2013 Fiscal Year Final Research Report
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 |
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| Section | 一般 |
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| Research Field |
Chemical biology
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| Research Institution | The Institute of Physical and Chemical Research |
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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)
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| Project Period (FY) |
2011 – 2013
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| 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 |
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| 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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[Journal Article] A small compound targeting TACC3 revealed its spatiotemporally different contributions to the spindle assembly in cancer cells2014
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
DOI
Peer Reviewed
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[Journal Article] Spectomycin B1 as a novel SUMOylation inhibitor that directly binds to SUMO E22013
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 K, Yoshida M, Ito A
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Journal Title
ACS Chem. Biol.
Volume: 8
Pages: 2635-2642
DOI
Peer Reviewed
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[Journal Article] Identification and characterization of an inhibitor of trichothecene 3-O-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
Biosci. Biotechnol. Biochem.
Volume: 77
Pages: 1958-1960
DOI
Peer Reviewed
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[Journal Article] Boronic acid inhibitors of acyl protein thioesterase 1 and 22013
Author(s)
Zimmermann TJ, Burger M, Tashiro E, Kondoh Y, Martinez NE, Gormer K, Rosin-steiner S, Shimizu T, Ozaki S, Mikoshiba K, Watanabe N, Hall D, Vetter IR, Osada H, Hedberg C, Waldmann H
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Journal Title
Chem Bio Chem
Volume: 14
Pages: 115-122
DOI
Peer Reviewed
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