title: DNA binding activity and inhibition of DNA-protein interactions. Differential effects of tetra-p-amidino-phenoxyneopentane and its 2'-bromo derivative.
abstract: In the present study are reported the differential DNA binding activity of the anti-tumor polyamidine tetra-p-amidinophenoxyneopentane (TAPP-H) and its 2'-halo derivative (TAPP-Br), and their effects on the binding of the recombinant Epstein-Barr virus (EBV) nuclear antigen to a synthetic oligonucleotide mimicking the target DNA sequence present in the EBV genome. In addition, the proliferation kinetics and cell cycle analysis of human leukemia K562 cells treated with TAPP-H and TAPP-Br are reported. The possible in vivo relationship between DNA binding affinity and cytotoxicity is also discussed.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Italy.
authors.forename: C
authors.initials: C
authors.lastname: Nastruzzi
authors.forename: E
authors.initials: E
authors.lastname: Menegatti
authors.forename: C
authors.initials: C
authors.lastname: Pastesini
authors.forename: R
authors.initials: R
authors.lastname: Cortesi
authors.forename: E
authors.initials: E
authors.lastname: Esposito
authors.forename: M
authors.initials: M
authors.lastname: Spano
authors.forename: R
authors.initials: R
authors.lastname: Biagini
authors.forename: E
authors.initials: E
authors.lastname: Cordelli
authors.forename: G
authors.initials: G
authors.lastname: Feriotto
authors.forename: R
authors.initials: R
authors.lastname: Gambari
mesh_terms: D000956:Antigens, Viral / Q000737:chemistry / Q000378:metabolism*; D001483:Base Sequence; D001550:Benzamidines / Q000494:pharmacology*; D002453:Cell Cycle; D002455:Cell Division / Q000187:drug effects; D004279:DNA, Viral / Q000378:metabolism*; D004268:DNA-Binding Proteins / Q000737:chemistry / Q000378:metabolism*; D004133:Diminazene / Q000031:analogs & derivatives / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D019309:Epstein-Barr Virus Nuclear Antigens; D006801:Humans; D008969:Molecular Sequence Data; D014407:Tumor Cells, Cultured / Q000187:drug effects
chemical_list: D000956:Antigens, Viral; D001550:Benzamidines; D004279:DNA, Viral; D004268:DNA-Binding Proteins; D019309:Epstein-Barr Virus Nuclear Antigens; C057885:1,3-di-(4-amidinophenoxy)-2,2-bis-(4-amidinophenoxymethyl)propane; C057886:4,4'-(2,2-bis((4-(aminoiminomethyl)-2-bromophenoxy)methyl)-1,3-propanediyl)bis(oxy))bis(3-bromobenzenecarboximidamide; C003915:diminazene aceturate; D004133:Diminazene