title: Quinoxapeptins: novel chromodepsipeptide inhibitors of HIV-1 and HIV-2 reverse transcriptase. I. The producing organism and biological activity.
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.
authors.affiliation: Merck Research Laboratories, Rahway, NJ 07065, U.S.A.
authors.forename: R B
authors.initials: RB
authors.lastname: Lingham
authors.forename: A H
authors.initials: AH
authors.lastname: Hsu
authors.forename: J A
authors.initials: JA
authors.lastname: O'Brien
authors.forename: J M
authors.initials: JM
authors.lastname: Sigmund
authors.forename: M
authors.initials: M
authors.lastname: Sanchez
authors.forename: M M
authors.initials: MM
authors.lastname: Gagliardi
authors.forename: B K
authors.initials: BK
authors.lastname: Heimbuch
authors.forename: O
authors.initials: O
authors.lastname: Genilloud
authors.forename: I
authors.initials: I
authors.lastname: Martin
authors.forename: M T
authors.initials: MT
authors.lastname: Diez
authors.forename: C F
authors.initials: CF
authors.lastname: Hirsch
authors.forename: D L
authors.initials: DL
authors.lastname: Zink
authors.forename: J M
authors.initials: JM
authors.lastname: Liesch
authors.forename: G E
authors.initials: GE
authors.lastname: Koch
authors.forename: S E
authors.initials: SE
authors.lastname: Gartner
authors.forename: G M
authors.initials: GM
authors.lastname: Garrity
authors.forename: N N
authors.initials: NN
authors.lastname: Tsou
authors.forename: G M
authors.initials: GM
authors.lastname: Salituro
mesh_terms: D000192:Actinomycetales / Q000145:classification / Q000378:metabolism; D054303:HIV Reverse Transcriptase; D015497:HIV-1 / Q000201:enzymology* / Q000235:genetics; D015498:HIV-2 / Q000201:enzymology*; D006801:Humans; D006912:Hydroxyquinolines / Q000737:chemistry / Q000494:pharmacology; D066298:In Vitro Techniques; D007700:Kinetics; D015394:Molecular Structure; D009154:Mutation; D019384:Nucleic Acid Synthesis Inhibitors; D010456:Peptides, Cyclic / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D011810:Quinoxalines / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D012194:RNA-Directed DNA Polymerase / Q000235:genetics / Q000378:metabolism*; D018894:Reverse Transcriptase Inhibitors / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D047630:Depsipeptides
chemical_list: D054303:HIV Reverse Transcriptase; D006912:Hydroxyquinolines; D019384:Nucleic Acid Synthesis Inhibitors; D010456:Peptides, Cyclic; D011810:Quinoxalines; D012194:RNA-Directed DNA Polymerase; D018894:Reverse Transcriptase Inhibitors; C099304:quinoxapeptin A; C099305:quinoxapeptin B; C029831:luzopeptins; D047630:Depsipeptides; C072416:reverse transcriptase, Human immunodeficiency virus 2