title: [DNA-binding and antiviral activities of bis-netropsins].
abstract: The DNA-binding and antiviral activitus of bis-netropsins in which two monomers are attached covalently via three glycin residue were studied. These compounds have the same C-end groups but contain clusters with different numbers of lysine residues at the N-end of the molecule. In the homologous series of these compounds, bis-neropsins containing 15 and 31 branched lysine residues at the N-end of the molecule appear to be the most effective inhibitors of reproduction of the simplex herpes virus of type I in the Vero cell culture, including the virus versions resistant to aciclovir, ganciclovir, and other medicinal preparations. It was shown that the cytotoxicity of all the compounds studied is much lower than that of netropsin. The antiviral activity of the compounds correlates with their ability to selectively interact with the expanded clusters of the AT-pairs of DNA bases in the form of a monomer or a dimer, stabilized by interaction between the C-end halves of two bis-netropsin molecules bound at the neighboring overlapping binding sites on the DNA. The possible sites of their binding are the expanded clusters of AT-pairs at the origin of replication of OriS and OriL of the herpes virus.
authors.forename: A N
authors.initials: AN
authors.lastname: Surovaia
authors.forename: V L
authors.initials: VL
authors.lastname: Andronova
authors.forename: S L
authors.initials: SL
authors.lastname: Grokhovskiĭ
authors.forename: G A
authors.initials: GA
authors.lastname: Galegov
authors.forename: G V
authors.initials: GV
authors.lastname: Gurskiĭ
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000737:chemistry / Q000494:pharmacology*; D002522:Chlorocebus aethiops; D004279:DNA, Viral / Q000378:metabolism*; D018259:Herpesvirus 1, Human / Q000378:metabolism*; D009429:Netropsin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D014709:Vero Cells; D014779:Virus Replication / Q000187:drug effects*
chemical_list: D000998:Antiviral Agents; D004279:DNA, Viral; D009429:Netropsin; C032161:bis-netropsin