Creation and evaluation of RXR partial agonists for the substitutes of steroidal anti-inflammatory agents
Project/Area Number |
22790108
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Research Category |
Grant-in-Aid for Young Scientists (B)
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Allocation Type | Single-year Grants |
Research Field |
Drug development chemistry
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Research Institution | Okayama University |
Principal Investigator |
KAKUTA Hiroki 岡山大学, 大学院・医歯薬学総合研究科, 准教授 (80362961)
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Project Period (FY) |
2010 – 2011
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Project Status |
Completed (Fiscal Year 2011)
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Budget Amount *help |
¥3,900,000 (Direct Cost: ¥3,000,000、Indirect Cost: ¥900,000)
Fiscal Year 2011: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2010: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
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Keywords | ステロイド / 抗炎症 / 核内受容体 / レチノイド / RXR / パーシャルアゴニスト / 皮膚炎モデル / 創薬化学 / レチノイドX受容体 |
Research Abstract |
Effective substitutes of steroidal anti-inflammatory agents for the treatment of allergies and inflammation are required. Thus, we aimed to create new non-steroidal anti-inflammatory agents by targeting retinoid x receptors. By structural development of NEt-3IB(6-[N-ethyl-N-(3-isobutoxy-4-isopropylphenyl) amino] nicotinic acid), a potent RXR agonist, several RXR partial agonists were found. Among them, NEt-4IB(6-[N-ethyl-N-(4-isobutoxy-3-isopropylphenyl) amino] nicotinic acid) was found as a new orally available RXR partial agonist. In addition, this compound showed potent anti-inflammatory activity against the TPA induced skin inflammation without significant side effects.
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Report
(3 results)
Research Products
(20 results)
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[Presentation] リバイバル創薬2011
Author(s)
加来田博貴
Organizer
日本薬学会第131年会
Place of Presentation
ツインメッセ静岡
Year and Date
2011-03-31
Related Report
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