抜粋
The viral enzyme integrase is essential for the replication of human immunodeficiency virus type 1 (HIV-1) and represents a remaining target for antiretroviral drugs. Here, we describe the modification of a quinolone antibiotic to produce the novel integrase inhibitor JTK-303 (GS 9137) that blocks strand transfer by the viral enzyme. It shares the core structure of quinolone antibiotics, exhibits an IC50 of 7.2 nM in the strand transfer assay, and shows an EC50 of 0.9 nM in an acute HIV-1 infection assay.
| 元の言語 | English |
|---|---|
| ページ（範囲） | 1506-1508 |
| ページ数 | 3 |
| ジャーナル | Journal of Medicinal Chemistry |
| 巻 | 49 |
| 発行部数 | 5 |
| DOI | |
| 出版物ステータス | Published - 2006 3 5 |
| 外部発表 | Yes |
ASJC Scopus subject areas
- Molecular Medicine
- Drug Discovery
フィンガープリント Novel HIV-1 integrase inhibitors derived from quinolone antibiotics' の研究トピックを掘り下げます。これらはともに一意のフィンガープリントを構成します。
これを引用
Sato, M., Motomura, T., Aramaki, H., Matsuda, T., Yamashita, M., Ito, Y., Kawakami, H., Matsuzaki, Y., Watanabe, W., Yamataka, K., Ikeda, S., Kodama, E., Matsuoka, M., & Shinkai, H. (2006). Novel HIV-1 integrase inhibitors derived from quinolone antibiotics. Journal of Medicinal Chemistry, 49(5), 1506-1508. https://doi.org/10.1021/jm0600139