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Design of inhibitors of amyloid beta aggregation and BACE1 for conquering Alzheimer's disease

Research Project

Project/Area Number 26460163
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Research Field Drug development chemistry
Research InstitutionKonan University (2016-2017)
Kobe Pharmaceutical University (2014-2015)

Principal Investigator

HAMADA Yoshio  甲南大学, フロンティアサイエンス研究科, 特別研究員 (70424968)

Project Period (FY) 2014-04-01 – 2018-03-31
Project Status Completed (Fiscal Year 2017)
Budget Amount *help
¥5,070,000 (Direct Cost: ¥3,900,000、Indirect Cost: ¥1,170,000)
Fiscal Year 2016: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2015: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2014: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Keywordsアルツハイマー病 / BACE1 / β-セクレターゼ / アミロイドβ / 凝集阻害剤 / BACE1阻害剤 / β‐セクレターゼ / 酵素阻害剤 / ドッキング計算 / 創薬 / 凝集祖愛剤 / アミロイドβペプチド
Outline of Final Research Achievements

The increase of dementia patients is a big issue for Japan as it faces a rapidly against society. To conquer Alzheimer's disease, this reaearch aimed the development of inhibitors of amyloid beta aggregation and BACE1. We designed and synthesized a series of small-sized BACE1 inhibitors with a thiadiazole moiety. These compounds with improved membrane permeability appear to have promise as drug candidates. And we synthesized aggregation inhibitors. These aggregation inhibitors could recognized a specific Abeta conformer, and are expected to use a research tool for pathogenic mechanism analysis.

Report

(5 results)
  • 2017 Annual Research Report   Final Research Report ( PDF )
  • 2016 Research-status Report
  • 2015 Research-status Report
  • 2014 Research-status Report
  • Research Products

    (48 results)

All 2018 2017 2016 2015 2014 Other

All Journal Article (10 results) (of which Peer Reviewed: 8 results,  Open Access: 2 results,  Acknowledgement Compliant: 7 results) Presentation (21 results) (of which Int'l Joint Research: 2 results,  Invited: 2 results) Book (6 results) Remarks (10 results) Patent(Industrial Property Rights) (1 results)

  • [Journal Article] DNA G-wire formation using an artificial peptide is controlled by protease activity2017

    • Author(s)
      Usui, K., Okada, A., Sakashita, S., Shimooka, M., Tsuruoka, T., Nakano, S., Miyoshi, D., Mashima, T., Katahira, M., Hamada, Y.
    • Journal Title

      Molecules

      Volume: 22 Issue: 11 Pages: 1991-1991

    • DOI

      10.3390/molecules22111991

    • NAID

      120006501324

    • Related Report
      2017 Annual Research Report
    • Peer Reviewed / Open Access
  • [Journal Article] Recent progress in prodrug design strategies based on generally applicable modifications2017

    • Author(s)
      Yoshio Hamada
    • Journal Title

      Bioorganic & Medicinal Chemistry Letters

      Volume: 27 Issue: 8 Pages: 1627-1632

    • DOI

      10.1016/j.bmcl.2017.02.075

    • Related Report
      2016 Research-status Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] Site-Specific Control of Multiple Mineralizations Using a Designed Peptide and DNA2016

    • Author(s)
      K. Usui, M. Ozaki, A. Yamada, Y. Hamada, T. Tsuruoka, T. Imai, K.-y. Tomizaki
    • Journal Title

      Nanoscale

      Volume: 8 Issue: 39 Pages: 17081-17084

    • DOI

      10.1039/c6nr03468c

    • Related Report
      2016 Research-status Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] New directions for protease inhibitors directed drug discovery2016

    • Author(s)
      Yoshio Hamada, Yoshiaki Kiso
    • Journal Title

      Biopolymers

      Volume: 106 Issue: 4 Pages: 563-579

    • DOI

      10.1002/bip.22780

    • Related Report
      2016 Research-status Report
    • Peer Reviewed
  • [Journal Article] Novel prodrugs with a spontaneous cleavable guanidine moiety2016

    • Author(s)
      Yoshio Hamada
    • Journal Title

      Bioorganic & Medicinal Chemistry Letters

      Volume: 26 Issue: 7 Pages: 1690-1695

    • DOI

      10.1016/j.bmcl.2016.02.060

    • Related Report
      2015 Research-status Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] A novel N-terminal degradation reaction of peptides via N-amidination2016

    • Author(s)
      Yoshio Hamada
    • Journal Title

      Bioorganic & Medicinal Chemistry Letters

      Volume: 26 Issue: 7 Pages: 1685-1689

    • DOI

      10.1016/j.bmcl.2016.02.058

    • Related Report
      2015 Research-status Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] Novel β-amyloid aggregation inhibitors possessing a turn mimic2015

    • Author(s)
      Yoshio Hamada, Naoko Miyamoto, Yoshiaki Kiso
    • Journal Title

      Bioorganic & Medicinal Chemistry Letters

      Volume: 25 Issue: 7 Pages: 1572-1576

    • DOI

      10.1016/j.bmcl.2015.02.016

    • Related Report
      2014 Research-status Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] 分子認識を基盤とした創薬研究2014

    • Author(s)
      濵田芳男
    • Journal Title

      化学工業

      Volume: 65 Pages: 405-410

    • Related Report
      2014 Research-status Report
    • Acknowledgement Compliant
  • [Journal Article] Drug discovery of β-secretase inhibitors based on quantum chemical interactions for the treatment of Alzheimer's disease2014

    • Author(s)
      Yoshio Hamada
    • Journal Title

      SOJ Pharmacy & Pharmaceutical Sciences

      Volume: 1 Pages: 1-8

    • Related Report
      2014 Research-status Report
    • Peer Reviewed / Open Access / Acknowledgement Compliant
  • [Journal Article] 生命分子・ペプチドを基盤とした創薬化学2014

    • Author(s)
      濵田芳男、木曽良明
    • Journal Title

      化学工業

      Volume: 65 Pages: 817-823

    • Related Report
      2014 Research-status Report
  • [Presentation] マラリア治療薬としての新規なキニーネプロドラッ グ2018

    • Author(s)
      濵田芳男
    • Organizer
      日本薬学会第138年会
    • Related Report
      2017 Annual Research Report
  • [Presentation] P3部位に環状構造を有するβ-セクレターゼ阻害剤の設計2017

    • Author(s)
      濵田芳男、木曽良明、臼井健二
    • Organizer
      日本薬学会第137年会
    • Place of Presentation
      仙台国際センター(宮城県仙台市)
    • Year and Date
      2017-03-24
    • Related Report
      2016 Research-status Report
  • [Presentation] アルツハイマー病を目指したBACE1阻害剤の開発研究2017

    • Author(s)
      浜田芳男
    • Organizer
      第34回 関西地区ペプチドセミナー
    • Related Report
      2017 Annual Research Report
    • Invited
  • [Presentation] Novel water-soluble prodrug of β-secretase inhibitor as an anti-Alzheimer’s disease drug2017

    • Author(s)
      Yoshio Hamada, Kenji Usui
    • Organizer
      第54回日本ペプチド討論会
    • Related Report
      2017 Annual Research Report
  • [Presentation] アルツハイマー病を目指したメディシナルケミストリー2017

    • Author(s)
      浜田芳男
    • Organizer
      甲南大学 サイエンスライブチケット part. 27
    • Related Report
      2017 Annual Research Report
    • Invited
  • [Presentation] Design of BACE1 inhibitors possessing a medium-ring structure at the P3 position2017

    • Author(s)
      Yoshio Hamada
    • Organizer
      Drug Discovery & Therapy World Congress 2017
    • Related Report
      2017 Annual Research Report
    • Int'l Joint Research
  • [Presentation] Novel HIV-1 protease inhibitor prodrug2017

    • Author(s)
      Yoshio Hamada
    • Organizer
      Drug Discovery & Therapy World Congress 2017
    • Related Report
      2017 Annual Research Report
    • Int'l Joint Research
  • [Presentation] 二種の人工ペプチドを用いたミネラリゼーションによる金-チタニア複合ナノ構造体の作製2017

    • Author(s)
      尾崎誠、坂下俊吾、今井崇人、鶴岡孝章、浜田芳男、富崎欣也、臼井健二
    • Organizer
      日本化学会第97春季年会2017
    • Place of Presentation
      慶応義塾大学日吉キャンパス(神奈川県横浜市)
    • Related Report
      2016 Research-status Report
  • [Presentation] 光リンカー含有ペプチド樹脂を用いた難水溶性物質の検出が可能な改良皮膚感作性試験法の構築2017

    • Author(s)
      南野祐槻、宮崎洋、岡平理湖、目片秀明、高石雅之、浜田芳男、臼井健二
    • Organizer
      日本化学会第97春季年会2017
    • Place of Presentation
      慶応義塾大学日吉キャンパス(神奈川県横浜市)
    • Related Report
      2016 Research-status Report
  • [Presentation] 外部刺激によりDNAグアニン四重鎖構造形成を抑制するPNAペプチドの設計2017

    • Author(s)
      下岡正幸、岡田亜梨沙、浜田芳男、臼井健二
    • Organizer
      日本化学会第97春季年会2017
    • Place of Presentation
      慶応義塾大学日吉キャンパス(神奈川県横浜市)
    • Related Report
      2016 Research-status Report
  • [Presentation] プロテアーゼを用いたアミロイド線維の分解による新規ナノ構造体の作製2017

    • Author(s)
      鶴見栄太、川田原瑠勇、原田陽滋、浜田芳男、臼井健二
    • Organizer
      日本化学会第97春季年会2017
    • Place of Presentation
      慶応義塾大学日吉キャンパス(神奈川県横浜市)
    • Related Report
      2016 Research-status Report
  • [Presentation] New N-Terminal Degradation Reaction of Peptides: Application to a Decapeptide2016

    • Author(s)
      Yoshio Hamada, Kenji Usui
    • Organizer
      第53回日本ペプチド討論会
    • Place of Presentation
      京都テルサ(京都不京都市)
    • Year and Date
      2016-10-26
    • Related Report
      2016 Research-status Report
  • [Presentation] Construction of Nanopeptides by Multiple Mineralization Using DNAs and Designed Peptides2016

    • Author(s)
      M. Ozaki, Y. Hamada, T. Imai,K.-Y. Tomizaki, K. Usui
    • Organizer
      第53回日本ペプチド討論会
    • Place of Presentation
      京都テルサ(京都不京都市)
    • Year and Date
      2016-10-26
    • Related Report
      2016 Research-status Report
  • [Presentation] A novel N-terminal Degradation Reaction of Peptide via Guanidine Derivatives2016

    • Author(s)
      Yoshio Hamada, Kenji Usui
    • Organizer
      34th European Peptide Symposium
    • Place of Presentation
      Leipzig University (Leipzig, Germany)
    • Year and Date
      2016-09-04
    • Related Report
      2016 Research-status Report
  • [Presentation] Site-Specific Control for Silica and Calcium Carbonate Mineralization Using a PNA Peptide and DNA2016

    • Author(s)
      M. Ozaki, K.-Y. Tomizaki, Y. Hamada, K. Usui
    • Organizer
      34th European Peptide Symposium
    • Place of Presentation
      Leipzig University (Leipzig, Germany)
    • Year and Date
      2016-09-04
    • Related Report
      2016 Research-status Report
  • [Presentation] 酵素によらない新規なアミド結合の切断反応2016

    • Author(s)
      浜田芳男
    • Organizer
      第21回日本病態プロテアーゼ学会学術集会
    • Place of Presentation
      千里ライフサイエンスセンター(大阪市吹田市)
    • Year and Date
      2016-08-05
    • Related Report
      2016 Research-status Report
  • [Presentation] 新規なペプチドのN末端アミノ酸 の切断反応2016

    • Author(s)
      濱田芳男
    • Organizer
      日本薬学会第135年会
    • Place of Presentation
      横浜
    • Year and Date
      2016-03-26
    • Related Report
      2015 Research-status Report
  • [Presentation] アルギニンメチルエステルの副反応を応用した新規プロドラッグ2015

    • Author(s)
      濱田芳男、宮田興子
    • Organizer
      第33回メディシナルケミストリーシンポジウム
    • Place of Presentation
      千葉
    • Year and Date
      2015-11-25
    • Related Report
      2015 Research-status Report
  • [Presentation] ターン構造としてプロリン鎖を有する新規アミロイド凝集阻害剤2015

    • Author(s)
      濵田芳男、宮本奈緒子、木曽良明、宮田興子
    • Organizer
      日本薬学会第135年会
    • Place of Presentation
      神戸
    • Year and Date
      2015-03-26 – 2015-03-28
    • Related Report
      2014 Research-status Report
  • [Presentation] P1側鎖にハイドロキノンを有するBACE1阻害剤2014

    • Author(s)
      濵田芳男、西村義則、木曽良明、石浦章一、Harichandra D. Tagad
    • Organizer
      第32回メディシナルケミストリーシンポジウム
    • Place of Presentation
      神戸
    • Year and Date
      2014-11-26 – 2014-11-28
    • Related Report
      2014 Research-status Report
  • [Presentation] β-Amyloid aggregation inhibitors possessing a turn mimic template2014

    • Author(s)
      Yoshio Hamada, Naoko Miyamoto, Yoshiaki Kiso
    • Organizer
      第51回日本ペプチド討論会
    • Place of Presentation
      徳島
    • Year and Date
      2014-10-22 – 2014-10-24
    • Related Report
      2014 Research-status Report
  • [Book] ペプチド固定化マイクロビーズを用いたバイオ計測デバイスの開発2017

    • Author(s)
      臼井健二、南野裕槻、宮崎洋、横田晋三一朗、山下邦彦、濵田芳男
    • Total Pages
      7
    • Publisher
      シーエムシー出版
    • ISBN
      9784781312675
    • Related Report
      2017 Annual Research Report
  • [Book] Computational Modeling of Drugs Against Alzheimer’s Disease2017

    • Author(s)
      Yoshio Hamada, Kenji Usui
    • Total Pages
      21
    • Publisher
      Springer Nature
    • ISBN
      9781493974030
    • Related Report
      2017 Annual Research Report
  • [Book] Quantitative Structure-activity Relationship2017

    • Author(s)
      Yoshio Hamada, Yoshiaki Kiso
    • Total Pages
      16
    • Publisher
      Intech
    • ISBN
      9789535134091
    • Related Report
      2017 Annual Research Report
  • [Book] DDS先端技術の製剤への応用開発2017

    • Author(s)
      浜田芳男
    • Total Pages
      9
    • Publisher
      技術情報協会
    • ISBN
      9784861046636
    • Related Report
      2017 Annual Research Report
  • [Book] Amino Acids, Peptides and Proteins, volume 392015

    • Author(s)
      Yoshio Hamada, Yoshiaki Kiso
    • Total Pages
      34
    • Publisher
      Royal Society of Chemistry
    • Related Report
      2014 Research-status Report
  • [Book] 機能性ペプチドの開発最前線2015

    • Author(s)
      濵田芳男、木曽良明
    • Total Pages
      12
    • Publisher
      シーエムシー出版
    • Related Report
      2014 Research-status Report
  • [Remarks] 濵田芳男のホームページ

    • URL

      https://sites.google.com/site/pynden/

    • Related Report
      2017 Annual Research Report
  • [Remarks] 浜田特別研究員の論文がF1000Primeの推薦論文に選ばれました。

    • URL

      http://www.usui-lab.com/0617.html

    • Related Report
      2017 Annual Research Report
  • [Remarks] F000prime - Article Recommendations

    • URL

      https://f1000.com/prime/726181487

    • Related Report
      2017 Annual Research Report
  • [Remarks] 濵田芳男のホームページ

    • URL

      https://sites.google.com/site/pynden/home

    • Related Report
      2016 Research-status Report 2015 Research-status Report 2014 Research-status Report
  • [Remarks] 神戸学院大学 新着情報:研究成果が『ACS Med Chem Lett』の表紙を飾りました。

    • URL

      http://www.kobegakuin.ac.jp/topics/headline_detail.cgi?kanriid=201203028

    • Related Report
      2016 Research-status Report 2015 Research-status Report
  • [Remarks] ACS Medicinal Chemistry Letters の表紙に掲載。

    • URL

      http://pubs.acs.org/toc/amclct/3/3

    • Related Report
      2016 Research-status Report 2015 Research-status Report
  • [Remarks] ACS Medicinal Chemistry Letters のハイライト記事に掲載。

    • URL

      http://pubs.acs.org/doi/full/10.1021/ml300036g

    • Related Report
      2016 Research-status Report 2015 Research-status Report 2014 Research-status Report
  • [Remarks] F1000primeの推薦論文に選出。

    • URL

      https://f1000.com/prime/726181487

    • Related Report
      2016 Research-status Report
  • [Remarks] 神戸学院大学 新着情報:研究成果が『ACS Med Chem Lett』の表紙を飾りました。

    • URL

      http://www.kobegakuin.ac.jp/topics/headline_detail.cgi?kanriid=201203028

    • Related Report
      2014 Research-status Report
  • [Remarks] ACS Medicinal Chemistry Letters の表紙に掲載。

    • URL

      http://pubs.acs.org/action/showLargeCover?jcode=amclct&vol=3&issue=3

    • Related Report
      2014 Research-status Report
  • [Patent(Industrial Property Rights)] 新規なプロドラッグ2015

    • Inventor(s)
      濵田芳男
    • Industrial Property Rights Holder
      濵田芳男
    • Industrial Property Rights Type
      特許
    • Industrial Property Number
      2015-188114
    • Filing Date
      2015-09-25
    • Related Report
      2015 Research-status Report

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Published: 2014-04-04   Modified: 2019-03-29  

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