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

Publication ,  Journal Article
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 in: Journal of medicinal chemistry
May 2021

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 (2.46 ± 0.48 at 2 h pi) was well improved compared with that of [18F]-FMISO (1.25 ± 0.14 at 2 h pi). A comparable distribution pattern was observed between ex vivo autoradiography of [18F]-23 and pimonidazole staining of the neighboring slice, indicating that [18F]-23 is a promising PET agent for hypoxia imaging.

Duke Scholars

Published In

Journal of medicinal chemistry

DOI

EISSN

1520-4804

ISSN

0022-2623

Publication Date

May 2021

Volume

64

Issue

9

Start / End Page

5593 / 5602

Related Subject Headings

  • Tumor Hypoxia
  • Transplantation, Heterologous
  • Sulfinic Acids
  • Radiopharmaceuticals
  • Positron-Emission Tomography
  • Polyethylene Glycols
  • Nitroimidazoles
  • Neoplasms
  • Mice, Nude
  • Mice, Inbred C57BL
 

Citation

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Wang, L., Wang, H., Shen, K., Park, H., Zhang, T., Wu, X., … Li, Z. (2021). Development of Novel 18F-PET Agents for Tumor Hypoxia Imaging. Journal of Medicinal Chemistry, 64(9), 5593–5602. https://doi.org/10.1021/acs.jmedchem.0c01962
Wang, Li, Hui Wang, Kun Shen, Hyejin Park, Tao Zhang, Xuedan Wu, Mei Hu, et al. “Development of Novel 18F-PET Agents for Tumor Hypoxia Imaging.Journal of Medicinal Chemistry 64, no. 9 (May 2021): 5593–5602. https://doi.org/10.1021/acs.jmedchem.0c01962.
Wang L, Wang H, Shen K, Park H, Zhang T, Wu X, et al. Development of Novel 18F-PET Agents for Tumor Hypoxia Imaging. Journal of medicinal chemistry. 2021 May;64(9):5593–602.
Wang, Li, et al. “Development of Novel 18F-PET Agents for Tumor Hypoxia Imaging.Journal of Medicinal Chemistry, vol. 64, no. 9, May 2021, pp. 5593–602. Epmc, doi:10.1021/acs.jmedchem.0c01962.
Wang L, Wang H, Shen K, Park H, Zhang T, Wu X, Hu M, Yuan H, Chen Y, Wu Z, Wang Q, Li Z. Development of Novel 18F-PET Agents for Tumor Hypoxia Imaging. Journal of medicinal chemistry. 2021 May;64(9):5593–5602.
Journal cover image

Published In

Journal of medicinal chemistry

DOI

EISSN

1520-4804

ISSN

0022-2623

Publication Date

May 2021

Volume

64

Issue

9

Start / End Page

5593 / 5602

Related Subject Headings

  • Tumor Hypoxia
  • Transplantation, Heterologous
  • Sulfinic Acids
  • Radiopharmaceuticals
  • Positron-Emission Tomography
  • Polyethylene Glycols
  • Nitroimidazoles
  • Neoplasms
  • Mice, Nude
  • Mice, Inbred C57BL