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.
|Number of pages||10|
|Publication status||Published - 2016 Oct 1|
Bibliographical noteFunding 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.
© 2016 Elsevier Ltd
- Solid tumor
ASJC Scopus subject areas
- Mechanics of Materials
- Ceramics and Composites