Screening of inhibitors for hedgehog signaling pathway by using chemical array
Project/Area Number |
23510287
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Research Category |
Grant-in-Aid for Scientific Research (C)
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Allocation Type | Multi-year Fund |
Section | 一般 |
Research Field |
Chemical biology
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Research Institution | The Institute of Physical and Chemical Research |
Principal Investigator |
KONDOH Yasumitsu 独立行政法人理化学研究所, 長田抗生物質研究室, 専任研究員 (80333342)
|
Project Period (FY) |
2011 – 2013
|
Project Status |
Completed (Fiscal Year 2013)
|
Budget Amount *help |
¥5,460,000 (Direct Cost: ¥4,200,000、Indirect Cost: ¥1,260,000)
Fiscal Year 2013: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2012: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2011: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
|
Keywords | 医薬品探索 / 生理活性 / シグナル伝達 / マイクロアレイ / ケミカルアレイ / ソニックヘッジホッグ / Shh / SPRイメージング |
Research Abstract |
The purpose of this research was investigation of the inhibitor that binds directly to sonic hedgehog (Shh) and inhibits Shh signaling pathway by chemical array screening. By chemical array screening using ShhN protein, 322 candidates among about 30 thousands of library compounds were identified. The interaction of ShhN and candidates were measured by surface plasmon resonance (SPR) imaging and 9 compounds had strong binding activities to ShhN with Kd of 6–60 nM. It is known that mouse undifferentiated mesenchymal cell C3H10T1/2 differentiates into osteoblast by treatment of ShhN. Among 9 compounds, 5 compounds inhibited the differentiation-inducing activity of ShhN dose-dependently.
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Report
(4 results)
Research Products
(59 results)
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[Journal Article] A small compound targeting TACC3 revealed its different spatiotemporal contributions for spindle assembly in cancer cells.2014
Author(s)
Yao R, Kondoh Y, Natsume Y, Yamanaka H, Inoue M, Toki H, Takagi R, Shimizu T, Yamori T, Osada H, Noda T
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Journal Title
Oncogene
Volume: in press
Issue: 33
Pages: 1-11
DOI
Related Report
Peer Reviewed / Open Access
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[Journal Article] Spectomycin B1 as a novel SUMOylation inhibitor that directly binds to SUMO E2.2013
Author(s)
Hirohama M, Kumar A, Fukuda I, Matsuoka S, Igarashi Y, Saitoh H, Takagi M, Shin-ya K, Honda K, Kondoh Y, Saito T, Nakao Y, Osada H, Zhang KY, Yoshida M, Ito A
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Journal Title
ACS Chem Biol
Volume: 8
Issue: 12
Pages: 2635-2642
DOI
Related Report
Peer Reviewed
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[Journal Article] Identification and Characterization of an Inhibitor of Trichothecene 3-<i>O</i>-Acetyltransferase, TRI101, by the Chemical Array Approach2013
Author(s)
Nakajima Y, Kawamura T, Maeda K, Ichikawa H, Motoyama T, Kondoh Y, Saito T, Kobayashi T, Yoshida M, Osada H, Kimura M
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Journal Title
Bioscience, Biotechnology, and Biochemistry
Volume: 77
Issue: 9
Pages: 1958-1960
DOI
NAID
ISSN
0916-8451, 1347-6947
Related Report
Peer Reviewed
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[Journal Article] Boronic acid inhibitors of acyl protein thioesterase 1 and 22013
Author(s)
Zimmermann, T.J., Burger, M., Tashiro, E., Kondoh, Y., Martinez, N.E., Gormer, K., Rosin-steiner, S., Shimizu, T. Ozaki, S., Mikoshiba, K., Watanabe, N., Hall, D., Vetter, I.R., Osada, H., Hedberg, C., & Waldmann, H
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Journal Title
ChemBioChem
Volume: 14
Issue: 1
Pages: 115-122
DOI
Related Report
Peer Reviewed
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[Journal Article] Xanthohumol impairs autophagosome maturation through direct inhibition of valosin-containing protein2012
Author(s)
Sasazawa, Y., Kanagaki, S., Tashiro, E., Nogawa, T., Muroi, M., Kondoh, Y., Osada, H., Imoto, M
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Journal Title
ACS Chemical Biology
Volume: (in press)
Issue: 5
Pages: 892-900
DOI
Related Report
Peer Reviewed
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[Journal Article] Crystal structure of the predicted phospholipase LYPLAL1 reveals unexpected functional plasticity despite close relationship to acyl protein thioesterases2012
Author(s)
Burger, M., Zimmermann, T. J., Kondoh, Y., Stege, P., Watanabe, N., Osada, H., Waldmann, H. & Vetter, I. R
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Journal Title
Journal of Lipid Research
Volume: 53
Issue: 1
Pages: 43-50
DOI
Related Report
Peer Reviewed
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[Presentation] Screening of LAP binding inhibitors of TGF-β activation reaction.2013
Author(s)
Yamamoto Y, Sakata K, Honda K, Kondoh Y, Saito T, Osada H, Muto Y, Hirano T, Hara M, Shirouzu M, Kojima S
Organizer
RIKEN-MAXPLANCK JOINTRESEARCH CENTER 2nd Symposium
Place of Presentation
RIKEN, Wako, Saitama
Related Report
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[Presentation] Structural and biochemical investigation of acyl protein thioesterase, a Ras-regulating protein.2013
Author(s)
Porfetye AT, Zimmermann TJ, Burger M, Tashiro E, Stege P, Kondoh Y, Watanabe N, Hedberg C, Osada H, Waldmann H, Vetter IR
Organizer
RIKEN-MAXPLANCK JOINTRESEARCH CENTER 2nd Symposium
Place of Presentation
RIKEN, Wako, Saitama
Related Report
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