Development of Novel 18 F-PET Agents for Tumor Hypoxia Imaging.

Journal Article (Journal Article)

Tumor hypoxia is a major factor responsible for tumor progression, metastasis, invasion, and treatment resistance, leading to low local tumor control and recurrence after radiotherapy in cancers. Here,18 F-positron emission tomography (PET) probes are developed for visualizing viable hypoxic cells in biopsies. Pimonidazole derivatives and nitroimidazole-based agents bearing sulfonyl linkers were evaluated. A small-animal PET study showed that the tumor uptake of [18 F]-23 [poly(ethylene glycols) (PEG)-sulfonyl linker] of 3.36 ± 0.29%ID/g was significantly higher (P < 0.01) than that of [18 F]-20 (piperazine-linker tracer, 2.55 ± 0.49%ID/g) at 2 h postinjection in UPPL tumors. The tumor-to-muscle uptake ratio of [18 F]-23 (2.46 ± 0.48 at 2 h pi) was well improved compared with that of [18 F]-FMISO (1.25 ± 0.14 at 2 h pi). A comparable distribution pattern was observed between ex vivo autoradiography of [18 F]-23 and pimonidazole staining of the neighboring slice, indicating that [18 F]-23 is a promising PET agent for hypoxia imaging.

Full Text

Duke Authors

Cited Authors

  • Wang, L; Wang, H; Shen, K; Park, H; Zhang, T; Wu, X; Hu, M; Yuan, H; Chen, Y; Wu, Z; Wang, Q; Li, Z

Published Date

  • May 1, 2021

Published In

Volume / Issue

  • 64 / 9

Start / End Page

  • 5593 - 5602

PubMed ID

  • 33901402

Pubmed Central ID

  • PMC8552308

Electronic International Standard Serial Number (EISSN)

  • 1520-4804

International Standard Serial Number (ISSN)

  • 0022-2623

Digital Object Identifier (DOI)

  • 10.1021/acs.jmedchem.0c01962


  • eng