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.