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EM2487, a novel anti-HIV-1 antibiotic, produced by Streptomyces sp. Mer-2487: taxonomy, fermentation, biological properties, isolation and structure elucidation.

作者信息

Takeuchi H, Asai N, Tanabe K, Kozaki T, Fujita M, Sakai T, Okuda A, Naruse N, Yamamoto S, Sameshima T, Heida N, Dobashi K, Baba M

机构信息

Tsukuba Research Laboratories, Eisai Co., Ltd., Ibaraki, Japan.

出版信息

J Antibiot (Tokyo). 1999 Nov;52(11):971-82. doi: 10.7164/antibiotics.52.971.

DOI:10.7164/antibiotics.52.971
PMID:10656569
Abstract

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.

摘要

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