Radiolabeled probes targeting hypoxia-inducible factor-1-active tumor microenvironments

Masashi Ueda, Hideo Saji

Research output: Contribution to journalArticle

2 Citations (Scopus)

Abstract

Because tumor cells grow rapidly and randomly, hypoxic regions arise from the lack of oxygen supply in solid tumors. Hypoxic regions in tumors are known to be resistant to chemotherapy and radiotherapy. Hypoxia-inducible factor-1 (HIF-1) expressed in hypoxic regions regulates the expression of genes related to tumor growth, angiogenesis, metastasis, and therapy resistance. Thus, imaging of HIF-1-active regions in tumors is of great interest. HIF-1 activity is regulated by the expression and degradation of its α subunit (HIF-1α), which is degraded in the proteasome under normoxic conditions, but escapes degradation under hypoxic conditions, allowing it to activate transcription of HIF-1-target genes. Therefore, to image HIF-1-active regions, HIF-1-dependent reporter systems and injectable probes that are degraded in a manner similar to HIF-1α have been recently developed and used in preclinical studies. However, no probe currently used in clinical practice directly assesses HIF-1 activity. Whether the accumulation of 18F-FDG or 18F-FMISO can be utilized as an index of HIF-1 activity has been investigated in clinical studies. In this review, the current status of HIF-1 imaging in preclinical and clinical studies is discussed.

Original languageEnglish
Article number165461
JournalThe Scientific World Journal
Volume2014
DOIs
Publication statusPublished - 2014

Fingerprint

Hypoxia-Inducible Factor 1
Tumor Microenvironment
hypoxia
tumor
targeting
Tumors
probe
Neoplasms
Genes
Oxygen supply
Imaging techniques
chemotherapy
Degradation
degradation
Chemotherapy
gene
Fluorodeoxyglucose F18
Radiotherapy
Proteasome Endopeptidase Complex
Transcription

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Environmental Science(all)
  • Medicine(all)

Cite this

Radiolabeled probes targeting hypoxia-inducible factor-1-active tumor microenvironments. / Ueda, Masashi; Saji, Hideo.

In: The Scientific World Journal, Vol. 2014, 165461, 2014.

Research output: Contribution to journalArticle

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