Conformation analysis and target molecule identification of PF1171 hexapeptides in vivo
| Project/Area Number |
16K07707
|
|---|
| Research Category |
Grant-in-Aid for Scientific Research (C)
|
| Allocation Type | Multi-year Fund |
|---|
| Section | 一般 |
|---|
| Research Field |
Bioorganic chemistry
|
|---|
| Research Institution | Mie University |
|---|
Principal Investigator |
MASUDA Yuichi 三重大学, 生物資源学研究科, 准教授 (90617755)
|
|---|
| Research Collaborator |
AKAGI Ken-ichi
|
|---|
| Project Period (FY) |
2016-04-01 – 2019-03-31
|
| Project Status |
Completed (Fiscal Year 2018)
|
| Budget Amount *help |
¥4,810,000 (Direct Cost: ¥3,700,000、Indirect Cost: ¥1,110,000)
Fiscal Year 2018: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2017: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2016: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
|
|---|
| Keywords | 環状ペプチド / カイコ / 立体配座 / 三次元構造 / 核磁気共鳴 / 安定同位体標識 / 分子プローブ / 有機化学 / NMR / アミノ酸 / 生理活性 / ケミカルバイオロジー |
|---|
| Outline of Final Research Achievements |
PF1171F is a cyclic hexapeptide with paralytic activity against silkworm larvae via oral administration. To elucidate its conformation in pseudo body’s internal environment (aqueous solution and silkworm’s hemolymph), PF1171F whose nitrogen atoms were labeled with 15N was analyzed by 1H-15N 2-dimentional Nuclear Magnetic Resonance (NMR) experiments. The conformation in aqueous solution was found to be quite different from those in organic solvents. On the other hand, no NMR signals were observed in the 2D spectrum of PF1171F in silkworm’s hemolymph. This might be because PF1171F sticks to large biomolecules such as hemocytes.
|
| Academic Significance and Societal Importance of the Research Achievements |
環状ペプチドの立体配座は、標的分子結合や体内動態と密接に関係しているが、実際に活性が発現する生体環境中における立体配座研究は、これまでほとんど行われていなかった。
本研究では、15N標識したPF1171Fを有機合成し、二次元NMRを駆使することにより、疑似生体環境中の立体配座解析を実現した。本解析法は、薬の候補分子として注目されている環状ペプチドの活性発現機構研究に有効である。また、本研究で得られた疑似生体環境中における立体配座の知見は、環状ペプチドの合理的設計につながる。
|
Report
(4 results)
Research Products
(19 results)
-
-
-
-
-
-
[Journal Article] Synthesis of (2S,3R,4R)-3,4-dihydroxyarginine and its inhibitory activity against nitric oxide synthase.2016
Author(s)
Masuda, Y., Maruyama, C., Kawabata, K., Hamano, Y., Doi, T.
-
Journal Title
Tetrahedron
Volume: 72
Issue: 36
Pages: 5602-5611
DOI
Related Report
Peer Reviewed / Open Access / Acknowledgement Compliant
-
-
-
-
-
-
-
-
-
-
-
-
-
