Document Detail


H-gemcitabine: a new gemcitabine prodrug for treating cancer.
MedLine Citation:
PMID:  23237198     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
In this report, we present a new strategy for targeting chemotherapeutics to tumors, based on targeting extracellular DNA. A gemcitabine prodrug was synthesized, termed H-gemcitabine, which is composed of Hoechst conjugated to gemcitabine. H-gemcitabine has low toxicity because it is membrane-impermeable; however, it still has high tumor efficacy because of its ability to target gemcitabine to E-DNA in tumors. We demonstrate here that H-gemcitabine has a wider therapeutic window than free gemcitabine.
Authors:
Madhuri Dasari; Abhinav P Acharya; Dongin Kim; Seungjun Lee; Sungmun Lee; Jeanne Rhea; Ross Molinaro; Niren Murthy
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Research Support, U.S. Gov't, Non-P.H.S.; Research Support, U.S. Gov't, P.H.S.     Date:  2012-12-26
Journal Detail:
Title:  Bioconjugate chemistry     Volume:  24     ISSN:  1520-4812     ISO Abbreviation:  Bioconjug. Chem.     Publication Date:  2013 Jan 
Date Detail:
Created Date:  2013-01-16     Completed Date:  2013-06-24     Revised Date:  2013-11-25    
Medline Journal Info:
Nlm Unique ID:  9010319     Medline TA:  Bioconjug Chem     Country:  United States    
Other Details:
Languages:  eng     Pagination:  4-8     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
Animals
Antimetabolites, Antineoplastic / administration & dosage,  chemistry*,  pharmacokinetics,  therapeutic use*
Binding Sites
Cell Line, Tumor
DNA / metabolism
Deoxycytidine / administration & dosage,  analogs & derivatives*,  chemistry,  pharmacokinetics,  therapeutic use
Drug Delivery Systems
Humans
Mice
Mice, Nude
Neoplasms / drug therapy*,  metabolism
Prodrugs / administration & dosage,  chemistry*,  pharmacokinetics,  therapeutic use*
Grant Support
ID/Acronym/Agency:
R01 HL096796/HL/NHLBI NIH HHS; R01 HL096796-01/HL/NHLBI NIH HHS; R21 AI098799/AI/NIAID NIH HHS
Chemical
Reg. No./Substance:
0/Antimetabolites, Antineoplastic; 0/Prodrugs; 0W860991D6/Deoxycytidine; 9007-49-2/DNA; B76N6SBZ8R/gemcitabine

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


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