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Creation of novel anticancer lead compounds by in silico design of XIAP antagonists

Research Project

Project/Area Number 22590107
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeSingle-year Grants
Section一般
Research Field Drug development chemistry
Research InstitutionTokyo University of Science

Principal Investigator

TAMURA Seiichi  東京理科大学, 薬学部薬学科, 教授 (10142449)

Co-Investigator(Kenkyū-buntansha) TAKASAWA Ryoko  東京理科大学, 薬学部・薬学科, 講師 (10398828)
Project Period (FY) 2010 – 2012
Project Status Completed (Fiscal Year 2012)
Budget Amount *help
¥4,550,000 (Direct Cost: ¥3,500,000、Indirect Cost: ¥1,050,000)
Fiscal Year 2012: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2011: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2010: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Keywords医薬分子設計 / 癌 / シグナル伝達 / 薬学
Research Abstract

XIAP, which is involved in resistances for anticancer drugs and irradiation, is an attractive target for the development of new anticancer drugs. In this study, we attempted to create novel lead compounds for new anticancer drugs. As a result, we could discover a novel agonistic compound, which possess a good binding form to XIAP.

Report

(4 results)
  • 2012 Annual Research Report   Final Research Report ( PDF )
  • 2011 Annual Research Report
  • 2010 Annual Research Report
  • Research Products

    (46 results)

All 2013 2012 2011 2010

All Journal Article (26 results) (of which Peer Reviewed: 26 results) Presentation (14 results) Book (6 results)

  • [Journal Article] PARP1 gene expression is downregulated by knockdown of PARG gene.2013

    • Author(s)
      Uchiumi F、Watanabe T、 Ohta R、 Abe H、 Tanuma S
    • Journal Title

      Oncol Rep

      Volume: 29 Pages: 1683-1688

    • Related Report
      2012 Annual Research Report 2012 Final Research Report
    • Peer Reviewed
  • [Journal Article] CHK1 cleavage in programmed cell death is intricately regulated by both caspase and non-caspase family proteases2013

    • Author(s)
      Okita N 、 Yoshimura M 、 Watanabe K、 Minato S、 Kudo Y、 Higami Y、 Tanuma S.
    • Journal Title

      Biochim Biophys Acta

      Volume: 1830(1) Pages: 2204-13

    • Related Report
      2012 Final Research Report
    • Peer Reviewed
  • [Journal Article] CHK1 cleavage in programmed cell death is intricately regulated by both caspase and non-caspase family proteases.2013

    • Author(s)
      Okita N, Yoshimura M, Watanabe K, Minato S, Kudo Y, Higami Y, Tanuma S.
    • Journal Title

      Biochim Biophys Acta.

      Volume: 1830 Issue: 1 Pages: 2204-2213

    • DOI

      10.1016/j.bbagen.2012.10.009

    • Related Report
      2012 Annual Research Report
    • Peer Reviewed
  • [Journal Article] DNA damage-induced CHK1 autophosphorylation at Ser296 is regulated by an intramolecular mechanism2012

    • Author(s)
      Okita N、 Minato S、 Ohmi E、 Tanuma S
    • Journal Title

      Higami Y. FEBS Lett

      Volume: 586(22) Pages: 3974-9

    • Related Report
      2012 Final Research Report
    • Peer Reviewed
  • [Journal Article] Novel compound SK-1009 suppresses interleukin-6 expression through modulation of activation of nuclear factor-kappaB pathway.2012

    • Author(s)
      Shimura M 、 Yamamoto M、 Fujii G、 Takahashi M、 Komiya M、 Noma N、 Tanuma S、 Yanaka A 、 Mutoh M.
    • Journal Title

      Biol Pharm Bull

      Volume: 35(12) Pages: 2186-91

    • Related Report
      2012 Final Research Report
    • Peer Reviewed
  • [Journal Article] Anticipation of a novel gene therapy inspired by a concept of iPS cells2012

    • Author(s)
      Fumiaki Uchiumi and Sei-ichi Tanuma.
    • Journal Title

      Pharmaceutica Analytica Acta.

      Volume: 3(10) Pages: 196-196

    • Related Report
      2012 Final Research Report
    • Peer Reviewed
  • [Journal Article] Effects of thujaplicins on the promoter activities of the human SIRT1 and telomere maintenance factor encoding genes.2012

    • Author(s)
      F. Uchiumi 、 H. Tachibana、 H. Abe、A. Yoshimori 、 T. Kamiya、 M. Fujikawa、 S. Larsen、 A.Honma 、 S. Ebizuka 、 S. Tanuma.
    • Journal Title

      Pharmaceutica Analytica Acta

      Volume: 3(5) Pages: 159-159

    • Related Report
      2012 Final Research Report
    • Peer Reviewed
  • [Journal Article] Effect of lignin glycosides extracted from pine cones on the human SIRT1 promoter.2012

    • Author(s)
      promoter. Fumiaki Uchiumi 、 Haruki Tachibana、 Steven Larsen、 Sei-ichi Tanuma
    • Journal Title

      Pharmaceutica Analytica Acta

      Volume: 8 Pages: 001-001

    • Related Report
      2012 Final Research Report
    • Peer Reviewed
  • [Journal Article] DNA damage-induced CHK1 autophosphorylation at Ser296 is regulated by an intramolecular mechanism.2012

    • Author(s)
      Okita N, Minato S, Ohmi E, Tanuma S, Higami Y.
    • Journal Title

      FEBS Lett.

      Volume: 586 Issue: 22 Pages: 3974-3979

    • DOI

      10.1016/j.febslet.2012.09.048

    • Related Report
      2012 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Novel compound SK-1009 suppresses interleukin-6 expression through modulation of activation of nuclear factor-kappaB pathway.2012

    • Author(s)
      Shimura M, Yamamoto M, Fujii G, Takahashi M, Komiya M, Noma N, Tanuma S, Yanaka A, Mutoh M.
    • Journal Title

      Biol Pharm Bull.

      Volume: 35 Pages: 2186-2191

    • Related Report
      2012 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Anticipation of a novel gene therapy inspired by a concept of iPS cells2012

    • Author(s)
      Fumiaki Uchiumi and Sei-ichi Tanuma
    • Journal Title

      Pharmaceutica Analytica Acta

      Volume: 3 Issue: 10 Pages: 1000196-1000196

    • DOI

      10.4172/2153-2435.1000196

    • Related Report
      2012 Annual Research Report
    • Peer Reviewed
  • [Journal Article] A new protocol to discover novel anti-aging compounds2012

    • Author(s)
      F. Uchiumi, T. Oyama, K. Ozaki, M. Fukui, H. Ogawa, Y. Sasaki, H. Tachibana, C. Fukushima, M. Fujikawa, H. Abe, S. Larsen, S. Tanuma
    • Journal Title

      Pharmaceutica Analytica Acta

      Volume: 3 Issue: 07 Pages: 166-166

    • DOI

      10.4172/2153-2435.1000166

    • Related Report
      2012 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Effects of thujaplicins on the promoter activities of the human SIRT1 and telomere maintenance factor encoding genes2012

    • Author(s)
      F. Uchiumi, H. Tachibana, H. Abe, A. Yoshimori , T. Kamiya, M. Fujikawa, S. Larsen, A. Honma, S. Ebizuka, S. Tanuma.
    • Journal Title

      Pharmaceutica Analytica Acta

      Volume: 3 Issue: 05 Pages: 159-159

    • DOI

      10.4172/2153-2435.1000159

    • Related Report
      2012 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Effect of lignin glycosides extracted from pine cones on the human SIRT1 promoter2012

    • Author(s)
      Fumiaki Uchiumi, Haruki Tachibana, Steven Larsen, Sei-ichi Tanuma
    • Journal Title

      Pharmaceutica Analytica Acta

      Volume: S8 Pages: 1-1

    • Related Report
      2012 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Structure-based design of dipeptide derivatives for the human neutral endopeptidase.2011

    • Author(s)
      Misawa K、 Suzuki Y、 Takahashi S、 Yoshimori A、Takasawa R、 Shibuya Y、 Tanuma S.
    • Journal Title

      Bioorg Med Chem.

      Volume: 19(20) Pages: 5935-47

    • Related Report
      2012 Final Research Report
    • Peer Reviewed
  • [Journal Article] Discovery of a new type inhibitor of human glyoxalase I by myricetin-based 4-point pharmacophore.2011

    • Author(s)
      Takasawa R、Tao A、 Saeki K、 Shionozaki N、 Tanaka R、 Uchiro H、 Takahashi S、 Yoshimori A、 Tanuma S.
    • Journal Title

      Bioorg Med Chem Lett

      Volume: 21(14) Pages: 4337-42

    • Related Report
      2012 Final Research Report
    • Peer Reviewed
  • [Journal Article] Cancer susceptibility polymorphism of p53 at codon 72 affects phosphorylation and degradation of p53 protein2011

    • Author(s)
      Ozeki C、 Sawai Y、 Shibata T、 Kohno T、 Okamoto K、 Yokota J、 Tashiro F、 Tanuma S、Sakai R、 Kawase T、 Kitabayashi I、 Taya Y、
    • Journal Title

      J Biol Chem

      Volume: 286(20) Pages: 18251-60

    • Related Report
      2012 Final Research Report
    • Peer Reviewed
  • [Journal Article] DR396、 an apoptotic DNase γ inhibitor、attenuates high mobility group box 1 release from apoptotic cells.2011

    • Author(s)
      Yamada Y、Fujii T、 Ishijima R、 Tachibana H、 Yokoue N、Takasawa R、Tanuma S.
    • Journal Title

      BioorgMed Chem.

      Volume: 19(1) Pages: 168-71

    • Related Report
      2012 Final Research Report
    • Peer Reviewed
  • [Journal Article] Structure-based design of dipeptide derivatives for the human neutral endopeptidase2011

    • Author(s)
      Misawa K, Suzuki Y, Takahashi S, Yoshimori A, Takasawa R, Shibuya Y, Tanuma S
    • Journal Title

      Bioorg Med Chem

      Volume: 19 Pages: 5935-5947

    • Related Report
      2011 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Discovery of a new type inhibitor of human glyoxalase I by myricetin-based 4-point pharmacophore2011

    • Author(s)
      Takasawa R, Tao A, Saeki K, Shionozaki N, Tanaka R, Uchiro H, Takahashi S, Yoshimori A
    • Journal Title

      Bioorg Med Chem Lett

      Volume: 21 Pages: 4337-4342

    • Related Report
      2011 Annual Research Report
    • Peer Reviewed
  • [Journal Article] DR396, an apoptotic DNase γ inhibitor, attenuates high mobility group box 1 release from apoptotic cells.2011

    • Author(s)
      Yamada Y, Fujii T, Ishijima R, Tachibana H, Yokoue N, Takasawa R, Tanuma S.
    • Journal Title

      Bioorg Med Chem.

      Volume: VOL.19 Pages: 168-171

    • Related Report
      2010 Annual Research Report
    • Peer Reviewed
  • [Journal Article] The release of high mobility group box1 in apoptosis is triggered by nucleosomal DNA fragmentation.2010

    • Author(s)
      Yamada Y、Fujii T、 Ishijima R、 Tachibana H、 Yokoue N、 Takasawa R、 Tanuma S.
    • Journal Title

      Arch Biochem Biophys.

    • Related Report
      2012 Final Research Report
    • Peer Reviewed
  • [Journal Article] Enhancement of paclitaxel-induced apoptosis in HER2-overexpressing human breast cancer cells by a pertuzumab mimetic peptide、 HRAP.2010

    • Author(s)
      Nakajima H、 Mizuta N、 Sakaguchi K、 Fujiwara I、Yoshimori A、 Magae J、Tanuma S.
    • Journal Title

      J Biosci Bioeng

      Volume: 110(2) Pages: 250-3

    • Related Report
      2012 Final Research Report
    • Peer Reviewed
  • [Journal Article] Characterization of the promoter region of the human IGHMBP2 (Smubp-2) gene and its response to TPA in HL-60 cells2010

    • Author(s)
      Uchiumi F、 Enokida K、 Shiraishi T、 Masumi A、 Tanuma S.
    • Journal Title

      Gene.

      Volume: 463(1-2) Pages: 8-17

    • Related Report
      2012 Final Research Report
    • Peer Reviewed
  • [Journal Article] Structural insights into the hot spot amino acid residues of mushroom tyrosinase for the bindings of thujaplicins.2010

    • Author(s)
      Takahashi S, Kamiya T, Saeki K, Nezu T, Takeuchi S, Takasawa R, Sunaga S, Yoshimori A, Ebizuka S, Abe T, Tanuma S.
    • Journal Title

      Bioorg Med Chem.

      Volume: VOL.18 Pages: 8112-8118

    • Related Report
      2010 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Delphinidin, a dietary anthocyanidin in berry fruits, inhibits human glyoxalase I.2010

    • Author(s)
      Takasawa R, Saeki K, Tao A, Yoshimori A, Uchiro H, Fujiwara M, Tanuma S.
    • Journal Title

      Bioorg Med Chem.

      Volume: VOL.18 Pages: 7029-7033

    • Related Report
      2010 Annual Research Report
    • Peer Reviewed
  • [Presentation] in silico 手法を用いた新規 HMGB1/RAGE新規 HMGB1/RAGE2012

    • Author(s)
      横上 菜月、 橘 晴輝、 手井 祐太、 吉森 篤史、 高澤涼子、 藤川 誠、田沼 靖一
    • Organizer
      第85回日本生化学会大会
    • Place of Presentation
      福岡国際会議場等
    • Related Report
      2012 Final Research Report
  • [Presentation] アポトーシス制御を標的としたin silico創薬2012

    • Author(s)
      田沼靖一
    • Organizer
      第30回日本ヒト細胞学会学術集会
    • Place of Presentation
      梅田スカイビル
    • Related Report
      2012 Final Research Report
  • [Presentation] p53アイソフォームΔ1stTAD-p53の機能解析と標的遺伝子の同定2012

    • Author(s)
      鈴木 詩織, 小関 知子, 堤 修一, 川瀬 竜也, 大出 祥子, 田沼 靖一, 油谷 浩幸, 並木 秀男, 大木 理恵子
    • Organizer
      第35回日本分子生物学会年会
    • Place of Presentation
      福岡国際会議場、マリンメッセ福岡
    • Related Report
      2012 Annual Research Report
  • [Presentation] 癌抑制遺伝子p53を標的とした新規抗癌剤の創製2012

    • Author(s)
      清水 美来, 松本 真悠子, 高木 基樹, 新家 一男, 田沼 靖一, 並木 秀雄, 大木 理恵子
    • Organizer
      第35回日本分子生物学会年会
    • Place of Presentation
      福岡国際会議場、マリンメッセ福岡
    • Related Report
      2012 Annual Research Report
  • [Presentation] 細胞死におけるポリ(ADP-リボシル)化の役割2012

    • Author(s)
      加藤 侑香, 太田 諒, 阿部 英明, 藤川 誠, 高澤 涼子, 田沼 靖一
    • Organizer
      第85回日本生化学会大会
    • Place of Presentation
      福岡国際会議場、マリンメッセ福岡
    • Related Report
      2012 Annual Research Report
  • [Presentation] in silico 手法を用いた新規HMGB1/RAGE結合阻害剤の創製2012

    • Author(s)
      横上 菜月, 橘 晴輝, 手井 祐太, 吉森 篤史, 高澤 涼子, 藤川 誠, 田沼 靖一
    • Organizer
      第85回日本生化学会大会
    • Place of Presentation
      福岡国際会議場、マリンメッセ福岡
    • Related Report
      2012 Annual Research Report
  • [Presentation] Omi/HtrA2によるGSK-3β限定分解の生理的意義の解明2012

    • Author(s)
      衛藤 慎一, 西岡 隼哉, 木下 裕太朗, 藤川 誠, 高澤 涼子, 田沼 靖一
    • Organizer
      第85回日本生化学会大会
    • Place of Presentation
      福岡国際会議場、マリンメッセ福岡
    • Related Report
      2012 Annual Research Report
  • [Presentation] 重複GGAA及びGC-box配列を含む人工プロモーター配列の構築2012

    • Author(s)
      秋山 良介, 谷浦 正尚, 飯嶋 努, スティーブン ラーセン, 田沼 靖一, 内海 文彰
    • Organizer
      第85回日本生化学会大会
    • Place of Presentation
      福岡国際会議場、マリンメッセ福岡
    • Related Report
      2012 Annual Research Report
  • [Presentation] Geranylgeranylacetone (GGA)の経肛門投与はマウスにおけるDSS腸炎を軽快させる2012

    • Author(s)
      高田朋美, 田沼靖一, 谷中昭典
    • Organizer
      第40回日本潰瘍学会
    • Place of Presentation
      京王プラザホテル
    • Related Report
      2012 Annual Research Report
  • [Presentation] アポトーシス制御とin silico創薬2012

    • Author(s)
      田沼靖一
    • Organizer
      第85回日本生化学会大会 メルク株式会社ランチョンセミナー
    • Place of Presentation
      福岡国際会議場、マリンメッセ福岡
    • Related Report
      2012 Annual Research Report
  • [Presentation] In silico 手法を用いた HMGB1/RAGE 相互作用部位の同定2011

    • Author(s)
      橘晴輝、藤井拓、横上菜月、石嶋麗、手井祐太、吉森篤史、高澤涼子、田沼靖一、
    • Organizer
      第34回日本分子生物学会年会
    • Place of Presentation
      パシフィコ横浜
    • Related Report
      2012 Final Research Report
  • [Presentation] タンパク質相互作用を標的としたin silico創薬方法論の実践2011

    • Author(s)
      田沼 靖一
    • Organizer
      第39回日本潰瘍学会
    • Place of Presentation
      つくば国際会議場
    • Related Report
      2012 Final Research Report
  • [Presentation] XIAP アンタゴニストin silico設計による新規制がん剤リード化合物の創製2011

    • Author(s)
      田沼 靖一
    • Organizer
      日本がん分子標的治療学会 第7回トランスレーショナルリサーチワークショップ
    • Place of Presentation
      都市センターホテル コスモホールII
    • Related Report
      2012 Final Research Report
  • [Presentation] Design and Synthesis of Apoptosis-Inducing Agents Bearing Chelation Linkers for Intracellular Metal Cations2010

    • Author(s)
      Tsukamoto M 、 Nakamura Y 、 Suzuki A 、Takasawa R、 Morita A、Kitamura M、 Tanuma S、 Ikekita、 M、 Aoki S
    • Organizer
      Pacifichem2010
    • Place of Presentation
      ハワイコンベンションセンターおよびシェラトンワイキキ、ヒルトンハワイアンビレッジ他、アメリカ
    • Year and Date
      2010-11-20
    • Related Report
      2012 Final Research Report
  • [Book] 東京理科大学坊ちゃん科学シリーズ 第4巻 生命科学がひらく未来2013

    • Author(s)
      田沼靖一,村上康文,秋本和憲,内海文彰
    • Total Pages
      183
    • Publisher
      東京書籍
    • Related Report
      2012 Annual Research Report
  • [Book] 第3版 マクマリー 生物有機化学 生化学編2013

    • Author(s)
      今西武,上田実,大澤貫寿,奥忠武,菅原二三男,多田全宏,田沼靖一,浪越通夫,平田敏文、、藤井政幸
    • Total Pages
      937
    • Publisher
      丸善出版
    • Related Report
      2012 Annual Research Report
  • [Book] いのちの不思議を探そう! 生命科学の大研究 遺伝子からiPS細胞・死生観まで2012

    • Author(s)
      田沼靖一
    • Total Pages
      63
    • Publisher
      PHP研究所
    • Related Report
      2012 Final Research Report
  • [Book] 學鐙 夏号 特集 社会の中の科学2012

    • Author(s)
      岡田拓司,横山広美,長瀧重信,安井至,田沼靖一,太田隆夫,藤島昭
    • Total Pages
      64
    • Publisher
      丸善出版
    • Related Report
      2012 Annual Research Report
  • [Book] いのちの不思議を探そう! 生命科学の大研究 遺伝子からips細胞、死生観まで2012

    • Author(s)
      田沼靖一
    • Total Pages
      63
    • Publisher
      PHP研究所
    • Related Report
      2012 Annual Research Report
  • [Book] ヒトはどうして死ぬのか-死の遺伝子の謎2010

    • Author(s)
      田沼靖一
    • Total Pages
      173
    • Publisher
      幻冬舎
    • Related Report
      2012 Final Research Report

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Published: 2010-08-23   Modified: 2019-07-29  

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