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2004 Fiscal Year Annual Research Report

生物新機能と創薬をめざす生体内分子科学

Research Project

Project/Area Number 13NP0401
Research InstitutionGifu University

Principal Investigator

鈴木 正昭  岐阜大学, 大学院・医学研究科, 教授 (90093046)

Co-Investigator(Kenkyū-buntansha) 渡辺 恭良  大阪市立大学, 大学院・医学研究科, 教授 (40144399)
松田 彰  北海道大学, 大学院・薬学研究科, 教授 (90157313)
石川 智久  東京工業大学, 大学院・生命理工学研究科, 教授 (60193281)
根岸 学  京都大学, 大学院・生命科学研究科, 教授 (60201696)
伊藤 誠二  関西医科大学, 医学部, 教授 (80201325)
Keywords3成分連結PG合成法 / non-RI光親和性標識法 / 蛍光プローブ / ABCトランスポーター / Socius / 神経性疼痛 / プラナーポジトロンイメージング / MicroPET
Research Abstract

リチウムエノラートの溶液構造とHMPAの効果を詳細に解析し、環境調和型高効率3成分連結PG合成法開発のための基礎理論を構築した。アルキルアジド基を活用した汎用non-RI光親和性標識法を開発し、HMG-CoA還元酵素やリアノジン受容体プローブに応用して標的タンパク質の標識に成功した。新規核内受容体RXRアゴニストを開発し、遺伝子発現プロファイルや受容体活性化作用を明らかにした。キラルシクロプロパンユニットを活用してヒスタミンH3受容体およびNMDA受容体プローブを創製した。新たなフルオレセイン系蛍光プローブの設計理論を構築し、β-ガラクトシダーゼ蛍光プローブを開発した。アロディニア誘発にかかわる新規アクロメリン酸受容体探索プローブを創製した。アスコルビン酸をコア構造とするチロシンポスファターゼ阻害剤ライブラリーを構築した。
高密度タイリングアレイを用いて5-FU刺激後の特定ゲノム配列の解析に成功した。ヒトABCトランスポーターABCG2の基質特異性自動化高速スクリーニング装置を開発、抗癌剤イリノテカン誘導体に応用して耐性を克服する薬剤設計理論を構築した。
RhoファミリーGタンパク質Rnd1およびG12ファミリーに結合する新規分子を発見しSociusと命名した。NADPH diaphorase染色に基づく難治性疼痛の可視化・定量化法を開発し、非可逆的神経損傷に伴う神経性疼痛がNO産生により維持されることを明らかにした。
プラナーポジトロンイメージング装置(PPIS)を用いて薬剤の脳内移行性を評価する手法を確立した。末梢性ベンゾジアゼピン受容体リガンドの^<18>F-標識体の合成とPETイメージングに成功した。MicroPET装置を用いて^<68>Gaを活用する手法を検討した。Cu-ATSMと^<18>F-FDGの同時投与によるPETイメージング診断法の有用性を実証した。

  • Research Products

    (58 results)

All 2005 2004 Other

All Journal Article (58 results)

  • [Journal Article] Involvement of Rho-kinase in through phosphorylation of myristoylated alanine-rich C-kinase substrate (MARCKS)2005

    • Author(s)
      S.Tatsumi
    • Journal Title

      Neuroscience 131・2

      Pages: 491-498

  • [Journal Article] Design of dantrolrne-derived probes for radioisotope-free photoaffinity labeling of proteins involved in the physiological Ca^<2+> release from sarcoplasmic reticulum of skeletal muscle.2005

    • Author(s)
      T.Hosoya
    • Journal Title

      Bioorg.Med.Chem.Lett. 15・5

      Pages: 1289-1294

  • [Journal Article] Novel bifunctional probe for radioisotope-free photoaffinity labeling : compact structure comprised of photospecific ligand ligation and detectable tag anchoring units2004

    • Author(s)
      T.Hosoya
    • Journal Title

      Org.Biomol.Chem. 2・5

      Pages: 637-641

  • [Journal Article] Manipulation of alternative splicing by a newly developed inhibitor of Clks.2004

    • Author(s)
      M.Muraki
    • Journal Title

      J.Biol.Chem. 279・23

      Pages: 24246-24254

  • [Journal Article] A simple acromelic acid analog potentially useful for receptor photoaffinity labeling and biochemical studies2004

    • Author(s)
      K.Furuta
    • Journal Title

      Tetrahedron Letters 45・20

      Pages: 3933-3936

  • [Journal Article] Anti-apoptotic and pro-apoptotic effect of NEPP11 on manganese-induced apoptosis and JNK pathway activation in PC12 cells2004

    • Author(s)
      Y.Hirata
    • Journal Title

      Brain Research 1021・2

      Pages: 241-247

  • [Journal Article] Rapid methylation on carbon frameworks leading to the synthesis of a PET tracer capable of imaging a novel CNS-type prostacyclin receptor in living human brain2004

    • Author(s)
      M.Suzuki
    • Journal Title

      Trends in Analytical Chemistry 23・8

      Pages: 595-607

  • [Journal Article] Synthesis of ^<11>C-labelled N, N'-diphenylurea and ethyl phenylcarbamate by a rhodium-promoted carbonylation via [^<11>C]isocyanatobenzene using phynyl azide and [^<11>C]carbon monoxide2004

    • Author(s)
      H.Doi
    • Journal Title

      Org.Biomol.Chem. 2・21

      Pages: 3063-3066

  • [Journal Article] ミニレビュー脳を探る分子プローブ設計:ヒト脳内IP_2受容体の分子イメージング2004

    • Author(s)
      鈴木正昭
    • Journal Title

      日本神経精神薬理学雑誌 24

      Pages: 221-229

  • [Journal Article] Positron Emission Tomography (PET)法による生体の分子イメージング研究と創薬・医療への応用2004

    • Author(s)
      鈴木正昭
    • Journal Title

      生物物理 44・6

      Pages: 265-270

  • [Journal Article] Structure-based Design of a Selective Heparanase Inhibitor as an Antimetastatic Agent.2004

    • Author(s)
      K.Ishida
    • Journal Title

      Mol.Cancer Therapeutics 3・9

      Pages: 1069-1077

  • [Journal Article] Design, Synthesis, and Structure-Activity Relationship of New Isobenzofuranone Ligands of Protein Kinase C2004

    • Author(s)
      Y.Baba
    • Journal Title

      Bioorg.Med.Chem.Lett. 14・11

      Pages: 2963-2967

  • [Journal Article] Evaluation of Series of Isobenzofuranone Dimers as PKCα Ligands : Implication for the Distance between the Two Ligand Binding Sites.2004

    • Author(s)
      Y.Baba
    • Journal Title

      Bioorg.Med.Chem.Lett. 14・11

      Pages: 2969-2972

  • [Journal Article] Amine-salt-controlled, Catalytic Asymmetric Conjugate Addition of Various Amines and Asymmetric Protonation.2004

    • Author(s)
      Y.Hamashima
    • Journal Title

      Org.Lett. 6・11

      Pages: 1861-1864

  • [Journal Article] Highly sensitive fluorescence probes for nitric oxide based on boron dipyrromethene chromophore-rational design of potentially useful bioimaging fluorescence probe.2004

    • Author(s)
      Y.Gabe
    • Journal Title

      J.Am.Chem.Soc. 126・10

      Pages: 3357-3367

  • [Journal Article] NMR conformational analysis of biosynthetic precursor-type lipid A : monomolecular state and supramolecular assembly2004

    • Author(s)
      M.Oikawa
    • Journal Title

      Org.Biomol.Chem. 2・24

      Pages: 3557-3565

  • [Journal Article] Ligand-dependent Toll-like receptor 4(TLR4)-oligomerization is directly linked with TLR4-signaling.2004

    • Author(s)
      S.Saitoh
    • Journal Title

      J.Endotoxin Res. 10・4

      Pages: 257-260

  • [Journal Article] Aggregates are the biologically active units of endotoxin2004

    • Author(s)
      M.Mueller
    • Journal Title

      J.Biol.Chem. 279・25

      Pages: 26307-26313

  • [Journal Article] Combinational clustering of receptors following stimulation by bacterial products determines lipopolysaccharide responses2004

    • Author(s)
      M.Triantafilou
    • Journal Title

      Biochem.J. 381・Pt2

      Pages: 527-536

  • [Journal Article] Lipid A antagonist, lipid 1Va, is distinct from lipid A in interaction with Toll-like receptor 4(TLR4)-MD-2 and ligand-induced TLR4 oligomerization2004

    • Author(s)
      S.Saitoh
    • Journal Title

      Int.Immun. 16・7

      Pages: 961-969

  • [Journal Article] Enantioselective total synthesis of batzelladine A.2004

    • Author(s)
      J.Shimokawa
    • Journal Title

      Angew.Chem.Int.Ed. 43・12

      Pages: 1559-1562

  • [Journal Article] Development of novel chiral urea catalysts for the hetero Michael reaction2004

    • Author(s)
      Y.Sohtome
    • Journal Title

      Chem.Pharm.Bull. 52・4

      Pages: 477-480

  • [Journal Article] Thalidomide as a nitric oxide synthase inhibitor and its structural development.2004

    • Author(s)
      R.Shimazawa
    • Journal Title

      Chem.Pharm.Bull. 52・4

      Pages: 498-499

  • [Journal Article] Synthesis of 1α,25-dihydroxyvitamin D_3-26,23-lactams (DLAMs), a novel series of 1α,25-dihydroxyvitamin D_3 antagonist.2004

    • Author(s)
      Y.Kato
    • Journal Title

      Bioorg.Med.Chem.Lett. 14・10

      Pages: 2579-2583

  • [Journal Article] Novel betaines from a Micronesian sponge Dysidea herbacea.2004

    • Author(s)
      R.Sakai
    • Journal Title

      J.Org.Chem. 69・4

      Pages: 1180-1185

  • [Journal Article] L-Glutamate in the extracellular space regulates endogeneous D-aspartate homeostasis in rat pheochromocytoma MPT1 cells.2004

    • Author(s)
      M.Adachi
    • Journal Title

      Arc.Biochem.Biophys. 424・1

      Pages: 89-96

  • [Journal Article] Characterization of novel L-threo-β-benzyloxyaspartate derivatives, potent blockers of the glutamate transporters.2004

    • Author(s)
      K.Shimamoto
    • Journal Title

      Mol.Pharmacol. 65・4

      Pages: 1008-1015

  • [Journal Article] Synthesis of carbamate-type cages derivatives of a novel glutamate transporter blocker.2004

    • Author(s)
      K.Takaoka
    • Journal Title

      Bioorg.Med.Chem. 12・13

      Pages: 3687-3694

  • [Journal Article] Molecular pharmacology of glutamate transporters, EAATs and VGLUTs.2004

    • Author(s)
      Y.Shigeri
    • Journal Title

      Brain Res.Rev. 45・3

      Pages: 250-265

  • [Journal Article] Alteration in the cellular response to retinoic acid of a human acute promyelocytic leukemia cell line UF-1, carrying a patient-derived mutant PML-RARα chimetric gene.2004

    • Author(s)
      A.Sato
    • Journal Title

      Leukemia Res. 28・9

      Pages: 959-967

  • [Journal Article] Design and synthesis of cyclic urea compounds : a pharmacological study for retinoidal activity.2004

    • Author(s)
      M.Kurihara
    • Journal Title

      Bioorg.Med.Chem.Lett. 14・16

      Pages: 4131-4134

  • [Journal Article] The Endocrine Disruptors Nonylphenol and Octylphenol Exert Direct Effects on T Cells to Suppress Th1 Development and Enhance Th2 Development.2004

    • Author(s)
      M.Iwata
    • Journal Title

      Immunol.Lett. 94・1-2

      Pages: 135-139

  • [Journal Article] Docosahexaenoic Acid Reduces Haloperidol-Induced Dyskinesias in Mice : Involvement of Nur77 and Retinoid Receptors.2004

    • Author(s)
      I.Ethier
    • Journal Title

      Biol.Psychiatry 56・7

      Pages: 522-526

  • [Journal Article] Novel Retinoid X Receptor (RXR) Antagonists Having a Dicarba-closo-dodecaborane as a Hydrophobic Moiety.2004

    • Author(s)
      K.Ohta
    • Journal Title

      Bioorg.Med.Chem.Lett. 14・23

      Pages: 5913-5918

  • [Journal Article] Differential modulation of PI3-kinase/Akt pathway during all-trans retinoic acid- and Am80-induced HL-60 cell differentiation revealed by DNA microarray analysis.2004

    • Author(s)
      S.Ishida
    • Journal Title

      Biochem.Pharmacol. 68・11

      Pages: 2177-2186

  • [Journal Article] Retinoic Acid Imprintis Gut-Homing Specificity on T Cells.2004

    • Author(s)
      M.Iwata
    • Journal Title

      Immunity 21・4

      Pages: 527-538

  • [Journal Article] Transport of SN-38 by the wild type of human ABC transporter ABCG2 and its inhibition by quercetin, a natural flavonoid.2004

    • Author(s)
      M.Yoshikawa
    • Journal Title

      J.Exp.Ther.Oncol. 4・1

      Pages: 25-35

  • [Journal Article] Functional evaluation of ABCB1 (P-Glycoprotein) polymorphisms : High-speed screening and Structure-activity relationship analyses.2004

    • Author(s)
      T.Ishikawa
    • Journal Title

      Drug Metabol.Pharmacokin. 19・1

      Pages: 1-14

  • [Journal Article] Novel camptothecin analogues that circumvent ABCG2-associated drug resistance in human tumor cells.2004

    • Author(s)
      M.Yoshikawa
    • Journal Title

      Int.J.Cancer 110・6

      Pages: 921-927

  • [Journal Article] Pharmacogenomics of drug transporters : a new approach to functional analysis of the genetic polymorphisms of ABCB1(P-glycoprotein/MDR1)2004

    • Author(s)
      T.Ishikawa
    • Journal Title

      Biol.Pharm.Bull. 27・7

      Pages: 939-948

  • [Journal Article] The genetic polymorphism of drug transpoters : functional analysis approaches.2004

    • Author(s)
      T.Ishikawa
    • Journal Title

      Pharmacogenomics 5・1

      Pages: 67-99

  • [Journal Article] Identification of splicing variants of Rapostlin, a novel RND2 effector that interacts with N-WASP(neural Wiskott-Aldorich syndrome protein) and induces neurite branching.2004

    • Author(s)
      T.kakimoto
    • Journal Title

      J.Biol.Chem. 279・14

      Pages: 14104-14110

  • [Journal Article] Regulation of binding of lamin B receptor to chromatin by SR protein kinase and cdc2 kinase in Xenopus egg extracts2004

    • Author(s)
      M.Takano
    • Journal Title

      J.Biol.Chem. 279・13

      Pages: 13265-13271

  • [Journal Article] Abnormal angiogenesis in Foxol (FKHR)-deficient mice.2004

    • Author(s)
      T.Furuyama
    • Journal Title

      J Biol Chem. 279・33

      Pages: 34741-34749

  • [Journal Article] Modulation of the stathmin-like microtubule destabilizing activity of RB3, a neural-specific member of the SCG10 family, by its N-terminal domain2004

    • Author(s)
      C.Nakao
    • Journal Title

      J.Biol.Chem. 279・22

      Pages: 23014-23021

  • [Journal Article] Direct interaction of NRSF with TBP : The chromatin-reorganization and the core promoter repression for neuron-specific gene transcription.2004

    • Author(s)
      K.Murai
    • Journal Title

      Nucl.Acid Res. 32・10

      Pages: 3180-3189

  • [Journal Article] 老化遺伝子2004

    • Author(s)
      森 望
    • Journal Title

      臨床整形外科 39・2

      Pages: 176-179

  • [Journal Article] ドッキング蛋白Shcの神経系における役割2004

    • Author(s)
      森 望
    • Journal Title

      生体の科学 55・2

      Pages: 103-110

  • [Journal Article] 脳の老化と寿命制御2004

    • Author(s)
      森 望
    • Journal Title

      日本老年医学会雑誌 41・3

      Pages: 266-270

  • [Journal Article] Pituitary adenylate cyclase-activating polypeptide is required for the development of spinal sensitization and induction of neuropathic pain.2004

    • Author(s)
      T.Mabuchi
    • Journal Title

      J.Neurosci. 24・33

      Pages: 7283-7291

  • [Journal Article] Acute and late effects on induction of allodynia by acromelic acid, a mushroom poison related structurally to kainic acid.2004

    • Author(s)
      T.Minami
    • Journal Title

      Br.J.Pharmacol. 142・4

      Pages: 679-688

  • [Journal Article] Novel peripheral benzodiazepine receptor ligand [^<11>C]DAA1106 for PET an imaging tool for glial cells in the brain.2004

    • Author(s)
      J.Maeda
    • Journal Title

      Synapse 52・4

      Pages: 283-291

  • [Journal Article] Development of a new radioligand, N-(5-fluoro-2-phenoxyphenyl)-N-(2-[^<18>F]fluoroethyl-5-methoxybenzyl) acetamide, for PET imaging of peripheral benzodiazepine receptor in primate brain.2004

    • Author(s)
      MR.Zhang
    • Journal Title

      J.Med.Chem. 47・9

      Pages: 2228-2235

  • [Journal Article] Effects of acute acetylcholinesterase inhibition on the cerebral cholinergic neuronal system and cognitive function : functional imaging of the conscious monkey brain using animal PET in combination with microdialysis.2004

    • Author(s)
      H.Tsukada
    • Journal Title

      Synapse 52・1

      Pages: 1-10

  • [Journal Article] Evaluation of [^<18>F]fluorinated sigma receptor ligands in the conscious monkey brain.2004

    • Author(s)
      P.H.Elsinga
    • Journal Title

      Synapse 52・1

      Pages: 29-37

  • [Journal Article] Evaluation of in vivo selective binding of [^<11>C]doxepine to histamine H_1 receptors in five animal species.2004

    • Author(s)
      K.Ishikawa
    • Journal Title

      Nucl.Med.Biol. 31・4

      Pages: 493-502

  • [Journal Article] Catalytic Asymmetric Addition of β-Ketoesters to Various Imines Using Chiral Pd Complexes.

    • Author(s)
      Y.Hamashima
    • Journal Title

      Angew.Chem.Int.Ed. (印刷中)

  • [Journal Article] Thalidomide as a multi-target drug and its application as a template for drug design.

    • Author(s)
      Y.Hashimoto
    • Journal Title

      Drugs Future (印刷中)

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Published: 2006-07-12   Modified: 2016-04-21  

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