Conception, preparation and biological evaluation of one inhibitor of the HIV-1 Tat-TAR complex

Citation
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
Citations number
8
Categorie Soggetti
Biochemistry & Biophysics
Journal title
NUCLEOSIDES & NUCLEOTIDES
ISSN journal
07328311 → ACNP
Volume
18
Issue
6-7
Year of publication
1999
Pages
1497 - 1499
Database
ISI
SICI code
0732-8311(1999)18:6-7<1497:CPABEO>2.0.ZU;2-Q
Abstract
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.