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Nucleic Acids Symposium Series 2006 50(1):177-178; doi:10.1093/nass/nrl088
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© 2006 Oxford University Press

Synthesis and properties of G-quartet oligonucleotide-HIV-1 tat peptide conjugate

Tetsuya Kumashiro1, Toru Otake2, Takuya Kawahata2, Masao Akagi1 and Hidehito Urata1

1 Osaka University of Pharmaceutical Sciences, 4-20-1 Nasahara, Takatsuki, Osaka 569-1094, Japan, 2 Osaka Prefectural Institute of Public Health, 1-3-69 Nakamichi, Higashinari-ku, Osaka 537-0025, Japan

Zintevir is a single strand DNA that forms an intramolecular quadruplex structure and shows potent anti-human immunodeficiency virus type 1 (HIV-1) activity. Zintevir was discovered as a potent inhibitor for HIV-1 integrase. Recently, the primary molecular target of Zintevir, however, was shown to be the HIV-1 gp120. In fact, in our previous study, Zintevir was shown to inhibit the only processes of the viral adsorption and the entry into the cell. This result suggests that Zintevir is not able to penetrate through the cell membranes. Therefore, we designed and synthesized the complex of D-17mer with HIV-1 tat peptide that has the cell membrane permeability.


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