2011 Fiscal Year Final Research Report
Design and synthesis of anti-HIV agents that inhibit the Vif-mediated proteasome degradation of APOBEC3G
| Project/Area Number |
22659024
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| Research Category |
Grant-in-Aid for Challenging Exploratory Research
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| Allocation Type | Single-year Grants |
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| Research Field |
Drug development chemistry
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| Research Institution | Kumamoto University |
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Principal Investigator |
OTSUKA Masami 熊本大学, 大学院・生命科学研究部, 教授 (40126008)
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| Co-Investigator(Kenkyū-buntansha) |
FUJITA Mikako 熊本大学, 薬学部附属創薬研究センター, 准教授 (00322256)
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| Project Period (FY) |
2010 – 2011
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| Keywords | 抗エイズ薬 / Vif / APOBEC3G |
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| Research Abstract |
APOBEC3G is a human antiviral protein that blocks HIV-1 replication. However, the antiviral activity of A3G is overcome by the HIV-1 protein Vif that degrades APOBEC3G. We designed and synthesized artificial compounds MF1, MF2, and MF3 to examine the Vif-inhibitory activity. We found that MF2 and MF1(generated by adding DTT to MF2) increase the expression of APOBEC3G to a level much higher than that observed in the absence of Vif, without affecting the level of Vif expression. Furthermore, MF2, MF3, and MF1(generated by adding DTT to MF2 or MF3) significantly inhibited the MAGI cell infectivity of wild-type HIV-1. These findings may contribute to the development of a novel anti-HIV-1 drug.
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[Journal Article] Design and synthesis of biotinylated inositol 1, 3, 4, 5-tetrakisphosphate targeting Grp1 Pleckstrin Homogy domain2011
Author(s)
Kensaku Anraku, Teruhiko Inoue, Kenji Sugimoto, Kota Kudo, Yoshinari Okamoto, Takashi Morii, Yasuo Mori, Masami Otsuka
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Journal Title
Bioorg. Med. Chem.
Volume: 19
Pages: 6833-6841
Peer Reviewed
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