Jr. Wyatt et al., COMBINATORIALLY SELECTED GUANOSINE-QUARTET STRUCTURE IS A POTENT INHIBITOR OF HUMAN-IMMUNODEFICIENCY-VIRUS ENVELOPE-MEDIATED CELL-FUSION, Proceedings of the National Academy of Sciences of the United Statesof America, 91(4), 1994, pp. 1356-1360
The phosphorothioate oligonucleotide T(2)G(4)T(2) was identified as an
inhibitor of HIV infection in vitro by combinatorial screening of a l
ibrary of phosphorothioate oligonucleotides that contained all possibl
e octanucleotide sequences. The oligonucleotide forms a parallel-stran
ded tetrameric guanosine-quartet structure. Tetramer formation and the
phosphorothioate backbone are essential for antiviral activity. The t
etramer binds to the human immunodeficiency virus envelope protein gp1
20 at the V3 loop and inhibits both cell to-cell and virus-to cell inf
ection.