PMID- 23689986
OWN - NLM
STAT- MEDLINE
DCOM- 20140619
LR  - 20211021
IS  - 1860-2002 (Electronic)
IS  - 1536-1632 (Linking)
VI  - 15
IP  - 6
DP  - 2013 Dec
TI  - Development of an oxygen-sensitive degradable peptide probe for the imaging of 
      hypoxia-inducible factor-1-active regions in tumors.
PG  - 713-21
LID - 10.1007/s11307-013-0647-6 [doi]
AB  - 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-1alpha 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-1alpha-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.
FAU - Ueda, Masashi
AU  - Ueda M
AD  - Radioisotopes Research Laboratory, Kyoto University Hospital, Faculty of 
      Medicine, Kyoto University, 54 Shogoin Kawahara-cho, Sakyo-ku, Kyoto, 606-8507, 
      Japan.
FAU - Ogawa, Kei
AU  - Ogawa K
FAU - Miyano, Azusa
AU  - Miyano A
FAU - Ono, Masahiro
AU  - Ono M
FAU - Kizaka-Kondoh, Shinae
AU  - Kizaka-Kondoh S
FAU - Saji, Hideo
AU  - Saji H
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - United States
TA  - Mol Imaging Biol
JT  - Molecular imaging and biology
JID - 101125610
RN  - 0 (Hypoxia-Inducible Factor 1)
RN  - 0 (Molecular Probes)
RN  - 0 (Peptides)
SB  - IM
MH  - Amino Acid Sequence
MH  - Animals
MH  - Autoradiography
MH  - Cell Hypoxia
MH  - Cell Line, Tumor
MH  - Female
MH  - HeLa Cells
MH  - Humans
MH  - Hypoxia-Inducible Factor 1/*analysis/chemistry/*metabolism
MH  - Mice
MH  - Mice, Inbred BALB C
MH  - Mice, Inbred C3H
MH  - Mice, Nude
MH  - *Molecular Probe Techniques
MH  - Molecular Probes/chemistry/*pharmacokinetics
MH  - Molecular Sequence Data
MH  - Peptides/*chemistry/pharmacokinetics
MH  - Tissue Distribution
MH  - Tomography, Emission-Computed, Single-Photon
EDAT- 2013/05/22 06:00
MHDA- 2014/06/20 06:00
CRDT- 2013/05/22 06:00
PHST- 2013/05/22 06:00 [entrez]
PHST- 2013/05/22 06:00 [pubmed]
PHST- 2014/06/20 06:00 [medline]
AID - 10.1007/s11307-013-0647-6 [doi]
PST - ppublish
SO  - Mol Imaging Biol. 2013 Dec;15(6):713-21. doi: 10.1007/s11307-013-0647-6.