S. Pairot et al., Conception, preparation and biological evaluation of one inhibitor of the HIV-1 Tat-TAR complex, NUCLEOS NUC, 18(6-7), 1999, pp. 1497-1499
A new compound Z-AG5-E potentially inhibitor of the HIV-1 Tat-TAR complex w
as prepared. This compound is constituted by a dinucleotide analog (PNA dim
er) bound, through a linker, to an arginine residue. Z-AG5-E inhibits viral
development in cell culture with a micromolar IC50 and without cellular to
xicity until 200 mu M concentration. Circular dichroism studies have shown
that Z-AG5-E binds a synthetic TAR-RNA.