Development of ligand screening using chemical array and membrane protein-expressed cells
| Project/Area Number |
18K05366
|
|---|
| Research Category |
Grant-in-Aid for Scientific Research (C)
|
| Allocation Type | Multi-year Fund |
|---|
| Section | 一般 |
|---|
| Review Section |
Basic Section 37030:Chemical biology-related
|
|---|
| Research Institution | Institute of Physical and Chemical Research |
|---|
Principal Investigator |
Kondoh Yasumitsu 国立研究開発法人理化学研究所, 環境資源科学研究センター, 専任研究員 (80333342)
|
|---|
| Project Period (FY) |
2018-04-01 – 2021-03-31
|
| Project Status |
Completed (Fiscal Year 2020)
|
| Budget Amount *help |
¥4,550,000 (Direct Cost: ¥3,500,000、Indirect Cost: ¥1,050,000)
Fiscal Year 2020: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2019: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2018: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
|
|---|
| Keywords | ケミカルアレイ / 膜結合蛋白質 / リガンド / ハイスループットスクリーニング / 膜受容体 / 細胞 |
|---|
| Outline of Final Research Achievements |
Chemical array was developed as a high-throughput screening technique for compounds that bind to target proteins by immobilizing compounds on glass slides. In order to establish the basic processing conditions for cell binding assays using membrane-bound proteins as targets, I examined various conditions in the chemical array and SPR imaging methods. In parallel, I also established screening conditions using intracellular calcium ion assay, and searched for natural products that enhance the response of receptors, and found that certain plant extracts had an enhancing effect.
|
| Academic Significance and Societal Importance of the Research Achievements |
GPCRのリガンド探索系としては、RIラベルされたリガンドを用いた結合アッセイや、細胞内のcAMPやCa2+濃度などシグナル伝達の下流に着目した活性測定の系が知られているが、いずれも高価な機器や試薬が必要であり、また、リガンド探索の際にライブラリー化合物を全てRIラベルすることは不可能である。これらの手法に代わるハイスループットなリガンド探索系が必要である。また、受容体の応答を増強する植物抽出物については、今後、活性本体の構造を決定することにより、その受容体で初めて見出した天然の応答増強物質として特許出願、論文発表をすることができる。
|
Report
(4 results)
Research Products
(37 results)
-
[Journal Article] Discovery of small-molecule modulator of heterotrimeric Gi-protein by integrated phenotypic profiling and chemical proteomics2020
Author(s)
16)Kawamura, T., Futamura, Y., Shang, E., Muroi, M., Janning, P., Ueno, M., Wilke, J., Takeda, S., Kondoh, Y., Ziegler, S., Watanabe, N., Waldmann, H., Osada, H.
-
Journal Title
Biosci. Biotechnol. Biochem.
Volume: 84
Issue: 12
Pages: 2484-2490
DOI
Related Report
Peer Reviewed / Int'l Joint Research
-
-
-
[Journal Article] Miclxin, a novel MIC60 inhibitor, induces apoptosis via mitochondrial stress in β-catenin mutant tumor cells.2020
Author(s)
20)Ikeda, H., Muroi, M., Kondoh, Y., Ishikawa, S., Kakeya, H., Osada, H., Imoto, M.
-
Journal Title
ACS Chem. Biol.
Volume: 15
Issue: 8
Pages: 2195-2204
DOI
Related Report
Peer Reviewed / Open Access
-
-
-
-
-
-
-
-
-
[Journal Article] Chemical array system, a platform to identify novel hepatitis B virus entry inhibitors targeting sodium taurocholate cotransporting polypeptide2018
Author(s)
Kaneko M, Futamura Y, Tsukuda S, Kondoh Y, Sekine T, Hirano H, Fukano K, Ohashi H, Saso W, Morishita R, Matsunaga S, Kawai F, Ryo A, Park S-Y, Suzuki R, Aizaki H, Ohtani N, Sureau C, Wakita T, Osada H, Watashi K
-
Journal Title
Scientific Reports
Volume: 8
Issue: 1
Pages: 2769-2769
DOI
Related Report
Peer Reviewed / Open Access / Int'l Joint Research
-
-
-
-
-
-
-
-
-
[Presentation] Identification and characterization of small-molecular compounds that inhibit salicylic acid-mediated signaling pathway in Arabidopsis2019
Author(s)
Nobuaki Ishihama, Yoshiteru Noutoshi, Seung-won Choi, Ivana Saska, Shuta Asai, Kaori Takizawa, Yasumitsu Kondoh, Yuko Nomura, Hirofumi Nakagami, Hiroyuki Osada, Ken Shirasu
Organizer
IS-MPMI XVIII Congress
Related Report
Int'l Joint Research
-
-
-
-
-
-
-
-
-
-
-
[Presentation] 植物免疫阻害剤を用いた植物免疫応答制御因子の探索2018
Author(s)
石濱伸明, 能年義輝, 崔 勝媛, Ivana Saska, 浅井秀太, 瀧澤 香, 野村有子, 中神弘史, 近藤恭光, 長田裕之, 白須 賢
Organizer
平成３0年度日本植物病理学会関東部会
Related Report
-
-
-
-
