Oligodeoxynucleoside phosphoramidates and phosphorothioates as inhibitors of human immunodeficiency virus.
Agrawal S, Goodchild J, Civeira MP [SP], Thornton AH, Sarin PS, Zamecnik PC.
Worcester Foundation for Experimental Biology, Shrewsbury, MA 01545.
Magazine: Proceedings of the National Academy of Sciences of the United States of America
Date: Sep 30, 1988Internal Medicine [SP]
Modified oligodeoxynucleotides complementary to RNA of human immunodeficiency virus 1 (HIV-1) were tested for their ability to inhibit virally induced syncytium formation and expression of viral p24 protein. The modifications of oligomers include replacement of backbone phosphodiester groups with phosphorothioates and various phosphoramidates.
All oligomers were found to be active. Oligomers with complete replacement of phosphodiesters with phosphoramidate or phosphorothioate groups were more active at the micromolar range than were unmodified oligomers of the same sequence. In addition, modified and unmodified homooligonucleotides also showed inhibition of HIV-1 replication.
It is suggested that different classes of oligonucleotides may inhibit HIV replication by different mechanisms.
CITATION Proc Natl Acad Sci U S A. 1988 Oct;85(19):7079-83
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