Peptide HIV-1 Integrase Inhibitors from HIV-1 Gene Products
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- 作者：Shintaro Suzuki ; Emiko Urano ; Chie Hashimoto ; Hiroshi Tsutsumi ; Toru Nakahara ; Tomohiro Tanaka ; Yuta Nakanishi ; Kasthuraiah Maddali ; Yan Han ; Makiko Hamatake ; Kosuke Miyauchi ; Yves Pommier ; John A. Be
- 刊名：Journal of Medicinal Chemistry
- 出版年：2010
- 出版时间：July 22, 2010
- 年：2010
- 卷：53
- 期：14
- 页码：5356-5360
- 全文大小：794K
- 年卷期：v.53,no.14(July 22, 2010)
- ISSN：1520-4804
文摘
Anti-HIV peptides with inhibitory activity against HIV-1 integrase (IN) have been found in overlapping peptide libraries derived from HIV-1 gene products. In a strand transfer assay using IN, inhibitory active peptides with certain sequential motifs related to Vpr- and Env-derived peptides were found. The addition of an octa-arginyl group to the inhibitory peptides caused a remarkable inhibition of the strand transfer and 3′-end-processing reactions catalyzed by IN and significant inhibition against HIV replication.