EM2487, a novel anti-HIV-1 antibiotic, produced by Streptomyces sp. Mer-2487: taxonomy, fermentation, biological properties, isolation and structure elucidation.
For the purpose of discovering novel agents that inhibit HIV-1 replication at the transcriptional level, we have established cell lines reflecting the HIV-1 long terminal repeat-driven gene expression. Using these cell lines, we have screened approximately 10,000 microorganism products and found that the culture supernatant of Streptomyces sp. Mer-2487 suppresses the HIV-1 Tat-induced gene expression without affecting the basal or tumor necrosis factor-alpha-induced transcription. The purified active component has a unique structure, as shown in Fig. 1. This compound has an inhibitory effect on HIV-1 replication in chronically infected cells as well as acutely infected cells, suggesting that the inhibition occurs at a postintegration step of HIV-1 proviral DNA in the HIV-1 replication cycle.
Takeuchi
H
H
Tsukuba Research Laboratories, Eisai Co., Ltd., Ibaraki, Japan.
Asai
N
N
Tanabe
K
K
Kozaki
T
T
Fujita
M
M
Sakai
T
T
Okuda
A
A
Naruse
N
N
Yamamoto
S
S
Sameshima
T
T
Heida
N
N
Dobashi
K
K
Baba
M
M
D000900:Anti-Bacterial Agents / Q000302:isolation & purification*; D019380:Anti-HIV Agents / Q000302:isolation & purification*; D002460:Cell Line; D005285:Fermentation; D015497:HIV-1 / Q000187:drug effects* / Q000235:genetics / Q000502:physiology; D006801:Humans; D010755:Organophosphates / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D013302:Streptomyces / Q000145:classification* / Q000378:metabolism; D014529:Uridine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D014779:Virus Replication / Q000187:drug effects
D000900:Anti-Bacterial Agents; D019380:Anti-HIV Agents; C400941:EM 2487; D010755:Organophosphates; D014529:Uridine