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Cell-Specific, Activatable, and Theranostic Prodrug for Dual-Targeted Cancer Imaging and Therapy
Open accessAbstract
Herein we describe the design and synthesis of a folate-doxorubicin conjugate with activatable fluorescence and activatable cytotoxicity. In this study we discovered that the cytotoxicity and fluorescence of doxorubicin are quenched (OFF) when covalently linked with folic acid. Most importantly, when the conjugate is designed with a disulfide bond linking the targeting folate unit and the cytotoxic doxorubicin, a targeted activatable prodrug is obtained that becomes activated (ON) within the cell by glutathione-mediated dissociation and nuclear translocation, showing enhanced fluorescence and cellular toxicity. In our novel design, folic acid acted as both a targeting ligand for the folate receptor as well as a quencher for doxorubicin's fluorescence.
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Cited by
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Yuan, Y., Kwok, R. T. K., Tang, B. Z., & Liu, B. (2014) · Journal of the American Chemical Society · doi:10.1021/ja411811w · Cited by 474
Noncanonical Self-Assembly of Multifunctional DNA Nanoflowers for Biomedical Applications
Zhu, G., Hu, R., Zhao, Z., Chen, Z., Zhang, X., & Tan, W. (2013) · Journal of the American Chemical Society · doi:10.1021/ja406115e · Cited by 429
Small conjugate-based theranostic agents: an encouraging approach for cancer therapy
Kumar, R., Shin, W. S., Sunwoo, K., Kim, W. Y., Koo, S., Bhuniya, S., & Kim, J. S. (2015) · Chemical Society Reviews · doi:10.1039/c5cs00224a · Cited by 381
ROS-Activated Ratiometric Fluorescent Polymeric Nanoparticles for Self-Reporting Drug Delivery
Zhang, M., Song, C.-C., Su, S., Du, F.-S., & Li, Z.-C. (2018) · ACS Applied Materials & Interfaces · doi:10.1021/acsami.7b18438 · Cited by 64
Metadata
- Authors
- Santra, S., Kaittanis, C., Santiesteban, O. J., & Perez, J. M.
- Venue
- Journal of the American Chemical Society
- Publisher
- American Chemical Society (ACS)
- Published
- 2011-09-27
- Volume
- 133
- Issue
- 41
- Pages
- 16680-16688
- ISSN
- 0002-7863 (ISSN-L)
- 1520-5126
- OpenAlex
- W2077085160
- Cited by
- 295
- References
- 0
- FWCI
- 11.30
- Type
- journal article
- Language
- en
- Open access
- green
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- Santra, S., Kaittanis, C., Santiesteban, O. J., & Perez, J. M. (2011). Cell-Specific, Activatable, and Theranostic Prodrug for Dual-Targeted Cancer Imaging and Therapy. Journal of the American Chemical Society. https://doi.org/10.1021/ja207463b
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Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
