title: [Interaction of alkylating oligonucleotide derivatives with mammalian cells. A study of the uptake mechanism of derivative cells].
abstract: Interaction of alkylating deoxyribooligonucleotide derivatives, bearing 4-[(N-2-chloroethyl-N-methyl)amino]benzylamine residues at their 5'-terminal phosphates, with mouse fibroblasts L929 and with ascite carcinoma cells Krebs 2 has been investigated. It was found, that the derivatives are taken up by the cells according to the endocytosis mechanism. At high concentration of the oligonucleotide derivatives in the cultivation medium (greater than 10 microM), the fluid phase endocytosis is the major pathway of uptake; binding of the derivatives by the cells is partially reversible and their intracellular mean concentration approaches 1/20 of their extracellular concentration. At low concentration of the oligonucleotide derivatives, the predominant mechanism is the more efficient adsorption endocytosis; at concentration of the derivatives less than 0.5 microM, their mean intracellular concentration exceeds that in the culture medium. Stability of the oligonucleotide derivatives in cells depends on their nucleotide composition. Their nucleolytic degradation rate is low enough to allow them to react with cellular biopolymers.
authors.forename: V V
authors.initials: VV
authors.lastname: Vlasov
authors.forename: E M
authors.initials: EM
authors.lastname: Ivanova
authors.forename: I V
authors.initials: IV
authors.lastname: Kutiavin
authors.forename: A S
authors.initials: AS
authors.lastname: Raĭt
authors.forename: L V
authors.initials: LV
authors.lastname: Iurchenko
mesh_terms: D000477:Alkylating Agents / Q000378:metabolism* / Q000494:pharmacology; D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D003854:Deoxyribonucleotides / Q000378:metabolism* / Q000494:pharmacology; D004591:Electrophoresis, Polyacrylamide Gel; D004705:Endocytosis; D007700:Kinetics; D007739:L Cells; D051379:Mice; D014407:Tumor Cells, Cultured / Q000187:drug effects / Q000378:metabolism*
chemical_list: D000477:Alkylating Agents; D003854:Deoxyribonucleotides
vernacular_title: Vzaimodeĭstvie alkiliruiushchikh proizvodnykh oligonukleotidov tkami mlekopitaiushchikh. Issledovanie mekhanizmov zakhvata proizvodnykh kletkami.