygen-dependent degradation Peptide Nuclear medical imaging |
発行日: | 21-May-2013 |
出版者: | Springer |
誌名: | Molecular imaging and biology |
巻: | 15 |
号: | 6 |
開始ページ: | 713 |
終了ページ: | 721 |
抄録: | [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. |
著作権等: | The final publication is available at Springer via http://dx.doi.org/10.1007/s11307-013-0647-6 この論文は出版社版でありません。引用の際には出版社版をご確認ご利用ください。 This is not the published version. Please cite only the published version. |
URI: | http://hdl.handle.net/2433/196858 |
DOI(出版社版): | 10.1007/s11307-013-0647-6 |
PubMed ID: | 23689986 |
出現コレクション: | 学術雑誌掲載論文等 |
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