title: H-gemcitabine: a new gemcitabine prodrug for treating cancer.
abstract: 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.affiliation: Wallace H. Coulter Department of Biomedical Engineering, Georgia Institute of Technology, Parker H. Petit Institute for Bioengineering and Bioscience, 315 Ferst Drive, Atlanta, GA 30332, USA.
authors.forename: Madhuri
authors.initials: M
authors.lastname: Dasari
authors.forename: Abhinav P
authors.initials: AP
authors.lastname: Acharya
authors.forename: Dongin
authors.initials: D
authors.lastname: Kim
authors.forename: Seungjun
authors.initials: S
authors.lastname: Lee
authors.forename: Sungmun
authors.initials: S
authors.lastname: Lee
authors.forename: Jeanne
authors.initials: J
authors.lastname: Rhea
authors.forename: Ross
authors.initials: R
authors.lastname: Molinaro
authors.forename: Niren
authors.initials: N
authors.lastname: Murthy
mesh_terms: D000818:Animals; D000964:Antimetabolites, Antineoplastic / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics / Q000627:therapeutic use*; D001665:Binding Sites; D045744:Cell Line, Tumor; D004247:DNA / Q000378:metabolism; D003841:Deoxycytidine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use; D016503:Drug Delivery Systems; D006801:Humans; D051379:Mice; D008819:Mice, Nude; D009369:Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D011355:Prodrugs / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics / Q000627:therapeutic use*; D000093542:Gemcitabine
chemical_list: D000964:Antimetabolites, Antineoplastic; D011355:Prodrugs; D003841:Deoxycytidine; D004247:DNA; D000093542:Gemcitabine