Novel HIV-1 integrase inhibitors derived from quinolone antibiotics

Motohide Sato; Takahisa Motomura; Hisateru Aramaki; Takashi Matsuda; Masaki Yamashita; Yoshiharu Ito; Hiroshi Kawakami; Yuji Matsuzaki; Wataru Watanabe; Kazunobu Yamataka; Satoru Ikeda; Eiichi Kodama; Masao Matsuoka; Hisashi Shinkai

doi:10.1021/jm0600139

Novel HIV-1 integrase inhibitors derived from quinolone antibiotics

Motohide Sato, Takahisa Motomura, Hisateru Aramaki, Takashi Matsuda, Masaki Yamashita, Yoshiharu Ito, Hiroshi Kawakami, Yuji Matsuzaki, Wataru Watanabe, Kazunobu Yamataka, Satoru Ikeda, Eiichi Kodama, Masao Matsuoka, Hisashi Shinkai

研究成果: Article › 査読

318 被引用数 (Scopus)

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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.

本文言語	English
ページ（範囲）	1506-1508
ページ数	3
ジャーナル	Journal of Medicinal Chemistry
巻	49
号	5
DOI	https://doi.org/10.1021/jm0600139
出版ステータス	Published - 2006 3月 5
外部発表	はい

ASJC Scopus subject areas

分子医療
創薬

UN SDG

この成果は、次の持続可能な開発目標に貢献しています

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10.1021/jm0600139

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abstract = "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.",

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AU - Sato, Motohide

AU - Motomura, Takahisa

AU - Aramaki, Hisateru

AU - Matsuda, Takashi

AU - Yamashita, Masaki

AU - Ito, Yoshiharu

AU - Kawakami, Hiroshi

AU - Matsuzaki, Yuji

AU - Watanabe, Wataru

AU - Yamataka, Kazunobu

AU - Ikeda, Satoru

AU - Kodama, Eiichi

AU - Matsuoka, Masao

AU - Shinkai, Hisashi

PY - 2006/3/5

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AB - 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.

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Novel HIV-1 integrase inhibitors derived from quinolone antibiotics

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ASJC Scopus subject areas

UN SDG

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