Title

Cell-Specific, Activatable, and Theranostic Prodrug for Dual-Targeted Cancer Imaging and Therapy

Authors

Authors

S. Santra; C. Kaittanis; O. J. Santiesteban;J. M. Perez

Comments

Authors: contact us about adding a copy of your work at STARS@ucf.edu

Abbreviated Journal Title

J. Am. Chem. Soc.

Keywords

FOLATE RECEPTOR; IN-VIVO; DRUG-DELIVERY; FOLIC-ACID; INFLAMMATORY; DISEASES; BIOLOGICAL EVALUATION; TUMOR-CELLS; NANOPARTICLES; DESIGN; PROBES; Chemistry, Multidisciplinary

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.

Journal Title

Journal of the American Chemical Society

Volume

133

Issue/Number

41

Publication Date

1-1-2011

Document Type

Article

Language

English

First Page

16680

Last Page

16688

WOS Identifier

WOS:000295997500060

ISSN

0002-7863

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