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

ABSTRACT: 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,¹⁸F-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 [¹⁸F]-23 [poly(ethylene glycols) (PEG)-sulfonyl linker] of 3.36 ± 0.29%ID/g was significantly higher (P < 0.01) than that of [¹⁸F]-20 (piperazine-linker tracer, 2.55 ± 0.49%ID/g) at 2 h postinjection in UPPL tumors. The tumor-to-muscle uptake ratio of [¹⁸F]-23 (

SUBMITTER: Wang L 

PROVIDER: S-EPMC8552308 | biostudies-literature | 2021 May

REPOSITORIES: biostudies-literature