Short, terminally phosphorylated oligoriboguanylic acids effectively inhibit cytopathicity caused by human immunodeficiency virus.
Various synthetic ribonucleic acids were evaluated for inhibition of HIV-induced cytopathicity of cultured cells; only poly and oligoguanylic acids, but not other homopolymers, showed potent inhibitory activity. Phosphorylation of either the 5'- or 3'-end of oligoribonucleotides converted short inactive oligomers, such as dimers to effective anti-HIV agents. The efficacy of the 3'-phosphorylated phosphorothioate trimer of guanylic acid was comparable to that of other longer oligonucleotides so far reported. Phosphorothioate oligoriboguanylic acids were superior to the corresponding oligodeoxyguanylic acids in their capacity to prevent HIV cytopathicity.
Fujihashi
T
T
Department of Pharmacology, Jefferson Medical College, Philadelphia, PA 19107.
Sakata
T
T
Kaji
A
A
Kaji
H
H
D000998:Antiviral Agents / Q000494:pharmacology*; D015496:CD4-Positive T-Lymphocytes; D002460:Cell Line; D003588:Cytopathogenic Effect, Viral / Q000187:drug effects*; D004247:DNA / Q000037:antagonists & inhibitors / Q000494:pharmacology; D006150:Guanine Nucleotides / Q000494:pharmacology*; D006678:HIV / Q000187:drug effects / Q000502:physiology*; D006801:Humans; D046911:Macromolecular Substances; D009843:Oligoribonucleotides / Q000737:chemistry / Q000494:pharmacology*; D010766:Phosphorylation; D011068:Poly G / Q000494:pharmacology; D011131:Polyribonucleotides / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013873:Thionucleotides / Q000494:pharmacology
D000998:Antiviral Agents; D006150:Guanine Nucleotides; D046911:Macromolecular Substances; D009843:Oligoribonucleotides; D011131:Polyribonucleotides; D013873:Thionucleotides; D011068:Poly G; D004247:DNA