Design and synthesis of anti-HIV agents that inhibit the Pr55Gag membrane localization
| Project/Area Number |
24790124
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| Research Category |
Grant-in-Aid for Young Scientists (B)
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| Allocation Type | Multi-year Fund |
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| Research Field |
Drug development chemistry
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| Research Institution | Kumamoto Health Science University |
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Principal Investigator |
ANRAKU Kensaku 熊本保健科学大学, 保健科学部, 講師 (80389543)
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| Project Period (FY) |
2012-04-01 – 2014-03-31
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| Project Status |
Completed (Fiscal Year 2013)
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| Budget Amount *help |
¥2,730,000 (Direct Cost: ¥2,100,000、Indirect Cost: ¥630,000)
Fiscal Year 2013: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2012: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
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| Keywords | 抗エイズ薬 / Pr55Gag / PI(4,5)P2 / HIV-1 / リン脂質 / ジアシルグリセロール / イノシトールリン酸 / BIACORE |
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| Research Abstract |
Pr55Gag of human immunodeficiency virus, the principal structural component required for virus assembly, is known to bind D-myo-phosphatidylinositol 4,5-bisphosphate (PI(4,5)P2). The N-terminus of Pr55Gag, MA domain, plays a critical role in the binding of Pr55Gag to the plasma membrane. We designed and synthesized PI(2,3,4,5,6)P5 analogs comprising highly phosphorylated inositol and variously modified diacylglycerol to examine the MA-binding property. The binding affinity for MA of Di-C7-PI(2,3,4,5,6)P5 (compound 2) is 70-fold higher than that of PI(4,5)P2 having the similar carbon length, suggesting the possibility of the PIP5 analog to block the Pr55Gag membrane binding by competing with PI(4,5)P2 in the MA-binding.
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Report
(3 results)
Research Products
(31 results)
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[Journal Article] Design and synthesis of lipid-coupled inositol 1,2,3,4,5,6-hexakisphosphate derivatives exhibiting high-affinity binding for HIV-1 MA domain2014
Author(s)
Hiroshi tateishi, Kensaku Anraku, Ryoko Koga, Yoshinari Okamoto, Mikako Fujita, Masami Otsuka
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Journal Title
Org. Biomol. Chem
Volume: 12
Pages: 5006-5022
Related Report
Peer Reviewed
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