Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2013 Dec;15(6):713-21.
doi: 10.1007/s11307-013-0647-6.

Development of an oxygen-sensitive degradable peptide probe for the imaging of hypoxia-inducible factor-1-active regions in tumors

Masashi Ueda  1 , Kei Ogawa, Azusa Miyano, Masahiro Ono, Shinae Kizaka-Kondoh, Hideo Saji
Affiliations
Free article

Development of an oxygen-sensitive degradable peptide probe for the imaging of hypoxia-inducible factor-1-active regions in tumors

Masashi Ueda et al. Mol Imaging Biol. 2013 Dec.
Free article

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 (125)I-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.

PubMed Disclaimer

Similar articles

See all similar articles

Cited by

References

    1. Trends Biochem Sci. 2012 Sep;37(9):364-72 - PubMed
    1. Histopathology. 2011 Jun;58(7):1136-47 - PubMed
    1. Int J Rad Appl Instrum B. 1992 Apr;19(3):289-95 - PubMed
    1. J Radiat Res. 2011;52(5):545-56 - PubMed
    1. Magn Reson Imaging. 2004 Sep;22(7):905-12 - PubMed

Publication types

MeSH terms

LinkOut - more resources