1. Quinoxapeptins: novel chromodepsipeptide inhibitors of HIV-1 and HIV-2 reverse transcriptase. I. The producing organism and biological activity.
- Author
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Lingham RB, Hsu AH, O'Brien JA, Sigmund JM, Sanchez M, Gagliardi MM, Heimbuch BK, Genilloud O, Martin I, Diez MT, Hirsch CF, Zink DL, Liesch JM, Koch GE, Gartner SE, Garrity GM, Tsou NN, and Salituro GM
- Subjects
- Actinomycetales classification, Actinomycetales metabolism, HIV Reverse Transcriptase, HIV-1 genetics, Humans, Hydroxyquinolines chemistry, Hydroxyquinolines pharmacology, In Vitro Techniques, Kinetics, Molecular Structure, Mutation, Nucleic Acid Synthesis Inhibitors, Peptides, Cyclic chemistry, Quinoxalines chemistry, RNA-Directed DNA Polymerase genetics, Reverse Transcriptase Inhibitors chemistry, HIV-1 enzymology, HIV-2 enzymology, Peptides, Cyclic metabolism, Peptides, Cyclic pharmacology, Quinoxalines metabolism, Quinoxalines pharmacology, RNA-Directed DNA Polymerase metabolism, Reverse Transcriptase Inhibitors metabolism, Reverse Transcriptase Inhibitors pharmacology
- Abstract
Quinoxapeptin A and B are novel chromodepsipeptides which were isolated from a nocardioform actinomycete with indeterminant morphology. Quinoxapeptins A and B are potent inhibitors of HIV-1 and HIV-2 reverse transcriptase and almost equally active against two single mutants forms as well as a double mutant form of HIV-1 reverse transcriptase. Quinoxapeptin A and B are specific inhibitors of HIV-1 and HIV-2 reverse transcriptase because they did not inhibit human DNA polymerase alpha, beta, gamma and delta. Quinoxapeptin A and B are structurally similar to luzopeptin A which was also active against HIV-1 and HIV-2 reverse transcriptase.
- Published
- 1996
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