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
Language
- eng