TAPP (TETRA-PARA-AMIDINOPHENOXYNEOPENTANE) INHIBITS THE BINDING OF NUCLEAR FACTORS TO TARGET DNA-SEQUENCES

The aromatic polyamidine tetra-p-amidinophenoxyneopentane (TAPP), a compound exhibiting strong anti tumor activity both 'in vivo' and 'in vitro', was tested for the ability to bind DNA and to interfere with protein-DNA interactions. In this paper we show that TAPP binds DNA and inhibits the binding of the nuclear protein factors GTATA/IFN-gamma, OTF-1, NFE-1 and Sp1 with specific target DNA sequences present in the HLA-DR-alpha gene, in the gamma-globin gene and in the LTR of HIV-1. These inhibitory effects of TAPP are comparable to those of distamycin, a DNA-binding drug able to suppress DNA-protein interactions. The gel retardation approach described in the present paper could represent a powerful tool to identify potential antitumor and antiviral drugs.