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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.


Madhuri Dasari, Abhinav P Acharya, Dongin Kim, Seungjun Lee, Sungmun Lee, Jeanne Rhea, Ross Molinaro, Niren Murthy. H-gemcitabine: a new gemcitabine prodrug for treating cancer. Bioconjugate chemistry. 2013 Jan 16;24(1):4-8

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PMID: 23237198

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