Inhibition of HIV-1 Replication by a Nonnucleoside Reverse Transcriptase Inhibitor

Medientyp: E-Artikel
Titel: Inhibition of HIV-1 Replication by a Nonnucleoside Reverse Transcriptase Inhibitor
Beteiligte: Merluzzi, Vincent J.; Hargrave, Karl D.; Labadia, Mark; Grozinger, Karl; Skoog, Mark; Wu, Joseph C.; Shih, Cheng-Kon; Eckner, Kristine; Hattox, Susan; Adams, Julian; Rosenthal, Alan S.; Faanes, Ronald; Eckner, Robert J.; Koup, Richard A.; Sullivan, John L.
Erschienen: American Association for the Advancement of Science (AAAS), 1990
Erschienen in: Science
Sprache: Englisch
DOI: 10.1126/science.1701568
ISSN: 0036-8075; 1095-9203
Entstehung:
Anmerkungen:
Beschreibung: <jats:p> A series of dipyridodiazepinones have been shown to be potent inhibitors of human immunodeficiency virus-1 (HIV-1) reverse transcriptase (RT). One compound, BI-RG-587, had a <jats:italic>K</jats:italic> <jats:sub>i</jats:sub> of 200 nanomolar for inhibition of HIV-1 RT that was noncompetitive with respect to deoxyguanosine triphosphate. BI-RG-587 was specific for HIV-1 RT, having no effect on feline and simian RT or any mammalian DNA polymerases. BI-RG-587 inhibited HIV-1 replication in vitro as demonstrated by in situ hybridization, inhibition of protein p24 production, and the lack of syncytia formation in cultured human T cell lines and freshly isolated human peripheral blood lymphocytes. Cytotoxicity studies of BI-RG-587 on human cells showed a high therapeutic index (>8000) in culture. </jats:p>

Nur in Feld suchen: