| Project/Area Number |
19590112
|
|---|
| Research Category |
Grant-in-Aid for Scientific Research (C)
|
| Allocation Type | Single-year Grants |
|---|
| Section | 一般 |
|---|
| Research Field |
Drug development chemistry
|
|---|
| Research Institution | Kobe Gakuin University |
|---|
Principal Investigator |
TSUDA Yuko Kobe Gakuin University, 薬学部, 教授 (10098478)
|
|---|
| Co-Investigator(Kenkyū-buntansha) |
YUKOI Toshio 神戸学院大学, 薬学部, 教授 (50122255)
OKADA Yoshio 神戸学院大学, 食品薬品総合科学研究科, 教授 (60068236)
|
|---|
| Project Period (FY) |
2007 – 2009
|
| Project Status |
Completed (Fiscal Year 2009)
|
| Budget Amount *help |
¥3,640,000 (Direct Cost: ¥2,800,000、Indirect Cost: ¥840,000)
Fiscal Year 2009: ¥650,000 (Direct Cost: ¥500,000、Indirect Cost: ¥150,000)
Fiscal Year 2008: ¥780,000 (Direct Cost: ¥600,000、Indirect Cost: ¥180,000)
Fiscal Year 2007: ¥2,210,000 (Direct Cost: ¥1,700,000、Indirect Cost: ¥510,000)
|
|---|
| Keywords | エンドモルフィン / オピオイド受容体 / 酵素安定性 / コンフォメーション解析 / 分子設計 |
|---|
| Research Abstract |
We synthesized the [2',6'-Dimethyl-L-tyrosine1]endomorphin 2 (EM-2) analogues containing proline mimics. Among them, [Dmt1, L-Pip2]EM-2 was potent and selective mu-agonist, while [Dmt1, Aze2]EM-2 was mu/delta-agoinist. [Dmt1, Aze2]EM-2 had a cis/trans equilibrium of ratio 2:1 and cis conformer was predominant in both DMSO or H2 O. The cis [Dmt1, Aze2]EM-2conformers took folded form. The further conformational analyses of the analogues are in progress.
|
