| Project/Area Number |
22510233
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Living organism molecular science
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| Research Institution | The University of Tokushima |
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Principal Investigator |
KASHIWADA Yoshiki 徳島大学, 大学院・ヘルスバイオサイエンス研究部, 准教授 (30169429)
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| Co-Investigator(Kenkyū-buntansha) |
TAKAISHI Yoshihisa 徳島大学, 大学院・ヘルスバイオサイエンス研究部, 教授 (60035558)
|
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| Research Collaborator |
LEE Kuo-hsiung ノースカロライナ大学チャペルヒル校, エシェルマン薬学部, 教授
QIAN Keduo ノースカロライナ大学チャペルヒル校, エシェルマン薬学部, 助教
CHEN Chin-ho デューク大学, 医学部, 教授
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| Project Period (FY) |
2010 – 2012
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| Project Status |
Completed (Fiscal Year 2012)
|
| Budget Amount *help |
¥4,550,000 (Direct Cost: ¥3,500,000、Indirect Cost: ¥1,050,000)
Fiscal Year 2012: ¥780,000 (Direct Cost: ¥600,000、Indirect Cost: ¥180,000)
Fiscal Year 2011: ¥780,000 (Direct Cost: ¥600,000、Indirect Cost: ¥180,000)
Fiscal Year 2010: ¥2,990,000 (Direct Cost: ¥2,300,000、Indirect Cost: ¥690,000)
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| Keywords | AIDS / 薬剤耐性 / トリテルペン / ベツリン |
|---|
| Research Abstract |
Based on our finding of a first-in-class drug candidate as a viral maturation inhibitor, bevirimat [3-O-(3',3'-dimethylsuccinyl)-betulinic acid], and potent anti-HIV active 3-O-acyl-(dihidro)betulin derivatives (e.g. 3-O-glutarydihydrobetulin and 3,28-di-O-dimethylsuccinylbetulin), a series of conjugates of 3,28-di-O-acylbetulin derivatives and HIV-reverse transcriptase inhibitor, AZT, as well as conjugates of 28-leucinyl-bevirimat and acyl-betulin derivatives were prepared and evaluated their anti-HIV activity. Several derivatives showed more potent anti-HIV activity than bevirimat.
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