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: C Nastruzzi, E Menegatti, C Pastesini, R Cortesi, E Esposito, M Spano, R Biagini, E Cordelli, G Feriotto, R Gambari
• Journal: Biochemical pharmacology (Biochem Pharmacol) Vol. 44 Issue 10 Pg. 1985-94 (Nov 17 1992) ISSN: 0006-2952 [Print] England
• PMID: 1449517 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antigens, Viral
• Benzamidines
• DNA, Viral
• DNA-Binding Proteins
• Epstein-Barr Virus Nuclear Antigens
• 1,3-di-(4-amidinophenoxy)-2,2-bis-(4-amidinophenoxymethyl)propane
• 4,4'-(2,2-bis((4-(aminoiminomethyl)-2-bromophenoxy)methyl)-1,3-propanediyl)bis(oxy))bis(3-bromobenzenecarboximidamide
• diminazene aceturate
• Diminazene

Topics

• Antigens, Viral (chemistry, metabolism)
• Base Sequence
• Benzamidines (pharmacology)
• Cell Cycle
• Cell Division (drug effects)
• DNA, Viral (metabolism)
• DNA-Binding Proteins (chemistry, metabolism)
• Diminazene (analogs & derivatives, pharmacology)
• Dose-Response Relationship, Drug
• Epstein-Barr Virus Nuclear Antigens
• Humans
• Molecular Sequence Data
• Tumor Cells, Cultured (drug effects)