title: An aptamer intrinsically comprising 5-fluoro-2'-deoxyuridine for targeted chemotherapy.
abstract: An aptamer specifically binding the interleukin-6 receptor and intrinsically comprising multiple units of the nucleoside analogue 5-fluoro-2'-deoxyuridine can exert a cytostatic effect direcly on certain cells presenting the receptor. Thus the modified aptamer fulfils the requirements for active drug targeting in an unprecedented manner. It can easily be synthesized in a single enzymatic step and it binds to a cell surface receptor that is conveyed into the lysosome. Upon degradation of the aptamer by intracellular nucleases the active drug is released within the targeted cells exclusively. In this way the aptamer acts as a prodrug meeting two major prerequisites of a drug delivery system: specific cell targeting and the controlled release of the drug triggered by an endogenous stimulus.
authors.affiliation: Institut für Biochemie und Molekularbiologie, Universität Hamburg, Martin-Luther-King Platz 6, 20146 Hamburg (Germany).
authors.forename: Sven
authors.initials: S
authors.lastname: Kruspe
authors.forename: Ulrich
authors.initials: U
authors.lastname: Hahn
mesh_terms: D000818:Animals; D017209:Apoptosis / Q000187:drug effects; D052157:Aptamers, Nucleotide / Q000737:chemistry* / Q000378:metabolism; D059447:Cell Cycle Checkpoints / Q000187:drug effects; D045744:Cell Line, Tumor; D003857:Deoxyuridine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000627:therapeutic use / Q000633:toxicity; D004337:Drug Carriers / Q000737:chemistry; D054856:G-Quadruplexes; D051379:Mice; D009369:Neoplasms / Q000188:drug therapy; D011355:Prodrugs / Q000737:chemistry / Q000627:therapeutic use / Q000633:toxicity; D011485:Protein Binding; D019947:Receptors, Interleukin-6 / Q000737:chemistry / Q000378:metabolism
chemical_list: C576827:5-fluoro-2'-deoxyuridine; D052157:Aptamers, Nucleotide; D004337:Drug Carriers; D011355:Prodrugs; D019947:Receptors, Interleukin-6; D003857:Deoxyuridine
keywords: aptamers; chemotherapeutics; drug delivery; nucleoside analogues; targeted therapy