Title

Cell-Specific, Activatable, And Theranostic Prodrug For Dual-Targeted Cancer Imaging And Therapy

Abstract

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. © 2011 American Chemical Society.

Publication Date

10-19-2011

Publication Title

Journal of the American Chemical Society

Volume

133

Issue

41

Number of Pages

16680-16688

Document Type

Article

Personal Identifier

scopus

DOI Link

https://doi.org/10.1021/ja207463b

Socpus ID

80054766761 (Scopus)

Source API URL

https://api.elsevier.com/content/abstract/scopus_id/80054766761

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