• Search Research Projects
  • Search Researchers
  • How to Use
  1. Back to project page

2009 Fiscal Year Final Research Report

Chemical proteomics to reveal interaction between chemicals and proteins at angstrom level

Research Project

  • PDF
Project/Area Number 17GS0221
Research Category

Grant-in-Aid for Creative Scientific Research

Allocation TypeSingle-year Grants
Research InstitutionThe Institute of Physical and Chemical Research

Principal Investigator

OSADA Hiroyuki  The Institute of Physical and Chemical Research, ケミカルバイオロジー研究基盤施設, 施設長 (80160836)

Co-Investigator(Kenkyū-buntansha) SAITO Akiko  独立行政法人理化学研究所, 化学情報・化合物創製チーム, 協力研究員 (40415162)
SHIMIZU Takeshi  独立行政法人理化学研究所, 化学情報・化合物創製チーム, 特別嘱託職員 (80087569)
SHIRO Yoshitsugu  独立行政法人理化学研究所, 城生体金属科学研究室, 主任研究員 (70183051)
KAKEYA Hideaki  京都大学, 薬学研究科, 教授 (00270596)
USUI Takeo  筑波大学, 生命環境科学研究科, 准教授 (60281648)
HAYASHI Yujiro  東京理科大学, 工学部, 教授 (00198863)
KOJIMA Soichi  独立行政法人理化学研究所, 分子リガンド生物研究チーム, チームリーダー (10202061)
Co-Investigator(Renkei-kenkyūsha) YOSHIDA Minoru  独立行政法人理化学研究所, 吉田化学遺伝学研究室, 主任研究員 (80191617)
TAKAHASHI Shunji  独立行政法人理化学研究所, 化学情報・化合物創製チーム, 専任研究員 (30311608)
OKUMURA Hideo  独立行政法人理化学研究所, 化合物ライブラリー評価研究チーム, 基礎科学特別研究員 (90377903)
Project Period (FY) 2005 – 2009
Keywords化学生物学 / 構造生物学 / バイオプローブ / 蛋白質 / 相互作用
Research Abstract

Chemical biology is the interdisciplinary research area combining organic chemistry and molecular biology. In this study, we fused the research of both chemical biology and structural biology to construct a novel academic framework. We have developed chemical array system which can efficiently detect an interaction between bioactive small molecules (ligands) and their target proteins (receptors), and rapidly analyze the structure-activity relationship. Moreover, the interaction between a ligand and its receptor was successfully confirmed by co-crystallography. Our research outline is expected to contribute to drug discovery and progress of bioscience.

  • Research Products

    (65 results)

All 2010 2009 2008 2007 2006 2005 Other

All Journal Article (61 results) (of which Peer Reviewed: 61 results) Presentation (2 results) Book (1 results) Patent(Industrial Property Rights) (1 results)

  • [Journal Article] Biochemical characterization of a novel indole prenyltransferase from Streptomyces sp. SN-593.2010

    • Author(s)
      Takahashi, S. (8名中1番目), Osada, H. (8名中8番目)
    • Journal Title

      J. Bacteriol. 192

      Pages: 2839-2851

    • Peer Reviewed
  • [Journal Article] Garbled messages and corrupted translations.2010

    • Author(s)
      Usui, T. (4名中2番目), Yoshida, M. (4名中4番目)
    • Journal Title

      Nat. Chem. Biol. 6

      Pages: 189-198

    • Peer Reviewed
  • [Journal Article] Syntheses and biological evaluation of irciniastatin A and the C1-C2 alkyne analogue.2010

    • Author(s)
      Usui, T. (8名中6番目)
    • Journal Title

      Org. Lett. 12

      Pages: 1040-1043

    • Peer Reviewed
  • [Journal Article] Syntheses of fumagillin and ovalicin.2010

    • Author(s)
      Hayashi, Y. (2名中2番目)
    • Journal Title

      Eur. J. Chem. 16

      Pages: 3884-3901

    • Peer Reviewed
  • [Journal Article] Functional characterization of TtnD and TtnF unveiling new insights into tautomycetin biosynthesis.2010

    • Author(s)
      Osada, H. (11名中10番目)
    • Journal Title

      J. Am. Chem. Soc. 132

      Pages: 6663-6671

    • Peer Reviewed
  • [Journal Article] Discovery of novel antiviral agents directed against the influenza A virus nucleoprotein using photo-cross-linked chemical arrays.2010

    • Author(s)
      Osada, H. (9名中8番目)
    • Journal Title

      Biochem. Biophys. Res. Commun. 394

      Pages: 721-727

    • Peer Reviewed
  • [Journal Article] A novel yeast cell-based screen identifies flavone as a tankyrase inhibitor.2010

    • Author(s)
      Osada, H. (11名中9番目), Yoshida, M. (11名中11番目)
    • Journal Title

      Biochem. Biophys. Res. Commun. 394

      Pages: 569-573

    • Peer Reviewed
  • [Journal Article] In vitro reconstruction of tetronate RK-682 biosynthesis.2010

    • Author(s)
      Osada, H. (7名中6番目)
    • Journal Title

      Nat. Chem. Biol. 6

      Pages: 99-101

    • Peer Reviewed
  • [Journal Article] Cleavable linker for photo-cross-linked small-molecule affinity matrix.2010

    • Author(s)
      Osada, H. (8名中7番目)
    • Journal Title

      Bioconjugate Chem. 21

      Pages: 182-186

    • Peer Reviewed
  • [Journal Article] Genome-wide maps of mononucleosomes and dinucleosomes containing hyper-acetylated histones of Aspergillus fumigatus.2010

    • Author(s)
      Osada, H. (6名中6番目)
    • Journal Title

      PLoS One 5

      Pages: 9916

    • Peer Reviewed
  • [Journal Article] The cytotoxic macrolide FD-891 induces caspase-8-dependent mitochondrial release of cytochrome c and subsequent apoptosis in human leukemia Jurkat cells.2009

    • Author(s)
      Usui, T. (7名中5番目)
    • Journal Title

      J. Antibiot. 62

      Pages: 507-512

    • Peer Reviewed
  • [Journal Article] Identification of cytochrome P450s required for fumitremorgin biosynthesis in Aspergillus fumigatus.2009

    • Author(s)
      Kakeya, H. (10名中5番目), Usui, T. (10名中7番目), Takahashi, S. (10名中8番目), Osada, H. (10名中10番目)
    • Journal Title

      Chembiochem 23

      Pages: 920-928

    • Peer Reviewed
  • [Journal Article] A cell-based screening to detect inhibitors of BRAF signaling pathway.2009

    • Author(s)
      Usui, T. (8名中7番目), Osada, H. (8名中8番目)
    • Journal Title

      J. Antibiot. 62

      Pages: 105-107

    • Peer Reviewed
  • [Journal Article] Osteoclast-targeting small molecules for the treatment of neoplastic bone metastases.2009

    • Author(s)
      Osada, H. (2名中2番目)
    • Journal Title

      Cancer Sci. 100

      Pages: 1999-2005

    • Peer Reviewed
  • [Journal Article] Structure-affinity relationship study of bleomycins and Shble protein by use of a chemical array.2009

    • Author(s)
      Okumura, H. (8名中2番目), Osada, H. (8名中10番目)
    • Journal Title

      Chembiochem 10

      Pages: 845-852

    • Peer Reviewed
  • [Journal Article] A p38 mitogen-activated protein kinase inhibitor screening method using growth recovery of Escherichia coli as an index.2009

    • Author(s)
      Saito, A. (4名中2番目), Osada, H. (4名中4番目)
    • Journal Title

      Anal. Biochem. 388

      Pages: 128-133

    • Peer Reviewed
  • [Journal Article] Involvement of cyclophilin D in mitochondrial permeability transition induction in intact cells.2009

    • Author(s)
      Osada, H. (5名中4番目)
    • Journal Title

      Arch. Biochem. Biophys. 481

      Pages: 59-64

    • Peer Reviewed
  • [Journal Article] Genome-wide maps of mono-and di-nucleosomes of Aspergillus fumigatus.2009

    • Author(s)
      Osada, H. (5名中5番目)
    • Journal Title

      Bioinformatics 25

      Pages: 2295-2297

    • Peer Reviewed
  • [Journal Article] Functional analyses of cytochrome P450 genes responsible for the early steps of brassicicene C biosynthesis.2009

    • Author(s)
      Takahashi, S. (9名中3番目), Osada, H. (9名中4番目)
    • Journal Title

      Bioorg. Med. Chem. Lett. 19

      Pages: 5640-5643

    • Peer Reviewed
  • [Journal Article] Exploring the chemical space of microbial natural products.2009

    • Author(s)
      Osada, H. (2名中1番目)
    • Journal Title

      Curr. Opin. Chem. Biol. 13

      Pages: 133-134

    • Peer Reviewed
  • [Journal Article] ATM blocks tunicamycin-induced endoplasmic reticu-lum stress.2009

    • Author(s)
      Osada, H. (10名中7番目)
    • Journal Title

      FEBS Lett. 583

      Pages: 903-908

    • Peer Reviewed
  • [Journal Article] Kerriamycin B inhibits protein SUMOylation.2009

    • Author(s)
      Osada, H. (7名中6番目), Yoshida, M. (7名中7番目)
    • Journal Title

      J. Antibiot. 62

      Pages: 221-224

    • Peer Reviewed
  • [Journal Article] Deficiency in chromosome congression by the inhibition of PLK1 polo box domain-dependent recognition.2009

    • Author(s)
      Osada, H. (7名中7番目)
    • Journal Title

      J. Biol. Chem. 284

      Pages: 2344-2353

    • Peer Reviewed
  • [Journal Article] Inhibition of protein tyrosine phosphatase 1B by lupeol and lupenone isolated from Sorbus commixta.2009

    • Author(s)
      Osada, H. (4名中3番目)
    • Journal Title

      J. Enzyme Inhib. Med. Chem. 24

      Pages: 1056-1059

    • Peer Reviewed
  • [Journal Article] Characterization of the tautomycetin biosynthetic gene cluster from Streptomyces griseochromogenes provides new insight into dialkylmaleic anhydride biosynthesis.2009

    • Author(s)
      Osada, H. (6名中5番目)
    • Journal Title

      J. Nat. Prod. 72

      Pages: 450-459

    • Peer Reviewed
  • [Journal Article] Polo-like kinase 1 phosphorylates and regulates Bcl-x(L) during pironetin-induced apoptosis.2009

    • Author(s)
      Osada, H. (7名中7番目)
    • Journal Title

      Oncogene 28

      Pages: 107-116

    • Peer Reviewed
  • [Journal Article] Functional characterization of ttmM unveils new tautomycin analogs and insight into tautomycin biosynthesis and activity.2009

    • Author(s)
      Osada, H. (8名中7番目)
    • Journal Title

      Org. Lett. 11

      Pages: 1639-1642

    • Peer Reviewed
  • [Journal Article] The asymmetric total synthesis of (+)-cytotrienin A, an ansamycin-type anticancer drug.2008

    • Author(s)
      Hayashi, Y. (10名中1番目), Kakeya, H. (10名中9番目), Osada, H. (10名中10番目)
    • Journal Title

      Angew. Chem. Int. Ed. 47

      Pages: 6657-6660

    • Peer Reviewed
  • [Journal Article] Crystal structure of VioE, a key player in the construction of the molecular skelton of violacein.2008

    • Author(s)
      Shiro, Y. (5名中4番目)
    • Journal Title

      J. Biol. Chem. 283

      Pages: 6459-6466

    • Peer Reviewed
  • [Journal Article] Purification and functional characterization of human 11βhydroxylase expressed in E. coli.2008

    • Author(s)
      Shiro, Y. (8名中6番目)
    • Journal Title

      FEBS J. 275

      Pages: 799-810

    • Peer Reviewed
  • [Journal Article] Crystal structure of CYP105A1 (P450SU-1) in complex with 1α2008

    • Author(s)
      Shiro, Y. (9名中8番目)
    • Journal Title

      25-dihydroxyvitamin D3., Biochemistry 47

      Pages: 4017-4027

    • Peer Reviewed
  • [Journal Article] Synthesis and structure-activity relationship studies on tryprostatin A, an inhibitor of breast cancer resistance protein.2008

    • Author(s)
      Kakeya, H. (15名中13番目), Osada, H. (15名中14番目)
    • Journal Title

      Bioorg. Med. Chem. 16

      Pages: 4626-4651

    • Peer Reviewed
  • [Journal Article] Synthesis and biological activities of reveromycin A and spirofungin a derivatives.2008

    • Author(s)
      Shimizu, T. (10名中1番目), Usui, T. (10名中2番目), Osada, H. (10名中9番目)
    • Journal Title

      Bioorg. Med. Chem. Lett. 18

      Pages: 3756-3760

    • Peer Reviewed
  • [Journal Article] A fungal metabolite, epoxyquinol B inhibits the NF-kappaB signal through the crosslinking of TAK1.2008

    • Author(s)
      Usui, T. (7名中2番目), Hayashi, Y. (7名中5番目), Kakeya, H. (7名中6番目), Osada, H. (7名中7番目)
    • Journal Title

      Biosci. Biotechnol. Biochem. 72

      Pages: 1894-1900

    • Peer Reviewed
  • [Journal Article] Robust and systematic drug screening method using chemical arrays and the protein library: Identification of novel inhibitors of carbonic anhydrase II.2008

    • Author(s)
      Osada, H. (5名中5番目)
    • Journal Title

      Biosci. Biotechnol. Biochem. 72

      Pages: 2739-2749

    • Peer Reviewed
  • [Journal Article] Synthesis and anti-angiogenic activity of cortistatin analogs.2008

    • Author(s)
      Usui, T. (7名中3番目), Osada, H. (7名中5番目)
    • Journal Title

      Biosci. Biotechnol. Biochem. 72

      Pages: 2992-2997

    • Peer Reviewed
  • [Journal Article] Azaspirene, a fungal product, inhibits angiogenesis by blocking Raf-1 activation.2008

    • Author(s)
      Kakeya, H. (8名中2番目), Kojima, S. (8名中4番目), Osada, H. (8名中8番目)
    • Journal Title

      Cancer Sci. 99

      Pages: 1853-1858

    • Peer Reviewed
  • [Journal Article] Inhibition of bone and muscle metastases of lung cancer cells by a decrease in the number of monocytes/macrophages.2008

    • Author(s)
      Osada, H. (12名中10番目)
    • Journal Title

      Cancer Sci. 99

      Pages: 1595-1602

    • Peer Reviewed
  • [Journal Article] Improvement of photoaffinity SPR imaging platform and determination of binding site of p62/SQSTM1 to p38 MAP kinase.2008

    • Author(s)
      Saito, A. (6名中1番目), Osada, H. (6名中6番目)
    • Journal Title

      Chemistry Asian J. 3

      Pages: 1607-1612

    • Peer Reviewed
  • [Journal Article] Fungal metabolite, epoxyquinol B, crosslinks proteins by epoxy-thiol conjugation.2008

    • Author(s)
      Usui, T. (8名中2番目), Hayashi, Y. (8名中6番目), Kakeya, H. (8名中7番目), Osada, H. (8名中8番目)
    • Journal Title

      J. Antibiot. 61

      Pages: 94-97

    • Peer Reviewed
  • [Journal Article] Specific regulation of cytokine dependent p38 MAP kinase activation by p62/SQSTM1.2008

    • Author(s)
      Saito, A. (4名中3番目), Osada, H. (4名中4番目)
    • Journal Title

      J. Biochem. 143

      Pages: 765-772

    • Peer Reviewed
  • [Journal Article] Characterization of the tautomycin biosynthetic gene cluster from Streptomyces spiroverticillatus unveiling new insights into dialkylmaleic anhydride and polyketide biosynthesis.2008

    • Author(s)
      Osada, H. (5名中4番目)
    • Journal Title

      J. Biol. Chem. 283

      Pages: 28607-28617

    • Peer Reviewed
  • [Journal Article] Epoxyquinol B shows antiangiogenic effects by inhibiting not only VEGFR2 but also EGFR, FGFR, and PDGFR.2008

    • Author(s)
      Kakeya, H. (7名中2番目), Usui, T. (7名中3番目), Hayashi, Y. (7名中6番目), Osada, H. (7名中7番目)
    • Journal Title

      Oncol. Res. 17

      Pages: 11-21

    • Peer Reviewed
  • [Journal Article] The identification of an osteoclastogenesis inhibitor through the inhibition of glyoxalase I.2008

    • Author(s)
      Okumura, H. (11名中2番目), Osada, H. (11名中11番目)
    • Journal Title

      Proc. Natl. Acad. Sci. USA 105

      Pages: 11691-11696

    • Peer Reviewed
  • [Journal Article] Inhibition of Hsp90 activates osteoclast c-Src signaling and promotes growth of prostate carcinoma cells in bone.2008

    • Author(s)
      Osada, H. (7名中6番目)
    • Journal Title

      Proc. Natl. Acad. Sci. USA 105

      Pages: 15541-15546

    • Peer Reviewed
  • [Journal Article] Distribution of photo-cross-linked products from 3-aryl-3-trifluoro-methyldiazirines and alcohols.2008

    • Author(s)
      Osada, H. (6名中6番目)
    • Journal Title

      Tetrahedron 64

      Pages: 5692-5698

    • Peer Reviewed
  • [Journal Article] Antiproliferating activity of the mitotic inhibitor pironetin against vindesine-and paclitaxel-resistant human small cell lung cancer H69 cells.2007

    • Author(s)
      Usui, T. (6名中4番目), Osada, H. (6名中5番目)
    • Journal Title

      Anticancer Res. 27

      Pages: 729-736

    • Peer Reviewed
  • [Journal Article] Glaziovianin A, a new isoflavone, from the leaves of Ateleia glazioviana and its cytotoxic activity against human cancer cells.2007

    • Author(s)
      Usui, T. (7名中3番目), Osada, H. (7名中5番目)
    • Journal Title

      Bioorg. Med. Chem. Lett. 17

      Pages: 3091-3094

    • Peer Reviewed
  • [Journal Article] Involvement of disulfide bond formation in the activation of heparanase.2007

    • Author(s)
      Osada, H. (7名中7番目)
    • Journal Title

      Cancer Res. 67

      Pages: 7841-7849

    • Peer Reviewed
  • [Journal Article] Synthesis of (+)-vinblastine and its analogues.2007

    • Author(s)
      Osada, H. (6名中4番目)
    • Journal Title

      Org. Lett. 9

      Pages: 4737-4740

    • Peer Reviewed
  • [Journal Article] Iejimalides shows anti-osteoclast activity via V-ATPase inhibition.2006

    • Author(s)
      Usui, T. (7名中5番目), Osada, H. (7名中7番目)
    • Journal Title

      Biosci. Biotechnol. Biochem. 70

      Pages: 1364-1370

    • Peer Reviewed
  • [Journal Article] Brasilicardin A, a natural immunosuppressant, targets amino acid transport system L.2006

    • Author(s)
      Usui, T. (7名中1番目), Osada, H. (7名中7番目)
    • Journal Title

      Chem. Biol. 13

      Pages: 1153-1160

    • Peer Reviewed
  • [Journal Article] Crystal structure of human indoleamine 2, 3-dioxygenase: insight into the catalytic mechanism of O2 incorporation by a hemecontaining dioxygenase.2006

    • Author(s)
      Shiro, Y. (6名中6番目)
    • Journal Title

      Proc. Natl. Acad. Sci. USA 103

      Pages: 2611-2616

    • Peer Reviewed
  • [Journal Article] Suppression of apoptosis by cyclophilin D via stabilization of hexokinase II mitochondrial binding in cancer cells.2006

    • Author(s)
      Osada, H. (3名中3番目)
    • Journal Title

      J. Biol. Chem. 281

      Pages: 14314-14320

    • Peer Reviewed
  • [Journal Article] Reveromycin A inhibits osteolytic bone metastasis of small-cell lung cancer cells, SBC-5, through an anti-osteoclastic activity.2005

    • Author(s)
      Osada, H. (7名中6番目)
    • Journal Title

      Clin. Cancer Res. 11

      Pages: 8822-8828

    • Peer Reviewed
  • [Journal Article] Cyclindependent kinase (CDK) phosphorylation destabilizes somatic Wee1 via multiple pathways.2005

    • Author(s)
      Osada, H. (7名中7番目)
    • Journal Title

      Proc. Natl. Acad. Sci. USA 102

      Pages: 11663-11668

    • Peer Reviewed
  • [Journal Article] Epoxytwinol A, a novel unique angiogenesis inhibitor with C2 symmetry, produced by a fungus.2005

    • Author(s)
      Osada, H. (4名中4番目)
    • Journal Title

      Chem. Commun. 20

      Pages: 2575-2577

    • Peer Reviewed
  • [Journal Article] Application of proteomic profiling based on 2-DIGE for classification of compounds according to the mechanism of action.

    • Author(s)
      Usui, T. (8名中7番目), Osada, H. (8名中8番目)
    • Journal Title

      Chem. Biol. (in press)

    • Peer Reviewed
  • [Journal Article] Glyoxalase-I is a novel target against Bcr-Abl(+) leukemic cells acquiring stem-like characteristics in a hypoxic environment.

    • Author(s)
      Osada, H. (16名中6番目)
    • Journal Title

      Cell Death Differ. (in press)

    • Peer Reviewed
  • [Journal Article] One-pot synthesis of chiral bicycle [3. 3. 0] octatrienes using diphenylprolinol silyl ether-mediated ene-type reaction.

    • Author(s)
      Hayashi, Y. (4名中4番目)
    • Journal Title

      Tetrahedron (in press)

    • Peer Reviewed
  • [Journal Article] Modulation of E-cadherin expression by K-Ras; involvement of DNA methyltransferase-3b.

    • Author(s)
      Osada, H. (10名中7番目)
    • Journal Title

      Carcinogenesis (in press)

    • Peer Reviewed
  • [Presentation] Large nonlinear effect observed in the enantiomeric excess of proline in solution and that in the solid state, and its implication to the homochirality in this universe.2009

    • Author(s)
      Hayashi, Y.
    • Organizer
      238th American Chemical Society National Meeting
    • Place of Presentation
      Washington, D.C., USA
    • Year and Date
      2009-08-17
  • [Presentation] Metabolomic and genomic analyses of Streptomyses reveromyceticus, a producer of antiosteoclasts compound.2007

    • Author(s)
      Osada, H.
    • Organizer
      INDUSTRIAL MICROBIOGY & BIOTECHNOLOGY, Society for Industrial Microbiology Annual Meeting
    • Place of Presentation
      Denver, USA
    • Year and Date
      2007-07-31
  • [Book] Protein Targeting with Small Molecules.2009

    • Author(s)
      Osada, H. Ed.
    • Total Pages
      289
    • Publisher
      A John Wiley, Sons, Inc.
  • [Patent(Industrial Property Rights)] 光学活性テトラヒドロピラン化合物の製造方法2009

    • Inventor(s)
      林雄二郎
    • Industrial Property Rights Holder
      東京理科大学
    • Industrial Property Number
      特許権・特願2009-165510
    • Filing Date
      2009-07-14

URL: 

Published: 2011-06-18   Modified: 2016-04-21  

Information User Guide FAQ News Terms of Use Attribution of KAKENHI

Powered by NII kakenhi