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Integrated medicinal chemistry research of intractable diseases based on peptidic small molecules

Research Project

Project/Area Number 23390029
Research Category

Grant-in-Aid for Scientific Research (B)

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

Principal Investigator

HAYASHI Yoshio  東京薬科大学, 薬学部, 教授 (10322562)

Co-Investigator(Kenkyū-buntansha) 山崎 有理  東京薬科大学, 薬学部, 助教 (70459725)
Project Period (FY) 2011-04-01 – 2015-03-31
Project Status Completed (Fiscal Year 2014)
Budget Amount *help
¥18,200,000 (Direct Cost: ¥14,000,000、Indirect Cost: ¥4,200,000)
Fiscal Year 2014: ¥3,770,000 (Direct Cost: ¥2,900,000、Indirect Cost: ¥870,000)
Fiscal Year 2013: ¥3,640,000 (Direct Cost: ¥2,800,000、Indirect Cost: ¥840,000)
Fiscal Year 2012: ¥4,810,000 (Direct Cost: ¥3,700,000、Indirect Cost: ¥1,110,000)
Fiscal Year 2011: ¥5,980,000 (Direct Cost: ¥4,600,000、Indirect Cost: ¥1,380,000)
Keywords薬学 / 創薬化学 / 生体分子 / ペプチド化学 / 有機化学 / 抗がん剤 / 難治性疾患 / リードスルー薬 / プロドラッグ / 遺伝子疾患治療薬 / システインプロテアーゼ阻害剤 / 固相ジスルフィド縮合法 / システインプロテーアゼ阻害剤 / ペプチド創薬
Outline of Final Research Achievements

Paying attention to the peptidic small molecule in which diverse pharmacological activity is expected, we performed a series of new integrated medicinal chemistry research to overcome intractable diseases such as cancer, genetic diseases and emerging infectious diseases.
Specific challenges are: (1) the design and synthesis of next-generation compounds of vascular disrupting agent (VDA) plinabulin which was developed by our group and is now in clinical trial, and the improvement of plinabulin as a prodrug that increases water-solubility and cancer tissue selectivity, (2) Development of a new chemotherapy for the treatment of nonsense-mediated genetic disease through the design and synthesis of new derivatives of natural product negamycin, which has a strong read-through activity, and (3) the design and synthesis of dipeptide type cysteine protease inhibitor for development of chemotherapy against severe acute respiratory syndrome (SARS).

Report

(5 results)
  • 2014 Annual Research Report   Final Research Report ( PDF )
  • 2013 Annual Research Report
  • 2012 Annual Research Report
  • 2011 Annual Research Report
  • Research Products

    (108 results)

All 2015 2014 2013 2012 2011 Other

All Journal Article (18 results) (of which Peer Reviewed: 17 results,  Acknowledgement Compliant: 3 results) Presentation (76 results) (of which Invited: 6 results) Book (3 results) Remarks (4 results) Patent(Industrial Property Rights) (7 results) (of which Overseas: 3 results)

  • [Journal Article] Identification of the Minimum Peptide from Mouse Myostatin Prodomain for Human Myostatin Inhibition2015

    • Author(s)
      Kentaro Takayama
    • Journal Title

      J Med Chem

      Volume: 58 Pages: 1544-1549

    • Related Report
      2014 Annual Research Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] Preparation of disulfide type prodrug of Plinabulin for antibody-drug conjugate2015

    • Author(s)
      Kyouhei Muguruma
    • Journal Title

      Peptide Science 2014, The Japanese Peptide Society (2015) in press

      Volume: 2014 Pages: 245-246

    • Related Report
      2014 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Development of cyclic didehydrodipeptide-type novel anti-microtubule agents possessing 2-pyridyl and benzophenone structures2015

    • Author(s)
      Yoshiki Hayashi
    • Journal Title

      Peptide Science 2014, The Japanese Peptide Society (2015) in press

      Volume: 2014 Pages: 243-244

    • Related Report
      2014 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Discovery of Natural Products Possessing Selective Eukaryotic Readthrough Activity: 3-epi-Deoxynegamycin and its Leucine Adduct2014

    • Author(s)
      Akihiro Taguchi
    • Journal Title

      Chem. Med. Chem

      Volume: 9 Pages: 2233-2237

    • Related Report
      2014 Annual Research Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] Development of a New Benzophenone-diketopiperazine-type Potent Anti-microtubule Agent Possessing a 2-Pyridine Structure2014

    • Author(s)
      Yoshiki Hayashi
    • Journal Title

      ACS Med Chem Lett

      Volume: 5 Pages: 1094-1098

    • Related Report
      2014 Annual Research Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] Design, synthesis, and biological evaluation of novel dipeptide-type SARS-CoV 3CL protease inhibitors: Structure–activity relationship study2013

    • Author(s)
      Pillaiyar Thanigaimalai
    • Journal Title

      Euro. J. Med. Chem

      Volume: 65 Pages: 436-447

    • Related Report
      2013 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Development of potent dipeptide-type SARS-CoV 3CL protease inhibitors with novel P3 scaffolds: Design, synthesis, biological evaluation, and docking studies2013

    • Author(s)
      Pillaiyar Thanigaimalai
    • Journal Title

      Euro. J. Med. Chem

      Volume: 68 Pages: 372-384

    • Related Report
      2013 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Medicinal chemistry and chemical biology of diketopiperazine-type anti-microtubule and vascular disrupting agents2013

    • Author(s)
      Yoshio Hayashi
    • Journal Title

      Chem. Pharm. Bull

      Volume: 61 Pages: 889-901

    • NAID

      130003360830

    • Related Report
      2013 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Design and synthesis of new tripeptide-type SARS-CoV 3CL protease inhibitors containing an electrophilic arylketone moiety2013

    • Author(s)
      Sho Konno
    • Journal Title

      Bioorganic Medicinal Chemistry

      Volume: 21 Pages: 412-424

    • Related Report
      2012 Annual Research Report
    • Peer Reviewed
  • [Journal Article] An Effective Click Strategy For Water-Soluble Prodrug of the Antimicrotubule Agent ‘Plinabulin’2013

    • Author(s)
      Fumika Yakushiji
    • Journal Title

      Peptide Science 2012

      Volume: 2012 Pages: 7-8

    • Related Report
      2012 Annual Research Report
  • [Journal Article] Structure Activity Relationship Study of Dipeptide Antibiotic (+)-Negamycin for the Potent Readthrough Promoting Activity2013

    • Author(s)
      Akihiro Taguchi
    • Journal Title

      Peptide Science 2012

      Volume: 2012 Pages: 205-206

    • Related Report
      2012 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Prodrug Study of Plinabulin Using a Click Strategy Focused on the Effects of a Replaceable Water-Solubilizing Moiety2012

    • Author(s)
      Fumika Yakushiji
    • Journal Title

      Chemical and Pharmaceutical Bulletin

      Volume: 60 Issue: 7 Pages: 877-881

    • DOI

      10.1248/cpb.c12-00216

    • NAID

      130001852497

    • ISSN
      0009-2363, 1347-5223
    • Related Report
      2012 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Synthesis and structure activity relationships of benzophenone-bearing diketopiperazine-type anti-microtubule agents2012

    • Author(s)
      Yamazaki Y, Sumikura M, Masuda Y, Hayashi Y, Yasui H, Kiso Y, Chinen T, Usui T, Yakushiji F, Potts B, Neuteboom S, Palladino M, Lloyd GK, Hayashi Y.
    • Journal Title

      Bioorganic Medicinal Chemisty

      Volume: 20 Issue: 14 Pages: 4279-4289

    • DOI

      10.1016/j.bmc.2012.05.059

    • Related Report
      2012 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Unusual expression of red fluorescence at M phase induced by anti-microtubule agents in HeLa cells expressing the fluorescent ubiquitination-based cell cycle indicator (Fucci)2012

    • Author(s)
      Asumi Honda-Uezono
    • Journal Title

      Biochem. Biophys. Res. Commun

      Volume: 428 Issue: 2 Pages: 224-229

    • DOI

      10.1016/j.bbrc.2012.10.014

    • Related Report
      2012 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Synthesis and Structure-Activity Relationship Study of Antimicrotubule Agents Phenylahistin Derivatives with a Didehydropiperazine-2,5-dione Structure2012

    • Author(s)
      Y.Yamazaki
    • Journal Title

      Journal of Medicinal Chemistry

      Volume: 55 Issue: 3 Pages: 1056-1071

    • DOI

      10.1021/jm2009088

    • Related Report
      2011 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Negamycin Analogue with Readthrough-Promoting Activity as a Potential Drug Candidate for Duchenne Muscular Dystrophy2012

    • Author(s)
      Akihiro Taguchi, Yoshio Hayashi, 他10人
    • Journal Title

      ACS Med.Chem.Lett.

      Volume: 3 Pages: 118-122

    • Related Report
      2011 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Water-Soluble Prodrug of Antimicrotubule Agent Plinabulin : Effective strategy with Click Chemistry2011

    • Author(s)
      Fumika Yakushiji, Yoshio Hayashi, 他4人
    • Journal Title

      Chemistry-A European Journal

      Volume: 17 Issue: 45 Pages: 12587-12590

    • DOI

      10.1002/chem.201102293

    • Related Report
      2011 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Development of [Ile40] HTLV-I protease inhibition assay using novel fluorogenic and chromogenic substrate2011

    • Author(s)
      Henri-Obadja Kumada, Yoshio Hayashi Yoshiaki Kiso, 他4人
    • Journal Title

      Journal Peptide Science

      Volume: 17 Pages: 569-575

    • Related Report
      2011 Annual Research Report
    • Peer Reviewed
  • [Presentation] 筋肉機能を強化するマイオスタチン阻害ペプチドのアラニンスキャンと二次構造解析2015

    • Author(s)
      高山 健太郎
    • Organizer
      日本薬学会第135年会
    • Place of Presentation
      神戸
    • Year and Date
      2015-03-25
    • Related Report
      2014 Annual Research Report
  • [Presentation] Development of (+)-negamycin-derived ester-type prodrugs promoting premature termination codon-readthrough and its application for supressing cancer cell growth2014

    • Author(s)
      Kentaro Takayama
    • Organizer
      The 2014 ASCB/IFCB Meeting
    • Place of Presentation
      Philadelphia, USA
    • Year and Date
      2014-12-06
    • Related Report
      2014 Annual Research Report
  • [Presentation] ピリジンおよびベンゾフェノン構造を有する環状ジデヒドロジペプチド型新規微小管脱重合剤の創製2014

    • Author(s)
      林 良樹
    • Organizer
      第 51 回ペプチド討論会
    • Place of Presentation
      徳島
    • Year and Date
      2014-10-22
    • Related Report
      2014 Annual Research Report
  • [Presentation] Plinabulinジスルフィド型プロドラッグの合成とその抗体薬物複合体への応用2014

    • Author(s)
      六車 共平
    • Organizer
      第 51 回ペプチド討論会
    • Place of Presentation
      徳島
    • Year and Date
      2014-10-22
    • Related Report
      2014 Annual Research Report
  • [Presentation] マイオスタチン阻害ペプチドの最小配列同定と二次構造解析2014

    • Author(s)
      淺利 知
    • Organizer
      第 58 回日本薬学会関東支部大会
    • Place of Presentation
      東京
    • Year and Date
      2014-10-04
    • Related Report
      2014 Annual Research Report
  • [Presentation] エステル型ネガマイシン誘導体の合成とそのリードスルー活性評価2014

    • Author(s)
      会田 俊
    • Organizer
      第 58 回日本薬学会関東支部大会
    • Place of Presentation
      東京
    • Year and Date
      2014-10-04
    • Related Report
      2014 Annual Research Report
  • [Presentation] Development of Didehydrocyclic Dipeptide-type Anti-Microtubule Agents with a 2-Pyridine Ring2014

    • Author(s)
      Yoshiki Hayashi
    • Organizer
      33rd European Peptide Symposium
    • Place of Presentation
      Sofia, Bulgaria
    • Year and Date
      2014-08-31
    • Related Report
      2014 Annual Research Report
  • [Presentation] Alanine Scan Study of Myostatin Inhibitory α-Helical Peptide2014

    • Author(s)
      Syota Takayama
    • Organizer
      33rd European Peptide Symposium
    • Place of Presentation
      Sofia, Bulgaria
    • Year and Date
      2014-08-31
    • Related Report
      2014 Annual Research Report
  • [Presentation] Structure Activity Relationship Study of (+)-Negamycin for Readthrough Activity at Duchenne Muscular Dystrophy2014

    • Author(s)
      Akihiro Taguchi
    • Organizer
      33rd European Peptide Symposium
    • Place of Presentation
      Sofia, Bulgaria
    • Year and Date
      2014-08-31
    • Related Report
      2014 Annual Research Report
  • [Presentation] Identification of Small Myostatin Inhibitory Peptides2014

    • Author(s)
      Kentaro Takayama
    • Organizer
      33rd European Peptide Symposium
    • Place of Presentation
      Sofia, Bulgaria
    • Year and Date
      2014-08-31
    • Related Report
      2014 Annual Research Report
  • [Presentation] 2-ピリジル環を有する新規ベンゾフェノン–ジケトピペラジン型微小管重合阻害剤の創製2014

    • Author(s)
      林 良樹
    • Organizer
      創薬懇話会2014
    • Place of Presentation
      岐阜
    • Year and Date
      2014-07-10
    • Related Report
      2014 Annual Research Report
  • [Presentation] 微小管重合阻害剤Plinabulinの抗体-薬物複合体型プロドラッグ創製研究2014

    • Author(s)
      六車 共平
    • Organizer
      創薬懇話会2014
    • Place of Presentation
      岐阜
    • Year and Date
      2014-07-10
    • Related Report
      2014 Annual Research Report
  • [Presentation] 筋肉機能強化を目指したマイオスタチン阻害ペプチドのアラニンスキャンによる構造活性相関研究2014

    • Author(s)
      高山 翔太
    • Organizer
      創薬懇話会2014
    • Place of Presentation
      岐阜
    • Year and Date
      2014-07-10
    • Related Report
      2014 Annual Research Report
  • [Presentation] ジペプチド型 SARS-CoV 3CL プロテアーゼ阻害剤の創製研究 - P3 位における構造活性相関2014

    • Author(s)
      山本 剛史
    • Organizer
      創薬懇話会2014
    • Place of Presentation
      岐阜
    • Year and Date
      2014-07-10
    • Related Report
      2014 Annual Research Report
  • [Presentation] Structure activity relationship study of (+)- negamycin derivatives at the C-terminal part as a readthrough drug2014

    • Author(s)
      Keisuke Hamada
    • Organizer
      18th Korean Peptide Protein Sympodium
    • Place of Presentation
      Busan, South Korea
    • Year and Date
      2014-07-07
    • Related Report
      2014 Annual Research Report
  • [Presentation] 微小管を標的とした新規ジケトピペラジン型有糸分裂阻害剤の創製2014

    • Author(s)
      林 良樹
    • Organizer
      第18回日本がん分子標的治療学会学術集会
    • Place of Presentation
      仙台
    • Year and Date
      2014-06-25
    • Related Report
      2014 Annual Research Report
  • [Presentation] 微小管作用薬Plinabulinの光親和性ビオチン化プローブの開発とそれらを利用した結合様式解析2012

    • Author(s)
      山崎有理、林良雄, 他6名
    • Organizer
      日本薬学会第132年会
    • Place of Presentation
      札幌
    • Year and Date
      2012-03-31
    • Related Report
      2011 Annual Research Report
  • [Presentation] ベンゾフェノン構造を有するジケトピペラジン型微小管作用薬の構造活性相関研究2012

    • Author(s)
      山崎有理, 林良雄, 他8名
    • Organizer
      日本薬学会第132年会
    • Place of Presentation
      札幌
    • Year and Date
      2012-03-31
    • Related Report
      2011 Annual Research Report
  • [Presentation] Plinabulinの水溶性プロドラッグ合成研究:水溶性置換基の寄与について2012

    • Author(s)
      六車共平、林良雄, 他3名
    • Organizer
      日本薬学会第132年会
    • Place of Presentation
      札幌
    • Year and Date
      2012-03-30
    • Related Report
      2011 Annual Research Report
  • [Presentation] クリックケミストリーを用いたチューブリン重合阻害剤Plinabulinの水溶性プロドラッグ合成研究2012

    • Author(s)
      田中達也、林良雄, 他4名
    • Organizer
      日本薬学会第132年会
    • Place of Presentation
      札幌
    • Year and Date
      2012-03-29
    • Related Report
      2011 Annual Research Report
  • [Presentation] トリペプチド型SARSコロナウイルス3CLプロテアーゼ阻害剤の開発-P4部位における構造活性相関研究-2012

    • Author(s)
      山本剛史、林良雄, 他10名
    • Organizer
      日本薬学会第132年会
    • Place of Presentation
      札幌
    • Year and Date
      2012-03-29
    • Related Report
      2011 Annual Research Report
  • [Presentation] Medicinal chemistry of small peptidic natural products against intractable diseases2011

    • Author(s)
      林良雄
    • Organizer
      The East Japan Scripps Biomedical Forum 2011
    • Place of Presentation
      東京
    • Year and Date
      2011-12-03
    • Related Report
      2011 Annual Research Report
  • [Presentation] Medicinal chemistry of small peptidic natural products against intractable diseases2011

    • Author(s)
      Yoshio Hayashi, Fumika Yakushiji, 他4人
    • Organizer
      8th AFMC International Medicinal Chemistry Symposium
    • Place of Presentation
      東京
    • Year and Date
      2011-12-02
    • Related Report
      2011 Annual Research Report
  • [Presentation] Water-soluble Prodrug of Anti-microtubule Agent 'Plinabulin' : Unique Monolactim System with Click Chemistry with Click Chemistry2011

    • Author(s)
      Fumika Yakushiji, Yoshio Hayashi, 他4人
    • Organizer
      8th AFMC International Medicinal Chemistry Symposium
    • Place of Presentation
      東京
    • Year and Date
      2011-12-01
    • Related Report
      2011 Annual Research Report
  • [Presentation] Synthesis and Biological Evaluation of Didehydro-type Tryprostatin B Derivatives2011

    • Author(s)
      Yuki Shinozaki, Yoshio Hayash, 他4人
    • Organizer
      8th AFMC International Medicinal Chemistry Symposium
    • Place of Presentation
      東京
    • Year and Date
      2011-12-01
    • Related Report
      2011 Annual Research Report
  • [Presentation] Development of SARS Coronavirus 3CL Protease Inhibitors with an Electrophilic Aryl Ketone Structure2011

    • Author(s)
      Sho Konno, Yoshio Hayashi, 他10人
    • Organizer
      8th AFMC International Medicinal Chemistry Symposium
    • Place of Presentation
      東京
    • Year and Date
      2011-12-01
    • Related Report
      2011 Annual Research Report
  • [Presentation] Development of Readthrough Peptidemimetics from Dipeptidic Antibiotics (+)-Negamycin for Duchenne Muscular Dystrophy Chemotherapy2011

    • Author(s)
      Akihiro Taguchi, Yoshio Hayashi, 他7人
    • Organizer
      8th AFMC International Medicinal Chemistry Symposium
    • Place of Presentation
      東京
    • Year and Date
      2011-12-01
    • Related Report
      2011 Annual Research Report
  • [Presentation] ジケトピペラジン型微小管重合阻害剤'Plinabulin'の水溶性プロドラッグ合成研究2011

    • Author(s)
      薬師寺文華, 林良雄, 他4名
    • Organizer
      第31回反応と合成の進歩シンポジウム
    • Place of Presentation
      徳島
    • Year and Date
      2011-11-08
    • Related Report
      2011 Annual Research Report
  • [Presentation] DESIGN, SYNTHESIS, AND EVALUATION OF TRIPEPTIDEMIMETICS WITH ARYLKETONE AS INHIBITORS OF SARS-COV 3CL PROTEASE2011

    • Author(s)
      Sho Konno, Yoshio Hayashi, 他11名
    • Organizer
      第48回ペプチド討論会
    • Place of Presentation
      札幌
    • Year and Date
      2011-09-28
    • Related Report
      2011 Annual Research Report
  • [Presentation] デュシェンヌ型ジストロフィー治療薬を目指した高リードスルー活性を有するネガマイシン誘導体研究2011

    • Author(s)
      田口晃弘、林良雄, 他4名
    • Organizer
      第48回ペプチド討論会
    • Place of Presentation
      札幌
    • Year and Date
      2011-09-27
    • Related Report
      2011 Annual Research Report
  • [Presentation] SARS-コロナウイルス3CLプロテアーゼ阻害剤のP4位における構造活性相関2011

    • Author(s)
      仲田聖彦、林良雄, 他8名
    • Organizer
      第16回日本病態プロテアーゼ学会学術集会
    • Place of Presentation
      大阪
    • Year and Date
      2011-08-26
    • Related Report
      2011 Annual Research Report
  • [Presentation] 天然由来ペプチド様小分子に基づく難病治療薬の創製研究2011

    • Author(s)
      林良雄
    • Organizer
      CBI学会第318回研究講演会
    • Place of Presentation
      東京
    • Year and Date
      2011-07-05
    • Related Report
      2011 Annual Research Report
  • [Presentation] Development of readthough peptides from dipeptidic antibiotics (+)-negamycin for Duchenne muscular dystrophy chemotherapy2011

    • Author(s)
      Yoshio Hayashi, 他9人
    • Organizer
      22nd American Peptide Symposium
    • Place of Presentation
      San Diego, USA
    • Year and Date
      2011-06-29
    • Related Report
      2011 Annual Research Report
  • [Presentation] Development of biotin-tagged plinabulin chemical probes towards the elucidation of binding mechanism of a diketopiperazine based anti-microtubule agent2011

    • Author(s)
      Yuri Yamazaki, Yoshio Hayashi, 他6人
    • Organizer
      22nd American Peptide Symposium
    • Place of Presentation
      San Diego, USA
    • Year and Date
      2011-06-29
    • Related Report
      2011 Annual Research Report
  • [Presentation] Synthesis and Structure Activity Relationship Study of Didehydro-derivatives of a Natural Diketopiperazine Tryprostatin2011

    • Author(s)
      Yuki Shinozaki, Yoshio Hayashi, 他4人
    • Organizer
      22nd American Peptide Symposium
    • Place of Presentation
      San Diego, USA
    • Year and Date
      2011-06-29
    • Related Report
      2011 Annual Research Report
  • [Presentation] ジケトピペラジン型微小管重合阻害剤Plinabulinの水溶性プロドラッグ開発研究2011

    • Author(s)
      薬師寺文華、山崎有理、林良雄
    • Organizer
      第15回日本がん分子標的治療学会学術集会
    • Place of Presentation
      東京
    • Year and Date
      2011-06-23
    • Related Report
      2011 Annual Research Report
  • [Presentation] 微小管作用薬Plinabulinのケミカルプローブの開発とそれらを利用した結合様式解析2011

    • Author(s)
      山崎有理、林良雄, 他6人
    • Organizer
      日本ケミカルバイオロジー学会第6回年会
    • Place of Presentation
      東京
    • Year and Date
      2011-05-24
    • Related Report
      2011 Annual Research Report
  • [Presentation] "Plinabulin" a Vascular Targeting Anti-cancer Agent Derived from Natural Diketopiperazine "Phenylahistin/Halimide2011

    • Author(s)
      Yoshio Hayashi
    • Organizer
      BIT'S 1st Annual World Congress of Marine Biotechnology
    • Place of Presentation
      Dalian, China
    • Year and Date
      2011-04-28
    • Related Report
      2011 Annual Research Report
  • [Presentation] Identification of myostatin inhibitory peptides from mouse myostatin prodomain

    • Author(s)
      Kentaro Takayama
    • Organizer
      4th Asia-Pacific International Peptide Symposium / 50th Japanese Peptide Symposium
    • Place of Presentation
      Osaka
    • Related Report
      2013 Annual Research Report
  • [Presentation] Preparation of non-covalent antibody-drug conjugate for tumor targeting of vascular disrupting agent “Plinabulin”

    • Author(s)
      Kyohei Muguruma
    • Organizer
      4th Asia-Pacific International Peptide Symposium / 50th Japanese Peptide Symposium
    • Place of Presentation
      Osaka
    • Related Report
      2013 Annual Research Report
  • [Presentation] Structure activity relationship study of (+)-negamycin for potent readthrough promoting activity at nonsense mutation

    • Author(s)
      Akihiro Taguchi
    • Organizer
      4th Asia-Pacific International Peptide Symposium / 50th Japanese Peptide Symposium
    • Place of Presentation
      Osaka
    • Related Report
      2013 Annual Research Report
  • [Presentation] Synthesis of a new solid-supported reagent for SH-group selective oligoarginine labeling

    • Author(s)
      Kentaro Fukumoto
    • Organizer
      4th Asia-Pacific International Peptide Symposium / 50th Japanese Peptide Symposium
    • Place of Presentation
      Osaka
    • Related Report
      2013 Annual Research Report
  • [Presentation] Structure-activity relationship study of myostatin inhibitory peptides by alanine scanning

    • Author(s)
      Syota Takayama
    • Organizer
      4th Asia-Pacific International Peptide Symposium / 50th Japanese Peptide Symposium
    • Place of Presentation
      Osaka
    • Related Report
      2013 Annual Research Report
  • [Presentation] Peptide Therapeutics for the Treatment of Muscular Diseases

    • Author(s)
      Yoshio Hayashi
    • Organizer
      9th AFMC International Medicinal Chemistry Symposium
    • Place of Presentation
      Taipei, Taiwan
    • Related Report
      2013 Annual Research Report
  • [Presentation] Discovery of Potent Readthrough Derivatives and Natural Products from Dipeptidyl Antibiotic (+)-Negamycin for the Development of Duchenne Muscular Dystrophy Drugs

    • Author(s)
      Akihiro Taguchi
    • Organizer
      Frontiers in Medicinal Chemistry 2013
    • Place of Presentation
      San Francisco, USA
    • Related Report
      2013 Annual Research Report
  • [Presentation] Development of novel potent and specific inhibitors of Myostatin signaling

    • Author(s)
      Yuri Noguchi
    • Organizer
      The 3rd International Symposium by JSPS Core-to-Core Program “Cooperative International Framework in TGF-b family Signaling”
    • Place of Presentation
      Ehime
    • Related Report
      2013 Annual Research Report
  • [Presentation] Development of New Diketopiperazine-Type Anti-Microtubule Agents with a 2-Pyridylmethylidene Structure

    • Author(s)
      Yoshiki Hayashi
    • Organizer
      2nd Annual Conference - ICBS 2013
    • Place of Presentation
      Kyoto
    • Related Report
      2013 Annual Research Report
  • [Presentation] Development of a thiol group selective solid-supported oligoarginine labeling reagent

    • Author(s)
      Kentaro Fukumoto
    • Organizer
      2nd Annual Conference - ICBS 2013
    • Place of Presentation
      Kyoto
    • Related Report
      2013 Annual Research Report
  • [Presentation] Medicinal Chemistry of Peptidic Compounds for the Treatment of Muscular Diseases

    • Author(s)
      Yoshio Hayashi
    • Organizer
      10th Australian Peptide Conference
    • Place of Presentation
      Penang, Malaysia
    • Related Report
      2013 Annual Research Report
    • Invited
  • [Presentation] Discovery of the myostatin inhibitory peptide deriving from the prodomain of mouse myostatin precursor

    • Author(s)
      Kentaro Takayama
    • Organizer
      10th Australian Peptide Conference
    • Place of Presentation
      Penang, Malaysia
    • Related Report
      2013 Annual Research Report
  • [Presentation] (+)-ネガマイシン誘導体の構造活性相関研究:リードスルー作用を主活性とする天然物の発見

    • Author(s)
      田口 晃弘
    • Organizer
      日本ケミカルバイオロジー学会第8回年会
    • Place of Presentation
      東京
    • Related Report
      2013 Annual Research Report
  • [Presentation] ミオスタチン新規阻害剤の開発

    • Author(s)
      野口 百合
    • Organizer
      平成25年度日本生化学会関東支部例会
    • Place of Presentation
      山梨
    • Related Report
      2013 Annual Research Report
  • [Presentation] ジペプチド型 SARS-CoV 3CL プロテアーゼ阻害剤の創製研究

    • Author(s)
      林 良雄
    • Organizer
      第31回メディシナルケミストリーシンポジウム
    • Place of Presentation
      広島
    • Related Report
      2013 Annual Research Report
  • [Presentation] 創薬合成研究からのリードスルー活性を有する天然物の発見

    • Author(s)
      田口 晃弘
    • Organizer
      第31回メディシナルケミストリーシンポジウム
    • Place of Presentation
      広島
    • Related Report
      2013 Annual Research Report
  • [Presentation] ピリジン環とベンゾフェノン構造を有する新規ジケトピペラジン型微小管重合阻害剤の創製

    • Author(s)
      林 良樹
    • Organizer
      第31回メディシナルケミストリーシンポジウム
    • Place of Presentation
      広島
    • Related Report
      2013 Annual Research Report
  • [Presentation] 筋肉機能を強化するマイオスタチン阻害ペプチドの創製 1:アラニンスキャンによる構造活性相関研究

    • Author(s)
      高山 翔太
    • Organizer
      第31回メディシナルケミストリーシンポジウム
    • Place of Presentation
      広島
    • Related Report
      2013 Annual Research Report
  • [Presentation] ジペプチド型 SARS-CoV 3CLpro 阻害剤の創製:P3 部位における構造活性相関研究

    • Author(s)
      小岩井 勇児
    • Organizer
      第 18 回日本病態プロテアーゼ学会学術集会
    • Place of Presentation
      大阪
    • Related Report
      2013 Annual Research Report
  • [Presentation] Medicinal Chemistry of Small Peptidic Natural Products against Intractable Diseases

    • Author(s)
      YoshioHayashi
    • Organizer
      International Conference on "Chemistry-Frontiers & Challenges"
    • Place of Presentation
      Tamil Nadu,India
    • Related Report
      2013 Annual Research Report
    • Invited
  • [Presentation] Identification of negamycin analogs with readthrough-promoting activity as potential drug candidates for Duchenne muscular dystrophy

    • Author(s)
      Akihiro Taguchi
    • Organizer
      244th American Chemical Society National Meeting & Exposition
    • Place of Presentation
      Philadelphia, USA
    • Related Report
      2012 Annual Research Report
    • Invited
  • [Presentation] Development of water-soluble prodrug of diketopiperazine-type antitumor agent “Plinabulin” by a skeletal transformation to monolactim

    • Author(s)
      Fumika Yakushiji
    • Organizer
      244th American Chemical Society National Meeting & Exposition
    • Place of Presentation
      Philadelphia, USA
    • Related Report
      2012 Annual Research Report
  • [Presentation] Development of SARS coronavirus 3CL protease inhibitors with an electrophilic aryl ketone structure

    • Author(s)
      Takehiro Yamamoto
    • Organizer
      244th American Chemical Society National Meeting & Exposition
    • Place of Presentation
      Philadelphia, USA
    • Related Report
      2012 Annual Research Report
  • [Presentation] Development of a series of diketopiperazine vascular targeting anticancer agents based on microtubule depolymerization activity

    • Author(s)
      Yoshio Hayashi
    • Organizer
      32th European Peptide Symposium
    • Place of Presentation
      Athens, Greece
    • Related Report
      2012 Annual Research Report
    • Invited
  • [Presentation] Structure activity relationship study of (+)-negamycin with readthrough-promoting activity for Duchenne muscular dystrophy chemotherapy

    • Author(s)
      Akihiro Taguchi
    • Organizer
      32th European Peptide Symposium
    • Place of Presentation
      Athens, Greece
    • Related Report
      2012 Annual Research Report
  • [Presentation] Promotion of premature termination codon-readthrough by (+)-negamycin derivatives for Duchenne muscular dystrophy chemotherapy

    • Author(s)
      Akihiro Taguchi
    • Organizer
      9th Japan-France symposium for ‘muscular dystrophy’
    • Place of Presentation
      Tokyo
    • Related Report
      2012 Annual Research Report
  • [Presentation] Medicinal Chemistry of Small Peptidic Natural Products against Genetic Diseases

    • Author(s)
      Yoshio Hayashi
    • Organizer
      14th Akabori Conference
    • Place of Presentation
      Niseko
    • Related Report
      2012 Annual Research Report
    • Invited
  • [Presentation] Peptidic cysteine protease inhibitors with an arylketone warhead for SARS Coronavirus

    • Author(s)
      Sho Konno
    • Organizer
      PEM6 (6th Peptide Engineering Meeting)
    • Place of Presentation
      Atlanta, USA
    • Related Report
      2012 Annual Research Report
  • [Presentation] Medicinal Chemistry of Small Peptidic Natural Products against Genetic Diseases

    • Author(s)
      Yoshio Hayashi
    • Organizer
      The 1st International Symposium on Chemical Biology of Natural Products: Target ID and Regulation of Bioactivity
    • Place of Presentation
      Kyoto
    • Related Report
      2012 Annual Research Report
    • Invited
  • [Presentation] (+)-Negamycin derivatives promoting premature termination codon-readthrough

    • Author(s)
      Kentaro Takayama
    • Organizer
      2012 The American Society for Cell Biology Annual Meeting
    • Place of Presentation
      San Francisco, USA
    • Related Report
      2012 Annual Research Report
  • [Presentation] 天然由来ペプチド様小分子に基づく難病治療薬の創製研究

    • Author(s)
      林 良雄
    • Organizer
      BIO tech 2012 アカデミックフォーラム
    • Place of Presentation
      東京
    • Related Report
      2012 Annual Research Report
  • [Presentation] ベンゾフェノン構造を有するジケトピペラジン型微小管重合阻害剤plinabulinの構造活性相関研究

    • Author(s)
      山崎 有理
    • Organizer
      日本ケミカルバイオロジー学会第7回年会
    • Place of Presentation
      京都
    • Related Report
      2012 Annual Research Report
  • [Presentation] ベンゾフェノン構造を有するジケトピペラジン型微小管作用薬の機能評価とそれらを利用した結合様式解析研究

    • Author(s)
      山崎 有理
    • Organizer
      第16回日本がん分子標的治療学会学術集会
    • Place of Presentation
      北九州
    • Related Report
      2012 Annual Research Report
  • [Presentation] 高リードスルー促進活性を目指したジペプチド型抗生物質ネガマイシンの構造活性相関研究

    • Author(s)
      田口 晃弘
    • Organizer
      第 49 回ペプチド討論会
    • Place of Presentation
      鹿児島
    • Related Report
      2012 Annual Research Report
  • [Presentation] 微小管重合阻害剤’PLINABULIN’の水溶性プロドラッグ創製研究:クリックケミストリーを用いた効率的手法の確立

    • Author(s)
      薬師寺 文華
    • Organizer
      第49回ペプチド討論会
    • Place of Presentation
      鹿児島
    • Related Report
      2012 Annual Research Report
  • [Presentation] プロ配列に由来するマイオスタチン阻害ペプチドの合成とその構造特性

    • Author(s)
      青木 進
    • Organizer
      日本薬学会第 133 年会
    • Place of Presentation
      横浜
    • Related Report
      2012 Annual Research Report
  • [Presentation] ナンセンス変異読み飛ばし活性に着目したネガマイシン誘導体の合成1:ネガマイシン3位アミノ基の誘導と生物活性評価

    • Author(s)
      小竹 優也
    • Organizer
      日本薬学会第 133 年会
    • Place of Presentation
      横浜
    • Related Report
      2012 Annual Research Report
  • [Presentation] ナンセンス変異読み飛ばし活性に着目したネガマイシン誘導体の合成2:ネガマイシン右翼ユニットの誘導と生物活性評価

    • Author(s)
      濱田 圭佑
    • Organizer
      日本薬学会第 133 年会
    • Place of Presentation
      横浜
    • Related Report
      2012 Annual Research Report
  • [Book] 次世代ペプチド医薬創製2014

    • Author(s)
      林 良雄、山本剛史、小岩井勇児
    • Total Pages
      140
    • Publisher
      メディカルドゥ
    • Related Report
      2014 Annual Research Report
  • [Book] ファルマシア(最前線)2014

    • Author(s)
      田口晃弘、濱田圭佑、林 良雄
    • Total Pages
      50
    • Publisher
      日本薬学会
    • Related Report
      2014 Annual Research Report
  • [Book] 遺伝子医学MOOK21号「最新ペプチド合成技術とその創薬研究への応用」2012

    • Author(s)
      山崎有理、林良雄
    • Total Pages
      7
    • Publisher
      株式会社メディカルドゥ
    • Related Report
      2011 Annual Research Report
  • [Remarks] 東京薬科大学薬学部 薬品化学教室

    • URL

      http://hinka-toyaku.s2.weblife.me/index.html

    • Related Report
      2014 Annual Research Report
  • [Remarks] 東京薬科大学薬学部 薬品化学教室

    • URL

      http://hinka-toyaku.s2.weblife.me/index.html

    • Related Report
      2013 Annual Research Report
  • [Remarks] 東京薬科大学薬学部 薬品化学教室

    • URL

      http://hinka-toyaku.s2.weblife.me/index.html

    • Related Report
      2012 Annual Research Report
  • [Remarks]

    • URL

      http://www.ps.toyaku.ac.jp/wp/yakuhinkagaku/

    • Related Report
      2011 Annual Research Report
  • [Patent(Industrial Property Rights)] マイオスタチン阻害ペプチド2014

    • Inventor(s)
      林良雄他8名
    • Industrial Property Rights Holder
      林良雄他8名
    • Industrial Property Rights Type
      特許
    • Filing Date
      2014-01-31
    • Related Report
      2013 Annual Research Report
    • Overseas
  • [Patent(Industrial Property Rights)] 新規化合物、その製造方法及びその用途2013

    • Inventor(s)
      林良雄他3名
    • Industrial Property Rights Holder
      林良雄他3名
    • Industrial Property Rights Type
      特許
    • Industrial Property Number
      2013-209166
    • Filing Date
      2013-10-04
    • Related Report
      2013 Annual Research Report
  • [Patent(Industrial Property Rights)] 微小管脱重合剤2013

    • Inventor(s)
      林良雄他4名
    • Industrial Property Rights Holder
      林良雄他4名
    • Industrial Property Rights Type
      特許
    • Industrial Property Number
      2013-159466
    • Filing Date
      2013-07-31
    • Related Report
      2013 Annual Research Report
  • [Patent(Industrial Property Rights)] マイオスタチン阻害ペプチド2013

    • Inventor(s)
      林良雄他8人
    • Industrial Property Rights Holder
      林良雄他8人
    • Industrial Property Rights Type
      特許
    • Industrial Property Number
      2013-017540
    • Filing Date
      2013-01-31
    • Related Report
      2012 Annual Research Report
  • [Patent(Industrial Property Rights)] リードスルー活性を有する化合物2012

    • Inventor(s)
      林良雄他4名
    • Industrial Property Rights Holder
      林良雄他4名
    • Industrial Property Rights Type
      特許
    • Filing Date
      2012-11-30
    • Related Report
      2012 Annual Research Report
    • Overseas
  • [Patent(Industrial Property Rights)] Preparation of dehydrophenylahistin analogs for treating vascular proliferatio2011

    • Inventor(s)
      Yamazaki, Yuri; Hayashi, Yoshio
    • Industrial Property Rights Holder
      Nereus Pharmaceuticals, Inc., USA
    • Filing Date
      2011-07-14
    • Related Report
      2011 Annual Research Report
    • Overseas
  • [Patent(Industrial Property Rights)] 終止コドンを読み飛ばす化合物2011

    • Inventor(s)
      林良雄, 他5人
    • Industrial Property Rights Holder
      東京薬科大学, 他1
    • Industrial Property Number
      2011-263404
    • Filing Date
      2011-12-02
    • Related Report
      2011 Annual Research Report

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Published: 2011-04-06   Modified: 2019-07-29  

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