Document Detail


Cell-Specific, Activatable and Theranostic Prodrug for Dual Targeted Cancer Imaging and Therapy.
MedLine Citation:
PMID:  21910482     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
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 target-ing 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 fluorescence.
Authors:
Santimukul Santra; Charalambos Kaittanis; Oscar J Santiesteban; J Manuel Perez
Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2011-9-12
Journal Detail:
Title:  Journal of the American Chemical Society     Volume:  -     ISSN:  1520-5126     ISO Abbreviation:  -     Publication Date:  2011 Sep 
Date Detail:
Created Date:  2011-9-13     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7503056     Medline TA:  J Am Chem Soc     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Descriptor/Qualifier:

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


Previous Document:  ANTIOXIDANT ACTIVITY OF ALKYLRESORCINOLS FROM RYE BRAN AND THEIR PROTECTIVE EFFECTS ON CELL VIABILIT...
Next Document:  Synthesis of Sterically Crowded Polyarylated Boron-Dipyrromethenes.