Quinoxapeptins: novel chromodepsipeptide inhibitors of HIV-1 and HIV-2 reverse transcriptase. I. The producing organism and biological activity.
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.
Lingham
R B
RB
Merck Research Laboratories, Rahway, NJ 07065, U.S.A.
Hsu
A H
AH
O'Brien
J A
JA
Sigmund
J M
JM
Sanchez
M
M
Gagliardi
M M
MM
Heimbuch
B K
BK
Genilloud
O
O
Martin
I
I
Diez
M T
MT
Hirsch
C F
CF
Zink
D L
DL
Liesch
J M
JM
Koch
G E
GE
Gartner
S E
SE
Garrity
G M
GM
Tsou
N N
NN
Salituro
G M
GM
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
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