Hypoxia-directed and activated theranostic agent: Imaging and treatment of solid tumor

Rajesh Kumar, Eun Joong Kim, Jiyou Han, Hyunseung Lee, Weon Sup Shin, Hyun Min Kim, Sankarprasad Bhuniya, Jong Seung Kim, Kwan Soo Hong

Research output: Contribution to journalArticlepeer-review

78 Citations (Scopus)


Hypoxia, a distinguished feature of various solid tumors, has been considered as a key marker for tumor progression. Inadequate vasculature and high interstitial pressures result in relatively poor drug delivery to these tumors. Herein, we developed an antitumor theranostic agent, 4, which is activated in hypoxic conditions and can be used for the diagnosis and treatment of solid tumors. Compound 4, bearing biotin, a tumor-targeting unit, and SN38, an anticancer drug, proved to be an effective theranostic agent for solid tumors. SN38 plays a dual role: as an anticancer drug for therapy and as a fluorophore for diagnosis, thus avoids an extra fluorophore and limits cytotoxicity. Compound 4, activated in the hypoxic environment, showed high therapeutic activity in A549 and HeLa cells and spheroids. In vivo imaging of solid tumors confirmed the tumor-specific localization, deep tissue penetration and activation of compound 4, as well as the production of a strong anticancer effect through the inhibition of tumor growth in a xenograft mouse model validating it as a promising strategy for the treatment of solid tumors.

Original languageEnglish
Pages (from-to)119-128
Number of pages10
Publication statusPublished - 2016 Oct 1

Bibliographical note

Funding Information:
This work was supported by the CRI project (No. 2009-0081566 to J.S.K.) from the NRF of Korea, a grant from Korea Basic Science Institute ( D35401 , K.S.H.) and Basic Research Program through the NRF funded by the Ministry of Science, ICT & Future Planning (No. 2015R1C1A1A02036905 ) and a Research Fellowship Grant from Korea University to J.H.

Publisher Copyright:
© 2016 Elsevier Ltd


  • Anti-tumor
  • Hypoxia
  • Prodrug
  • Solid tumor
  • Theranostic

ASJC Scopus subject areas

  • Mechanics of Materials
  • Ceramics and Composites
  • Bioengineering
  • Biophysics
  • Biomaterials


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