2011 Fiscal Year Final Research Report
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 |
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| Research Field |
Drug development chemistry
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| Research Institution | Okayama University |
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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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| 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 |
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| 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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