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Peptide HIV-1 Integrase Inhibitors from HIV-1 Gene Products

  1. Author:
    Suzuki, S.
    Urano, E.
    Hashimoto, C.
    Tsutsumi, H.
    Nakahara, T.
    Tanaka, T.
    Nakanishi, Y.
    Maddali, K.
    Han, Y.
    Hamatake, M.
    Miyauchi, K.
    Pommie, Y.
    Beutler, J. A.
    Sugiura, W.
    Fuji, H.
    Hoshino, T.
    Itotani, K.
    Nomura, W.
    Narumi, T.
    Yamamoto, N.
    Komano, J. A.
    Tamamura, H.

  2. Author Address

    [Suzuki, Shintaro; Hashimoto, Chic; Tsutsumi, Hiroshi; Nakahara, Toru; Tanaka, Tomohiro; Nakanishi, Yuta; Itotani, Kyoko; Nomura, Wataru; Narumi, Tetsuo; Tamamura, Hirokazu] Tokyo Med & Dent Univ, Inst Biomat & Bioengn, Dept Med Chem, Chiyoda Ku, Tokyo 1010062, Japan. [Urano, Emiko; Han, Yan; Hamatake, Makiko; Miyauchi, Kosuke; Sugiura, Wataru; Yamamoto, Naoki; Komano, Jun A.] Natl Inst Infect Dis, AIDS Res Ctr, Shinjuku Ku, Tokyo 1628640, Japan. [Maddali, Kasthuraiah; Pommie, Yves] NCI, Mol Pharmacol Lab, Ctr Canc Res, NIH, Bethesda, MD 20892 USA. [Fuji, Hideyoshi; Hoshino, Tyuji] Chiba Univ, Grad Sch Pharmaceut Sci, Dept Phys Chem, Inage Ku, Chiba 2638522, Japan. [Beutler, John A.] NCI, Mol Targets Lab, Ctr Canc Res, NIH, Frederick, MD 21702 USA.;Tamamura, H, Tokyo Med & Dent Univ, Inst Biomat & Bioengn, Dept Med Chem, Chiyoda Ku, 2-3-10 Kandasurugadai, Tokyo 1010062, Japan.;tarnamura.mr@tmd.ac.jp
    1. Year: 2010
    2. Date: Jul
  2. Journal: Journal of Medicinal Chemistry
    1. 53
    2. 14
    3. Pages: 5356-5360
  4. Type of Article: Article
  5. ISSN: 0022-2623
  1. Abstract:

    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.

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External Sources

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  2. DOI: 10.1021/jm1003528
  3. View record in Web of Science®
  4. WOS: 000279787200026

Library Notes

  1. Fiscal Year: FY2009-2010
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