Kimura Tooru 木村徹

… Alternative Names

KIMURA Tooru 木村徹

木村徹キムラトオル

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Researcher Number	70204980
Other IDs
External Links
Affiliation (Current)	2025: 京都薬科大学, 薬学部, 准教授
Affiliation (based on the past Project Information) *help	2007 – 2012: Kyoto Pharmaceutical University, 薬学部, 准教授 1992 – 2006: 京都薬科大学, 薬学部, 助手 1990: 京都薬科大学, 薬学部, 助手
Review Section/Research Field	Principal Investigator Chemical pharmacy / Drug development chemistry / Chemical pharmacy / 医薬分子機能学 Except Principal Investigator Biological Sciences / Chemical pharmacy / 医薬分子機能学 / Drug development chemistry / Bioorganic chemistry
Keywords	Principal Investigator プロテアーゼ / 固相ペプチド合成 / HIV / ケミカルリゲーション / エイズ / ATL / HAM / HTLV / プロテアーゼ阻害剤 / レトロウイルス … More / Solid Phase Peptide Synthesis / Protease / Chemical Ligation / アロフェニルノルスタチン / ロピナビル / 薬剤耐性 / HIVプロテアーゼ阻害剤 / 治療薬 / 分子認識 / 遷移状態ミメティック / 阻害剤 / HTLV-I / 医薬品化学 / AIDS / HIVプロテアーゼ / 可溶化 / 分子内転位反応 / プロドラッグ / 還元的酸処理脱保護法 / 樹脂担体 / リンカー / 安全装置付保護 / 保護基 / アフィニティークロマトグラフィー / ペプチド合成 … More Except Principal Investigator ドラッグデザイン / ペプチド合成 / HIVプロテアーゼ阻害剤 / 酵素阻害剤 / アスパラギン酸プロテアーゼ / 基質遷移状態誘導体 / 酵素・阻害剤複合体 / 抗ウイルス薬 / ペプチドミメティック / 分子認識 / HIVプロテアーゼ / エイズ治療薬 / 薬剤耐性 / 基質遷移状態 / プロテアーゼ阻害剤 / Peptide Synthesis / ペプチドミミック / Anti-HIV Activity / Enzyme Inhibitor / Substrate Transition State / AIDS Therapeutics / Molecular Recognition / プラスメプシン / セクレターゼ / アルツハイマー病 / 酵素活性中心 / X線結晶構造解析 / 抗エイズ薬 / 効率的固相合成法 / 分子設計 / HIV Protease Inhibitor / 抗HIV活性 / 縮合剤 / β-セクレターゼ / プロテアーゼ / マラリア / コンフォメーション / 固相合成 / 酵素阻害剤複合体 / 基質遷移状態概念 / solid pahse synthesis / HIV Protease / AIDS / プロドラッグ / Anti-AIDS Drug / Drug Resistant Virus / X-ray Crystallography / Conformational Analysis / Substrate Transition State Analog / Enzyme・Inhibitor Complex / HIV Protease Inhibitors / コンフォメーション解析 / 薬剤耐性ウイルス / エイズ / アミロイド産生 / 老化 / 抗ATL薬 / HTLVプロテアーゼ阻害剤 / コンフォーメーション解析 / リ-ドオプチマイゼーション / HTLV-1プロテアーゼ / レニン阻害剤 / Enemy metabolism / Antioxidation / Iron sulfur cluster / Electron transport / Parasitism / Entamoeba histolytica / エネルギー代謝 / 抗酸化 / 鉄硫黄クラスター / 電子伝達 / 寄生 / 赤痢アメーバ / HTLV-1 protease / adult T-cell leukemia / plasmepsin / β-secretase / Alzheimer's disease / aspartic protease / enzyme inhibitors / 難病治療薬 / 成人T細胞白血病 / プロドラック / CIP reagent / dolastatin 15 / coupling reaction / デブシペプチド / Nメチルアミノ酸 / 固相上縮合 / CIP試薬 / ドラスタチン15 / 縮合反応 / fibrinogen binding / RGD structure / Heck reaction / intramolecular cyclization / コンビナトリアル合成 / RGD誘導体 / Heck反応 / フィブリノーゲン結合阻害 / RGD構造 / ヘック反応 / 分子内環化反応 / Double Drug / HIV protease inhibitor / HIV protease / thiazoline / dialkyl amino acid / mirabazole / anti-cancer alkaloid / coupling reagent / チアゾリン / ジアルキルアミノ酸 / ミラバゾール / 抗腫瘍アルカロイド / コンフォンメーション解析 / Prodrug / dipeptide / Inhibitor / Protease / エイズ薬 / ジペプチド / 阻害剤 / Peptide synthesis / クリックペプチド / クリプタイド / ss-セクレターゼ / BACE1 / プラスメプシンII / ダブルドラッグ / ウイルスプロテアーゼ / 化学合成 / インスリン / シリルクロリド / 位置選択的形成 / ジスルフィド結合 / ヒトインスリン / キノスタチン-272 / ATL治療薬 / 高血圧症治療薬 / ペプチドmimic / HIVプロテア-ゼ / レニン / アスパラギン酸プロテア-ゼ Less

薬剤耐性HIVプロテアーゼに対する高活性阻害剤の設計研究Principal Investigator
- Principal Investigator
  
  木村徹
- Project Period (FY)
  2010 – 2012
- Research Category
  
  Grant-in-Aid for Scientific Research (C)
- Research Field
  
  Drug development chemistry
- Research Institution
  Kyoto Pharmaceutical University
Design and Medicinal Chemistry Research on Therapeutics ofDifficult Diseases based on Molecular Recognition
- Principal Investigator
  
  KISO Yoshiaki
- Project Period (FY)
  2009 – 2012
- Research Category
  
  Grant-in-Aid for Scientific Research (A)
- Research Field
  
  Drug development chemistry
- Research Institution
  Nagahama Institute of Bio-Science and Technology
  Kyoto Pharmaceutical University
Design and medicinal chemistry research on drugs for difficult diseases based on molecular recognition of proteases
- Principal Investigator
  
  KISO Yoshiaki
- Project Period (FY)
  2006 – 2008
- Research Category
  
  Grant-in-Aid for Scientific Research (A)
- Research Field
  
  Drug development chemistry
- Research Institution
  Kyoto Pharmaceutical University
Synthetic study of membrane permeable inhibitor of HTLV-I proteasePrincipal Investigator
- Principal Investigator
  
  KIMURA Tooru
- Project Period (FY)
  2006 – 2008
- Research Category
  
  Grant-in-Aid for Scientific Research (C)
- Research Field
  
  Drug development chemistry
- Research Institution
  Kyoto Pharmaceutical University
アルツハイマー病克服をめざしたアミロイドセクレターゼ制御分子のデザインと合成
- Principal Investigator
  
  木曽良明
- Project Period (FY)
  2004
- Research Category
  
  Grant-in-Aid for Scientific Research on Priority Areas
- Review Section
  
  Biological Sciences
- Research Institution
  Kyoto Pharmaceutical University
Biosyrdiesis of iron-sulfur proteins in Enlanoeba histotyrica
- Principal Investigator
  
  NOZAKI Tomoyoshi, 木曽良明
- Project Period (FY)
  2004 – 2005
- Research Category
  
  Grant-in-Aid for Scientific Research on Priority Areas
- Review Section
  
  Biological Sciences
- Research Institution
  Gunma University
  Kyoto Pharmaceutical University
アルツハイマー病克服をめざしたアミロイドセクレターゼ制御分子のデザインと合成
- Principal Investigator
  
  木曽良明
- Project Period (FY)
  2003
- Research Category
  
  Grant-in-Aid for Scientific Research on Priority Areas
- Review Section
  
  Biological Sciences
- Research Institution
  Kyoto Pharmaceutical University
病原体酵素の分子認識に基づくエイズ・マラリアの治療薬開発と薬剤耐性克服研究
- Principal Investigator
  
  木曽良明
- Project Period (FY)
  2003
- Research Category
  
  Grant-in-Aid for Scientific Research on Priority Areas
- Review Section
  
  Biological Sciences
- Research Institution
  Kyoto Pharmaceutical University
Design and development of therapeutic drugs for intractable diseases based on molecular recognition of aspartic proteases
- Principal Investigator
  
  KISO Yoshiaki
- Project Period (FY)
  2003 – 2005
- Research Category
  
  Grant-in-Aid for Scientific Research (B)
- Research Field
  
  Drug development chemistry
- Research Institution
  Kyoto Pharmaceutical University
Study for Synthesis of HTLV-I Protease Analog using Chemical LigationPrincipal Investigator
- Principal Investigator
  
  KIMURA Tooru
- Project Period (FY)
  2003 – 2004
- Research Category
  
  Grant-in-Aid for Scientific Research (C)
- Research Field
  
  Chemical pharmacy
- Research Institution
  Kyoto Pharmaceutical University
アルツハイマー病克服をめざしたアミロイドセクレターゼ制御分子のデザインと合成
- Principal Investigator
  
  木曽良明
- Project Period (FY)
  2002
- Research Category
  
  Grant-in-Aid for Scientific Research on Priority Areas
- Review Section
  
  Biological Sciences
- Research Institution
  Kyoto Pharmaceutical University
変異HIVをターゲットとするダブルドラッグ型阻害剤のデザインと開発研究
- Principal Investigator
  
  木曽良明
- Project Period (FY)
  2001
- Research Category
  
  Grant-in-Aid for Scientific Research on Priority Areas (A)
- Review Section
  
  Biological Sciences
- Research Institution
  Kyoto Pharmaceutical University
プロテアーゼ・リガンド複合体の動的構造解析に基づく阻害剤のデザイン
- Principal Investigator
  
  木曽良明
- Project Period (FY)
  2001 – 2002
- Research Category
  
  Grant-in-Aid for Scientific Research on Priority Areas
- Review Section
  
  Biological Sciences
- Research Institution
  Kyoto Pharmaceutical University
ジスルフィド架橋型HIVプロテアーゼダイマー誘導体の合成研究Principal Investigator
- Principal Investigator
  
  木村徹
- Project Period (FY)
  2001 – 2002
- Research Category
  
  Grant-in-Aid for Young Scientists (B)
- Research Field
  
  Chemical pharmacy
- Research Institution
  Kyoto Pharmaceutical University
変異HIVをターゲットとするハイブリッド型阻害剤のデザインと開発研究
- Principal Investigator
  
  木曽良明
- Project Period (FY)
  2000
- Research Category
  
  Grant-in-Aid for Scientific Research on Priority Areas (A)
- Review Section
  
  Biological Sciences
- Research Institution
  Kyoto Pharmaceutical University
Design of resistance-surmountable HIV protease inhibitors based on molecular recognition analysis of mutant protease
- Principal Investigator
  
  KISO Yoshiaki
- Project Period (FY)
  2000 – 2002
- Research Category
  
  Grant-in-Aid for Scientific Research (B)
- Research Field
  
  医薬分子機能学
- Research Institution
  Kyoto Pharmaceutical University
アスパラギン酸プロテアーゼ活性中心をターゲットとしてデザインされた阻害剤の開発
- Principal Investigator
  
  木曽良明
- Project Period (FY)
  1999
- Research Category
  
  Grant-in-Aid for Scientific Research on Priority Areas (A)
- Research Institution
  Kyoto Pharmaceutical University
変異HIVに対する阻害剤のデザインとウイルス病原性の分子機構解明への展開
- Principal Investigator
  
  木曽良明
- Project Period (FY)
  1999
- Research Category
  
  Grant-in-Aid for Scientific Research on Priority Areas (A)
- Review Section
  
  Biological Sciences
- Research Institution
  Kyoto Pharmaceutical University
プロテアーゼ・リガンド複合体の動的構造解析に基づく阻害剤のデザイン
- Principal Investigator
  
  木曽良明
- Project Period (FY)
  1999 – 2000
- Research Category
  
  Grant-in-Aid for Scientific Research on Priority Areas (A)
- Review Section
  
  Biological Sciences
- Research Institution
  Kyoto Pharmaceutical University
アスパラギン酸プロテアーゼ活性中心をターゲットとしてデザインされた阻害剤の開発
- Principal Investigator
  
  木曽良明
- Project Period (FY)
  1998
- Research Category
  
  Grant-in-Aid for Scientific Research on Priority Areas (A)
- Research Institution
  Kyoto Pharmaceutical University
ケミカルリゲーション法を用いたHIVプロテアーゼ誘導体の合成研究Principal Investigator
- Principal Investigator
  
  木村徹
- Project Period (FY)
  1998 – 1999
- Research Category
  
  Grant-in-Aid for Encouragement of Young Scientists (A)
- Research Field
  
  Chemical pharmacy
- Research Institution
  Kyoto Pharmaceutical University
Study on strategy for AIDS drugs against mutant viruses
- Principal Investigator
  
  KISO Yoshiaki
- Project Period (FY)
  1998 – 1999
- Research Category
  
  Grant-in-Aid for Scientific Research (A).
- Research Field
  
  医薬分子機能学
- Research Institution
  KYOTO PHARMACEUTICAL UNIVERSITY
Intramolecularcyclization by solid-phase olefination and its application to combinatorial synthesis
- Principal Investigator
  
  AKAJI Kenichi
- Project Period (FY)
  1998 – 1999
- Research Category
  
  Grant-in-Aid for Scientific Research (B)
- Research Field
  
  Chemical pharmacy
- Research Institution
  Osaka University
  Kyoto Pharmaceutical University
Convergent synthesis and SAR of dolastatin 15 by solid phase coupling
- Principal Investigator
  
  AKAJI Kenichi
- Project Period (FY)
  1998 – 1999
- Research Category
  
  Grant-in-Aid for Scientific Research (C)
- Research Field
  
  Chemical pharmacy
- Research Institution
  Osaka University
  Kyoto Pharmaceutical University
アスパラギン酸プロテアーゼ活性中心をターゲットとしてデザインされた阻害剤の開発
- Principal Investigator
  
  木曽良明
- Project Period (FY)
  1997
- Research Category
  
  Grant-in-Aid for Scientific Research on Priority Areas
- Research Institution
  Kyoto Pharmaceutical University
Molecular design of HIV protease inhibitors restricted to active conformation
- Principal Investigator
  
  KISO Yoshiaki
- Project Period (FY)
  1997 – 1999
- Research Category
  
  Grant-in-Aid for Scientific Research (B)
- Research Field
  
  医薬分子機能学
- Research Institution
  KYOTO PHARMACEUTICAL UNIVERSITY
アスパラギン酸プロテアーゼ活性中心をターゲットとしてデザインされた阻害剤の開発
- Principal Investigator
  
  木曽良明
- Project Period (FY)
  1996
- Research Category
  
  Grant-in-Aid for Scientific Research on Priority Areas
- Research Institution
  Kyoto Pharmaceutical University
Joint Study on AIDS Drug Based on HIV Protease
- Principal Investigator
  
  KISO Yoshiaki
- Project Period (FY)
  1996 – 1997
- Research Category
  
  Grant-in-Aid for international Scientific Research
- Research Field
  
  Chemical pharmacy
- Research Institution
  KYOTO PHARMACEUTICAL UNIVERSITY
Molecular design and synthesis of HIV protease inhibitors with structurally constrained active conformation
- Principal Investigator
  
  KISO Yoshiki
- Project Period (FY)
  1996
- Research Category
  
  Grant-in-Aid for Scientific Research (B)
- Research Field
  
  Chemical pharmacy
- Research Institution
  Kyoto Pharmaceutical University
Convergent Synthesis of Anti-Cancer Alkaloid, Mirabazols, using a New Coupling Reagent
- Principal Investigator
  
  AKAJI Kenichi
- Project Period (FY)
  1996 – 1997
- Research Category
  
  Grant-in-Aid for Scientific Research (C)
- Research Field
  
  Chemical pharmacy
- Research Institution
  Kyoto Pharmaceutical University
ATL治療薬をめざしたHTLV-1プロテアーゼ阻害剤のデザイン
- Principal Investigator
  
  木曽良明
- Project Period (FY)
  1995
- Research Category
  
  Grant-in-Aid for Scientific Research on Priority Areas
- Research Institution
  Kyoto Pharmaceutical University
活性型コンフォメーションに構造規制されたHIVプロテアーゼ阻害剤の分子設計
- Principal Investigator
  
  木曽良明
- Project Period (FY)
  1995
- Research Category
  
  Grant-in-Aid for General Scientific Research (B)
- Research Field
  
  医薬分子機能学
- Research Institution
  Kyoto Pharmaceutical University
エイズウイルスプロテアーゼ阻害剤の分子内アシル転位型プロドラッグの合成研究Principal Investigator
- Principal Investigator
  
  木村徹
- Project Period (FY)
  1995
- Research Category
  
  Grant-in-Aid for Encouragement of Young Scientists (A)
- Research Field
  
  Chemical pharmacy
- Research Institution
  Kyoto Pharmaceutical University
Molecular design of AIDS therapeutics based on molecular recognition of enzymes.
- Principal Investigator
  
  KISO Yoshiaki
- Project Period (FY)
  1995 – 1996
- Research Category
  
  Grant-in-Aid for Scientific Research (A)
- Research Field
  
  Bioorganic chemistry
- Research Institution
  Kyoto Pharmaceutical University
Development of Low Molecular Weight HIV Protease Inhibitor for Oral Use
- Principal Investigator
  
  AKAJI Kenichi
- Project Period (FY)
  1995 – 1996
- Research Category
  
  Grant-in-Aid for Scientific Research (B)
- Research Field
  
  Chemical pharmacy
- Research Institution
  Kyoto Pharmaceutical University
プロテアーゼ・阻害剤複合体の構造解析に基づく阻害剤の構造活性相関研究
- Principal Investigator
  
  木曽良明
- Project Period (FY)
  1994
- Research Category
  
  Grant-in-Aid for Scientific Research on Priority Areas
- Research Institution
  Kyoto Pharmaceutical University
ATL治療薬をめざしたHTLV-1プロテアーゼ阻害剤のデザイン
- Principal Investigator
  
  木曽良明
- Project Period (FY)
  1994
- Research Category
  
  Grant-in-Aid for Scientific Research on Priority Areas
- Research Institution
  Kyoto Pharmaceutical University
安全装置付き保護戦略による固相ぺプチド合成研究Principal Investigator
- Principal Investigator
  
  木村徹
- Project Period (FY)
  1994
- Research Category
  
  Grant-in-Aid for Encouragement of Young Scientists (A)
- Research Field
  
  Chemical pharmacy
- Research Institution
  Kyoto Pharmaceutical University
ATL治療薬をめざしたHTLV-1プロテアーゼ阻害剤のデザイン
- Principal Investigator
  
  木曽良明
- Project Period (FY)
  1993
- Research Category
  
  Grant-in-Aid for Cancer Research
- Research Institution
  Kyoto Pharmaceutical University
アスパラギン酸プロテアーゼの基質遷移状態概念に基づく医薬品の分子設計
- Principal Investigator
  
  木曽良明
- Project Period (FY)
  1993 – 1994
- Research Category
  
  Grant-in-Aid for General Scientific Research (B)
- Research Field
  
  医薬分子機能学
- Research Institution
  Kyoto Pharmaceutical University
位置選択的架橋反応を用いるヒトインスリンの高効率合成
- Principal Investigator
  
  赤路健一
- Project Period (FY)
  1993 – 1994
- Research Category
  
  Grant-in-Aid for General Scientific Research (C)
- Research Field
  
  Chemical pharmacy
- Research Institution
  Kyoto Pharmaceutical University
エイズウイルス固有のプロテアーゼの合成研究Principal Investigator
- Principal Investigator
  
  木村徹
- Project Period (FY)
  1993
- Research Category
  
  Grant-in-Aid for Encouragement of Young Scientists (A)
- Research Field
  
  医薬分子機能学
- Research Institution
  Kyoto Pharmaceutical University
アスパラギン酸プロテアーゼの基質遷移状態概念に基づく阻害剤の分子設計と合成研究
- Principal Investigator
  
  木曽良明
- Project Period (FY)
  1992
- Research Category
  
  Grant-in-Aid for General Scientific Research (C)
- Research Field
  
  Chemical pharmacy
- Research Institution
  Kyoto Pharmaceutical University
アスパラギン酸プロテア-ゼの基質遷移状態概念に基づく阻害剤の分子設計と合成研究
- Principal Investigator
  
  KISO Yoshiaki
- Project Period (FY)
  1990
- Research Category
  
  Grant-in-Aid for General Scientific Research (C)
- Research Field
  
  Chemical pharmacy
- Research Institution
  Kyoto Pharmaceutical University

All 2011 2010 2009 2008 2007 2006 2005 2004 2003

All Journal Article Presentation

[Journal Article] Maintaining potent HTLV-I protease inhibition without the P3-cap moiety in small tetrapeptidic inhibitors.2011
- Author(s)
  Jeffrey-Tri Nguyen, Keiko Kato, Henri-Obadja Kumada, Koushi Hidaka, Tooru Kimura, Yoshiaki Kiso
- Journal Title
  
  Bioorg. Med. Chem. Lett.
  
  Volume: 21 Issue: 6 Pages: 1832-1837
- DOI
  10.1016/j.bmcl.2011.01.048
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-21249007, KAKENHI-PROJECT-23790145
[Journal Article] Design and synthesis of several small-size HTLV-I protease inhibitors with different hydrophilicity profiles.2011
- Author(s)
  Jeffrey-Tri Nguyen, Keiko Kato, Koushi Hidaka, Henri-Obadja Kumada, Tooru Kimura, Yoshiaki Kiso
- Journal Title
  
  Bioorg. Med. Chem. Lett.
  
  Volume: 21 Issue: 8 Pages: 2425-2429
- DOI
  10.1016/j.bmcl.2011.02.066
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-21249007, KAKENHI-PROJECT-23790145
[Journal Article] Development of L40I HTLV-I protease inhibition assay using novel fluorogenic and chromogenic substrate.2011
- Author(s)
  Henri-Obadja Kumada, Jeffrey-Tri Nguyen, Keiji Nishiyama, Taeko Kakizawa, Yasuhiro Arii, Koushi Hidaka, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso
- Journal Title
  
  J. Peptide Science
  
  Volume: 17(8) Issue: 8 Pages: 569-575
- DOI
  10.1002/psc.1375
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-21249007, KAKENHI-PROJECT-22790119, KAKENHI-PROJECT-23790145
[Journal Article] Structure-guided design and synthesis of P1' position 1-phenylcycloalkyl-amine-derived pentapeptidic BACE1 inhibitors.2011
- Author(s)
  Harichandra D. Tagad, Yoshio Hamada, Jeffrey-Tri Nguyen, Koushi Hidaka, Takashi Hamada, Youhei Sohma, Tooru Kimura, Yoshiaki Kiso
- Journal Title
  
  Bioorg. Med. Chem.
  
  Volume: 19 Issue: 17 Pages: 5238-5246
- DOI
  10.1016/j.bmc.2011.07.002
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-21249007, KAKENHI-PROJECT-22790118, KAKENHI-PROJECT-23590137
[Journal Article] Racemization- free synthesis of cyclic peptide by use of the O-acyl isopeptide method.2010
- Author(s)
  Taku Yoshiya, Hiroyuki Kawashima, Yuka Hasegawa, Kazuhiro Okamoto, Tooru Kimura, Youhei Sohma, Yoshiaki Kiso
- Journal Title
  
  J. Peptide Science.
  
  Volume: 16(8) Issue: 8 Pages: 437-442
- DOI
  10.1002/psc.1261
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-21249007, KAKENHI-PROJECT-22790118
[Journal Article] Design of pentapeptidic BACE1 inhibitors with carboxylic acid bioisosteres at P1' and P4 positions.2010
- Author(s)
  Harichandra D. Tagad, Yoshio Hamada, Jeffrey-Tri Nguyen, Takashi Hamada, Hamdy Abdel-Rahman, Abdellah Yamani, Ayaka Nagamine, Hayato Ikari, Naoto Igawa, Koushi Hidaka, Youhei Sohma, Tooru Kimura, Yo shiaki Kiso
- Journal Title
  
  Bioorg.Med. Chem.
  
  Volume: 18(9) Issue: 9 Pages: 3175-3186
- DOI
  10.1016/j.bmc.2010.03.032
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-21249007
[Journal Article] Crystal growth proce- dure of HIV-1 protease-inhibitor KNI-272 com-plex for neutron structural analysis at 1.9A re- solution.2010
- Author(s)
  Noriko Shimizu, Shigeru Sugiyama, Mihoko Maruyama, Yoshinori Takahashi, Motoyasu Adachi, Taro Tamada, Koushi Hidaka, Yoshio Hayashi, Tooru Kimura, Yoshiaki Kiso, Hiroaki Adachi, Kazufumi Takano, Satoshi Murakami, Tsuyoshi Inoue, Ryota Kuroki, Yusuke, Mori, Hiroyoshi Matsumura
- Journal Title
  
  Crystal Growth Design
  
  Volume: 10 Issue: 6 Pages: 2990-2994
- DOI
  10.1002/psc.1239
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-21249007
[Journal Article] Tetrapeptides, as small-sized peptidic inhibitors; synthesis and their inhibitory activity against2010
- Author(s)
  Taeko Kakizawa, Koushi Hidaka, Daisuke Hamada, Ryoji Yamaguchi, Tsuyoshi Uemura, Hitomi Kitamura, Harichandra D. Tagad, Takashi Hamada, Zyta Ziora, Yoshio Hamada, Tooru Kimura, Yoshiaki Kiso
- Journal Title
  
  BACE1. J. Peptide Science
  
  Volume: 16 Issue: 6 Pages: 257-262
- DOI
  10.1002/psc.1238
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-21249007, KAKENHI-PROJECT-22790119
[Journal Article] Improvement of both plasmepsin inhibitory activity and Antimalarial activity by 2-aminoethylamino substitution.2010
- Author(s)
  Takuya Miura, Koushi Hidaka, Tsuyoshi Uemura, Keisuke Kashimoto, Yuto Hori, Yuko Kawasaki, Adam J. Ruben, Ernesto Freire, Tooru Kimura, Yoshiaki Kiso
- Journal Title
  
  Bioorg. Med. Chem. Lett.
  
  Volume: 20(16) Issue: 16 Pages: 4836-4839
- DOI
  10.1016/j.bmcl.2010.06.099
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-21249007
[Journal Article] Small-sized HIV-1 protease inhibitors containing allo- phenylnorstatine to explore S2' pocket.2009
- Author(s)
  Koushi Hidaka, Tooru Kimura, Hamdy M. Abdel-Rahman, Jeffrey-Tri Nguyen, Keith F. McDaniel, William E. Kohlbrenner, Akhteru- zzaman Molla, Motoyasu Adachi, Taro Tamada, Ryota Kuroki, Noriko Katsuki, Yoshiaki Tanaka, Hikaru Matsumoto, Jun Wang, Yoshio Hayashi, Dale J. Kempf, Yoshiaki Kiso
- Journal Title
  
  J. Med. Chem.
  
  Volume: 52(23) Issue: 23 Pages: 7604-7617
- DOI
  10.1021/jm9005115
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-21249007
[Journal Article] Mito- cryptide-2: purification, identification, and characterization of a novel cryptide that activates neutrophils.2009
- Author(s)
  Hidehito Mukai, Tetsuo Seki, Hiroko Nakano, Yoshinori Hokari, Toshifumi Takao, Masanori Kawanami, Hiroyuki Tsukagoshi, Hirokazu Kimura, Yoshiaki Kiso, Yasutsugu Shimonishi, Yoshisuke Nishi, Eisuke Munekata
- Journal Title
  
  J. Immunology
  
  Volume: 182(8) Issue: 8 Pages: 5072-5080
- DOI
  10.4049/jimmunol.0802965
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-21249007, KAKENHI-PROJECT-21603014
[Journal Article] "Click peptide" : pH-triggered in situ production and aggregation of monomer As1-422009
- Author(s)
  A. Taniguchi, Y. Sohma, Y. Hirayama, H. Mukai, T. Kimura, Y. Hayashi, K. Matsuzaki, Y. Kiso
- Journal Title
  
  Chem Bio Chem 10(4)
  
  Pages: 710-715
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18209005
[Journal Article] Synthesis of amyloid SS peptide1-42 (E22〓) click peptide: pH-triggered in situ production of its native form.2009
- Author(s)
  Hui Wang, Taeko Kakizawa, Atsuhiko Taniguchi, Takaaki Mizuguchi, Tooru Kimura, Yoshiaki Kiso
- Journal Title
  
  Bioorg. Med. Chem.
  
  Volume: 17 (14) Issue: 14 Pages: 4881-4887
- DOI
  10.1016/j.bmc.2009.06.017
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-21249007
[Journal Article] efficient synthesis of isopeptide segment and application to racemization-free segment condensation.2009
- Author(s)
  Taku Yoshiya, Hiroyuki Kawashima, YouheiSohma, Tooru Kimura, Yoshiaki Kiso: O-Acylisopeptide method
- Journal Title
  
  Org. Biomol. Chem.
  
  Volume: 7(14) Issue: 14 Pages: 2894-2904
- DOI
  10.1039/b903624e
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-21249007
[Journal Article] Structure of HIV-1 protease in complex with potent inhibitor KNI-272 determined by high resolution X-ray and neutron crystallography, Proc2009
- Author(s)
  M. Adachi, T. Ohhara, K. Kurihara, T. Tamada, E. Honjo, N. Okazaki, S. Arai, Y. Shoyama, K. Kimura, H. Matsumura, S. Sugiyama, H. Adachi, K. Takano, Y. Mori, K. Hidaka, T. Kimura, Y. Hayashi, Y. Kiso, R. Kuroki
- Journal Title
  
  Natl. Acad. Sci. USA 106(12)
  
  Pages: 4641-4646
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18209005
[Journal Article] Structure of HIV-1 protease incomplex with potent inhibitor KNI-272 determinedby high-resolution X-ray and neutron crystallography2009
- Author(s)
  M. Adachi, T. Kimura, Y. Kiso, 他16名
- Journal Title
  
  Proc.Natl.Acad.Sci.USA 106
  
  Pages: 4641-4646
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18209005
[Journal Article] Isopeptide method : Development of S-acyl isopeptide method for the synthesis of difficult sequence-containing peptides2008
- Author(s)
  T. Yoshiya, N. Ito, T. Kimura, Y. Kiso
- Journal Title
  
  J. Peptide Sci 14(11)
  
  Pages: 1203-1208
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18209005
[Journal Article] Locking the two ends of tetrapeptidic HTLV-I protease inhibitors inside the enzyme2008
- Author(s)
  Meihui Zhang, Jeffrey-Tri Nguyen, Henri-Obadja Kumada, Tooru Kimura, Maosheng Cheng,Yoshio Hayashi, Yoshiaki Kiso
- Journal Title
  
  Bioorg. Med. Chem. 16(14)
  
  Pages: 6880-6890
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18590110
[Journal Article] BACE1 inhibitors : Optimization by replacing the P1' residue with non-acidic moiety2008
- Author(s)
  Y. Hamada, H. Abdel-Rahman, A. Yamani, J.-T. Nguyen, K. Hidaka, T. Kimura, Y. Hayashi, K. Saito, S. Ishiura, Y. Kiso
- Journal Title
  
  Bioorg. Med. Chem. Lett 18(5)
  
  Pages: 1649-1653
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18209005
[Journal Article] Truncation and non-natural amino acid substitution studies on HTLV-I protease hexapeptidic inhibitors2008
- Author(s)
  Jeffrey-Tri Nguyen, Meihui Zhang, Henri-Obadja Kumada, Ayako Itami, Keiji Nishiyama, Tooru Kimura, Maosheng Cheng, Yoshio Hayashi, Yoshiaki Kiso
- Journal Title
  
  Bioorg. Med. Chem. Lett 18(1)
  
  Pages: 366-370
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18590110
[Journal Article] Novel nonpeptidic and small-sized BACE1 inhibitors2008
- Author(s)
  Y. Hamada, H. Ohta, N. Miyamoto, R. Yamaguchi, A. Yamani, K. Hidaka, T. Kimura, K. Saito, Y. Hayashi, S. Ishiura, Y. Kiso
- Journal Title
  
  Bioorg. Med. Chem. Lett 18(5)
  
  Pages: 1654-1658
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18209005
[Journal Article] Locking the two ends of tetrapeptidic HTLV-1 protease inhibitors inside the enzyme2008
- Author(s)
  M. Zhang, J.-T. Nguyen, H. Kumada, T. Kimura, M. Cheng, Y. Hayashi, Y. Kiso
- Journal Title
  
  Bioorg. Med. Chem 16(14)
  
  Pages: 6880-6890
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18209005
[Journal Article] Design of potent aspartic protease inhibitors to treat various diseases2008
- Author(s)
  J.-T. Nguyen, Y. Hamada, T. Kimura, Y. Kiso
- Journal Title
  
  Arch. Pharm. Chem. Life Sci 341(9)
  
  Pages: 523-535
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18209005
[Journal Article] Controlled production of Alzheimer's amyloid β peptide from a photo-triggered, water-soluble precursor "click peptide"2008
- Author(s)
  A. Taniguchi, M. Skwarczynski, Y. Sohma, T. Nagano, T. Okada, K. Ikeda, H. Prakash, H. Mukai, Y. Hayashi, T. Kimura, S. Hirota, K. Matsuzaki, Y. Kiso
- Journal Title
  
  Chem Bio Chem 9(18)
  
  Pages: 3055-3065
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18209005
[Journal Article] Synthesis and activity of tetrapeptidic HTLV-1 protease inhibitors possessing different P3-cap moieties2008
- Author(s)
  Meihui Zhang, Jeffrey-Tri Nguyen, Henri-Obadja Kumada, Tooru Kimura, Maosheng Cheng, Yoshio Hayashi, Yoshiaki Kiso
- Journal Title
  
  Bioorg. Med. Chem 16(10)
  
  Pages: 5795-5802
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18590110
[Journal Article] Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin2008
- Author(s)
  K. Hidaka, T. Kimura, A.J. Ruben, T. Uemura, M. Kamiya, A. Kiso, T. Okamoto, Y. Tsuchiya, Y. Hayashi, E. Freire, Y. Kiso
- Journal Title
  
  Bioorg. Med. Chem 16(23)
  
  Pages: 10049-10060
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18209005
[Journal Article] Combination of Non-naturalD-amino acid derivatives and allophenylnorstatine-dimethylthioproline scaffold in HIV proteaseinhibitors have high efficacy in mutant HIV2008
- Author(s)
  S. Nakatani, T. Kimura, Y. Kiso, 他10名
- Journal Title
  
  J.Med.Chem. 51
  
  Pages: 2992-3004
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18209005
[Journal Article] Combination of non-natural D-amino acid derivatives and allophenylnorstatine-dimethyl-thioproline scaffold in HIV protease inhibitors have high efficacy in Mutant HIV2008
- Author(s)
  S. Nakatani, K. Hidaka, E. Ami, K. Nakahara, A. Sato, J.-T. Nguyen, Y. Hamada, Y. Hori, N. Ohnishi, A. Nagai, T. Kimura, Y. Hayashi, Y. Kiso
- Journal Title
  
  J. Med. Chem 51(10)
  
  Pages: 2992-3004
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18209005
[Journal Article] Truncation and non-natural amino acid substitution studies on HTLV-I protease hexapeptidic inhibitors2008
- Author(s)
  J-T. Nguyen, M. Zhang, H. Kumada, A. Itami, K. Nishiyama, T. Kimura, M. Cheng, Y. Hayashi, Y. Kiso
- Journal Title
  
  Bioorg. Med. Chem. Lett 18(1)
  
  Pages: 366-370
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18209005
[Journal Article] Synthesis and activity of tetrapeptidic HTLV-I protease inhibitors possessing different P3-cap moieties2008
- Author(s)
  M. Zhang, J. Nguyen, H. Kumada, T. Kimura, M. Cheng, Y. Hayashi, Y. Kiso
- Journal Title
  
  Bioorg. Med. Chem 16(10)
  
  Pages: 5795-5802
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18209005
[Journal Article] Chipping at large,potent human T-cell leukemia virus type 1 protease inhibitors to uncover smaller,equipotent inhibitors2007
- Author(s)
  Tooru Kimura
- Journal Title
  
  Bioorganic Medicinal Chemistry Letters 17
  
  Pages: 3276-3280
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18209005
[Journal Article] "O-Acyl isopeptide method" for peptide synthesis : synthesis of forty kinds of "O-acyl isodipeptide unit" Boc-Ser/Thr(Fmoc-Xaa)-OH2007
- Author(s)
  T. Yoshiya, A. Taniguchi, Y. Sohma, F. Fukao, S. Nakamura, N. Abe, N. Ito, M. Skwarczynski, T. Kimura, Y. Hayashi, Y. Kiso
- Journal Title
  
  Org. Biomol. Chem 5(11)
  
  Pages: 1720-1730
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18209005
[Journal Article] Chipping at large, potent human T-cell leukemia virus type 1 protease inhibitors to uncover smaller, equipotent inhibitors2007
- Author(s)
  T. Kimura, J.-T. Nguyen, H. Maegawa, K. Nishiyama, Y. Arii, Y. Matsui, Y. Hayashi, Y. Kiso
- Journal Title
  
  Bioorg. Med. Chem. Lett. 17(12)
  
  Pages: 3276-3280
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18209005
[Journal Article] Synthesis and antiviral property of allophenylnorstatine-based HIV protease inhibitors incorporating D-cysteine derivatives as P2/P3 moieties. Bioorg2007
- Author(s)
  E. Ami, K. Nakahara, A. Sato, J.-T. Nguyen, K. Hidaka, Y. Hamada, S. Nakatani, T. Kimura, Y. Hayashi, Y. Kiso
- Journal Title
  
  Med. Chem. Lett 17(15)
  
  Pages: 4213-4217
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18209005
[Journal Article] Development of "O-Acyl Isopeptide Method"2007
- Author(s)
  Y. Sohma, T. Yoshiya, A. Taniguchi, T. Kimura, Y. Hayashi, Y. Kiso
- Journal Title
  
  Biopolymers Peptide Science 88(2)
  
  Pages: 253-262
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18209005
[Journal Article] Design and synthesis of BASE1 inhibitors containing a novel norstatine derivative(2R,3R) -3-amino-2-hydroxy-4-(phenylthio)butyric acid.2007
- Author(s)
  Z.Ziora, S.Kasai, K.Hidaka, A.Nagamine, T.Kimura, Y.Hayashi, et al.
- Journal Title
  
  Bioorg. Med. Chem. Lett 17(6)
  
  Pages: 1629-1633
- Data Source
  KAKENHI-PROJECT-18590110
[Journal Article] Chipping at large,potent human T-cell leukemia virus type 1 protease inhibitors to uncover smaller,equipotent inhibitors2007
- Author(s)
  T.Kimura, J.-T.Nguyen, H.Maegawa, K.Nishiyama, Y.Arii, et. al.
- Journal Title
  
  Bioorg.Med.Chem.Lett. 17(12)
  
  Pages: 3276-3280
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18590110
[Journal Article] Design and synthesis of BACE1 inhibitors containing a novel norstatine derivative (2R, 3R)-3-amino-2-hydroxy-4-(phenylthio) butyric acid2007
- Author(s)
  Z. Ziora, S. Kasai, K. Hidaka, A. Nagamine, T. Kimura, Y. Hayashi, Y. Kiso
- Journal Title
  
  Bioorg. Med. Chem. Lett 17(6)
  
  Pages: 1629-1633
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18209005
[Journal Article] Additional interaction of allophenylnorstatine containing tripeptidomimetics with malarial aspartic protease plasmepsin II2007
- Author(s)
  K. Hidaka, T. Kimura, Y. Tsuchiya, M. Kamiya, A. J. Ruben, E. Freire, Y. Hayashi, Y. Kiso
- Journal Title
  
  Bioorg. Med. Chem. Lett 17(11)
  
  Pages: 3048-3052
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18209005
[Journal Article] "O-Acyl isopeptide method" for peptide synthesis : Solvent effects in the synthesis of As1-42 isopeptide using "O-acyl isodipeptide unit"2007
- Author(s)
  A. Taniguchi, T. Yoshiya, N. Abe, F. Fukao, Y. Sohma, T. Kimura, Y. Hayashi, Y. Kiso
- Journal Title
  
  J. Peptide Sci 13(12)
  
  Pages: 868-874
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18209005
[Journal Article] Design and synthesis of BACE1 inhibitors containing a novel norstatine derivative (2R, 3R)-3-amino-2-hydroxy-4-(phenylthio)butyric acid2007
- Author(s)
  Zyta Ziora, Soko Kasai, Koushi Hidaka, Ayaka Nagamine, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso
- Journal Title
  
  Bioorg. Med. Chem. Lett 17(6)
  
  Pages: 1629-1633
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18590110
[Journal Article] Synthesis and antiviral property of allophenylnorstatine-based HIV protease inhibitors incorporating D-cysteine derivatives as P2/P3 moieties2007
- Author(s)
  Ei'ichi Ami, Koichiro Nakahara, Akihiko Sato, Jeffrey-Tri Nguyen, Koushi Hidaka, Yoshio Hamada, Shingo Nakatani, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso
- Journal Title
  
  Bioorg. Med. Chem. Lett 17(15)
  
  Pages: 4213-4217
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18590110
[Journal Article] Chipping at large, potent human T-cell leukemia virus type 1 protease inhibitors to uncover smaller, equipotent inhibitors2007
- Author(s)
  Tooru Kimura, Jeffrey-Tri Nguyen, Hikoichiro Maegawa, Keiji Nishiyama, Yasuhiro Arii, Yasuko Matsui, Yoshio Hayashi and Yoshiaki Kiso
- Journal Title
  
  Bioorg. Med. Chem. Lett 17(12)
  
  Pages: 3276-3280
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18590110
[Journal Article] O-N Intramolecular acyloxy migration of typical protective groups in hydroxyamino acids.2006
- Author(s)
  M.Skwarczynski, Y.Sohma, M.Noguchi, T.Kimura, Y.Hayashi, et al.
- Journal Title
  
  J.Org.Chem 71(6)
  
  Pages: 2542-2545
- Data Source
  KAKENHI-PROJECT-18590110
[Journal Article] β-Secretase inhibitors : Modification at the P4 position and improvement of inhibitory activity in cultured cell2006
- Author(s)
  Y. Hamada, N. Igawa, H. Ikari, Z. Ziora, J.-T. Nguyen, A. Yamani, K. Hidaka, T. Kimura, K. Saito, Y. Hayashi, M. Ebina, S. Ishiura, Y. Kiso
- Journal Title
  
  Bioorg. Med. Chem. Lett 16(16)
  
  Pages: 4354-4359
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18209005
[Journal Article] Development of first photo responsive prod rug of paclitaxel.2006
- Author(s)
  M.Skwarczynski, M.Noguchi, S.Hirota, Y.Sohma, T.Kimura, Y.Hayashi, et al.
- Journal Title
  
  Bioorg. Med. Chem. Lett 16(17)
  
  Pages: 4492-4496
- Data Source
  KAKENHI-PROJECT-18590110
[Journal Article] "O-Acyl isopeptide method" : racemization- free segment condensation in solid phase peptide synthesis2006
- Author(s)
  T. Yoshiya, Y. Sohma, T. Kimura, Y. Hayashi, Y. Kiso
- Journal Title
  
  Tetrahedron Lett 47(45)
  
  Pages: 7905-7909
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18209005
[Journal Article] Design and synthesis of potent β-secretase (BACE1) inhibitors with P1' carboxylic acid bioisosteres.2006
- Author(s)
  Tooru Kimura
- Journal Title
  
  Bioorganic Medicinal Chemistry Letters 16(9)
  
  Pages: 2380-2386
- Data Source
  KAKENHI-PROJECT-15390039
[Journal Article] Design and synthesis of potent β-secretase (BACE1) inhibitors with P1'carboxylic acid bioisosteres.2006
- Author(s)
  T.Kimura, Y.Hamada, M.Stochaj, H.Ikari, A.Nagamine, et al.
- Journal Title
  
  Bioorg. Med. Chem. Lett 16(9)
  
  Pages: 2380-2386
- Data Source
  KAKENHI-PROJECT-18590110
[Journal Article] "Click peptide" : a novel "O-acyl isopeptide method" for peptide synthesis and chemical biology-oriented synthesis of amyloid β peptide analogues2006
- Author(s)
  Y. Sohma, A. Taniguchi, T. Yoshiya, Y. Chiyomori, F. Fukao, S. Nakamura, M. Skwarczynski, T. Okada, K. Ikeda, Y. Hayashi, T. Kimura, S. Hirota, K. Matsuzaki, Y. Kiso
- Journal Title
  
  J. Peptide Science 12(12)
  
  Pages: 823-828
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18209005
[Journal Article] "O-Acyl isopeptide method" for the efficient synthesis of difficult sequence-containing peptides : use of "O-acyl isodipeptide unit"2006
- Author(s)
  Youhei Sohma, Atsuhiko Taniguchi, Mariusz Skwarczynski, Taku Yoshiya, Fukue Fukao, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso
- Journal Title
  
  Tetrahedron Letters 47(18)
  
  Pages: 3013-3017
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18590110
[Journal Article] β-Secretase inhibitors : Modification at the P4 position and improvement of inhibitory activity in cultured cell2006
- Author(s)
  Yoshio Hamada, Naoto Igawa, Hayato Ikari, Zyta Ziora, Jeffrey-Tri Nguyen, Abdellah Yamani, Koushi Hidaka, Tooru Kimura, Kazuki Saito, Yoshio Hayashi, Maiko Ebina, Shoichi Ishiura, Yoshiaki Kiso
- Journal Title
  
  Bioorg. Med. Chem. Lett 16(16)
  
  Pages: 4354-4359
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18590110
[Journal Article] Small-sized BACE1 inhibitors2006
- Author(s)
  Zyta Ziora, Tooru Kimura, Yoshiaki Kiso
- Journal Title
  
  Drugs of the Future 31(1)
  
  Pages: 53-63
- Description
  「研究成果報告書概要(欧文)」より
- Data Source
  KAKENHI-PROJECT-15390039
[Journal Article] Development of first photoresponsive prodrug of paclitaxel2006
- Author(s)
  Mariusz Skwarczynski, Mayo Noguchi, Shun Hirota, Youhei Sohma, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso
- Journal Title
  
  Bioorg. Med. Chem. Lett 16(17)
  
  Pages: 4492-4496
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18590110
[Journal Article] O-N Intramolecular acyloxy migration of typical protective groups in hydroxyamino acids2006
- Author(s)
  Mariusz Skwarczynski, Youhei Sohma, Mayo Noguchi, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso
- Journal Title
  
  J. Org. Chem 71(6)
  
  Pages: 2542-2545
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18590110
[Journal Article] Design and synthesis of potent s-secretase (BACE1) inhibitors with P1' carboxylic acid bioisosteres2006
- Author(s)
  T. Kimura, Y. Hamada, M. Stochaj, H. Ikari, A. Nagamine, H. Abdel-Rahman, N. Igawa, K. Hidaka, J.-T. Nguyen, K. Saito, Y. Hayashi, Y. Kiso
- Journal Title
  
  Bioorg. Med. Chem. Lett 16(9)
  
  Pages: 2380-2386
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18209005
[Journal Article] Design and synthesis of potent β-secretase (BACE1) inhibitors with P1' carboxylic acid bioisosteres2006
- Author(s)
  Tooru Kimura, Yoshio Hamada, Monika Stochaj, Hayato Ikari, Ayaka Nagamine, Hamdy Abdel-Rahman, Naoto Igawa, Koushi Hidaka, Jeffrey-Tri Nguyen, Kazuki saito, Yoshio Hayashi, Yoshiaki Kiso
- Journal Title
  
  Bioorg. Med. Chem. Lett 16(9)
  
  Pages: 2380-2386
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18590110
[Journal Article] "O-Acyl isopeptide method" for the efficient synthesis of difficult sequence-containing peptides : use of "O-acyl isodipeptide unit"2006
- Author(s)
  Y. Sohma, A. Taniguchi, M. Skwarczynski, T. Yoshiya, F. Fukao, T. Kimura, Y. Hayashi, Y. Kiso
- Journal Title
  
  Tetrahedron Lett 47(18)
  
  Pages: 3013-3017
- Peer Reviewed
- Data Source
  KAKENHI-PROJECT-18209005
[Journal Article] Design and synthesis of highly active Alzheimer's β-secretase (BACE1) inhibitors, KMI-420 and KMI-429, with enhanced chemical stability2005
- Author(s)
  Tooru Kimura, Daisuke Shuto Yoshio Hamada, Naoto Igawa, et al.
- Journal Title
  
  Bioorg.Med.Chem.Lett. 15(1)
  
  Pages: 211-215
- Description
  「研究成果報告書概要(欧文)」より
- Data Source
  KAKENHI-PROJECT-15590030
[Journal Article] Design and synthesis of highly active Alzheimer's β-secretase(BACE1) inhibitors, KMI-420 and KMI-429, with enhanced chemical stability2005
- Author(s)
  Tooru Kimura, Daisuke Shuto, Yoshio Hamada, Naoto Igawa, et al.
- Journal Title
  
  Bioorg.Med.Chem.Lett. 15(1)
  
  Pages: 211-215
- Description
  「研究成果報告書概要(和文)」より
- Data Source
  KAKENHI-PROJECT-15590030
[Journal Article] Design and synthesis of highly active Alzheimer's β-secretase (BACE1) inhibitors KMI-420 and KMI-429, with enhanced chemical stability.2005
- Author(s)
  Tooru Kimura
- Journal Title
  
  Bioorganic Medicinal Chemistry Letters 15(1)
  
  Pages: 211-215
- Data Source
  KAKENHI-PROJECT-15390039
[Journal Article] Design and synthesis of highly active Alzheimer's β-secretase (BACE1) inhibitors, KMI-420 and KMI-429, with enhanced chemical stability2005
- Author(s)
  Tooru Kimura, Daisuke Shuto, Yoshio Hamada, Naoto Igawa, et al.
- Journal Title
  
  Bioorg.Med.Chem.Lett. 15(1)
  
  Pages: 211-215
- Data Source
  KAKENHI-PROJECT-15590030
[Journal Article] Design and synthesis of highly active Alzheimer's β-secretase (BACE1) inhibitors, KMI-420 and KMI-429, with enhanced chemical stability.2005
- Author(s)
  Tooru Kimura
- Journal Title
  
  Bioorganic Medicinal Chemistry Letters 15(1)
  
  Pages: 211-215
- Data Source
  KAKENHI-PROJECT-16015304
[Journal Article] Design of inhibitors against HIV, HTLV-I, and Plasmodium falciparum aspartic proteases2004
- Author(s)
  Hamdy M.Abdel-Rahman, Tooru Kimura, Koushi Hidaka, et al.
- Journal Title
  
  Biological Chemsitry 385(11)
  
  Pages: 1035-1039
- Description
  「研究成果報告書概要(欧文)」より
- Data Source
  KAKENHI-PROJECT-15590030
[Journal Article] Water-soluble prodrugs of dipeptide HIV protease inhibitors based on O-N intramolelcular acyl migration : design, synthesis and kinetic study2004
- Author(s)
  Y.Hamada, H.Matsumoto, S.Yamaguchi, T.Kimura, Y.Hayashi, et al.
- Journal Title
  
  Biorg.Med.Chem. 12(1)
  
  Pages: 159-170
- Description
  「研究成果報告書概要(欧文)」より
- Data Source
  KAKENHI-PROJECT-15590030
[Journal Article] Identification of peptidomimetic HTLV-1 protease inhibitors containing hydroxymethylcarbonyl (HMC) isostere as the transition-state mimic2004
- Author(s)
  Hikoichiro Maegawa, Tooru Kimura, Yasuhiro Arii, Yasuko Matsui, et al.
- Journal Title
  
  Bioorg.Med.Chem.Lett. 14(23)
  
  Pages: 5925-5929
- Description
  「研究成果報告書概要(欧文)」より
- Data Source
  KAKENHI-PROJECT-15590030
[Journal Article] Design of inhibitors against HIV, HTLV-I, and Plasmodium falciparum aspartic proteases2004
- Author(s)
  Hamdy M.Abdel-Rahman, Tooru Kimura, Koushi Hidaka, et al.
- Journal Title
  
  Biological Chemistry 385(11)
  
  Pages: 1035-1039
- Description
  「研究成果報告書概要(和文)」より
- Data Source
  KAKENHI-PROJECT-15590030
[Journal Article] Search for substrate-based inhibitors fitting the S2' space of malarial aspartic protease plasmepsin II2004
- Author(s)
  Aiko Kiso, Koushi Hidaka, Tooru Kimura, Yoshio Hayashi, et al.
- Journal Title
  
  J.Peptide Sci. 10(11)
  
  Pages: 641-647
- Description
  「研究成果報告書概要(和文)」より
- Data Source
  KAKENHI-PROJECT-15590030
[Journal Article] KMI-358 and KMI-370, highly potent and small-sized BACE1 inhibitors containing phenylnorstatine2004
- Author(s)
  T.Kimura, D.Shuto, S.Kasai, P.Liu, K.Hidaka, T.Hamada, Y.Hayashi, et al.
- Journal Title
  
  Biorg.Med.Chem.Lett. 14(6)
  
  Pages: 1527-1531
- Description
  「研究成果報告書概要(和文)」より
- Data Source
  KAKENHI-PROJECT-15590030
[Journal Article] Rigid backbone moiety of KNI-272, a highly selective HIV protease inhibitor2004
- Author(s)
  Mitsunobu Doi, Tooru Kimura, Toshimasa Ishida, Yoshiaki Kiso
- Journal Title
  
  Acta Crystallographica Sect.B B60(4)
  
  Pages: 433-437
- Description
  「研究成果報告書概要(和文)」より
- Data Source
  KAKENHI-PROJECT-15590030
[Journal Article] Water-soluble prodrugs of dipeptide HIV protease inhibitors based on O-N intramolecular acyl migration : design, synthesis and kinetic study2004
- Author(s)
  Y.Hamada, H.Matsumoto, S.Yamaguchi, T.Kimura, Y.Hayashi, et al.
- Journal Title
  
  Biorg.Med.Chem. 12(1)
  
  Pages: 159-170
- Description
  「研究成果報告書概要(和文)」より
- Data Source
  KAKENHI-PROJECT-15590030
[Journal Article] Identification of peptidomimetic HTLV-1 protease inhibitors containing hydroxymethylcarbonyl(HMC) isostere as the transition-state mimic2004
- Author(s)
  Hikoichiro Maegawa, Tooru Kimura, Yasuhiro Arii, Yasuko Matsui, et al.
- Journal Title
  
  Bioorg.Med.Chem.Lett. 14(23)
  
  Pages: 5925-5929
- Description
  「研究成果報告書概要(和文)」より
- Data Source
  KAKENHI-PROJECT-15590030
[Journal Article] Development of water-soluble prodrugs of the HIV-1 protease inhibitor KNI-7272003
- Author(s)
  Y.Sohma, Y.Hayashi, T.Ito, H.Matsumoto, T.Kimura, Y.Kiso
- Journal Title
  
  J.Med.Chem. 46(19)
  
  Pages: 4124-4135
- Description
  「研究成果報告書概要(欧文)」より
- Data Source
  KAKENHI-PROJECT-15590030
[Journal Article] Development of water-soluble prodrugs of the HIV-1 protease inhibitor KNI-7272003
- Author(s)
  Y.Sohma, Y.Hayashi, T.ITo, H.Matsumoto, T.Kimura, Y.Kiso
- Journal Title
  
  J.Med.Chem. 46(19)
  
  Pages: 4124-4135
- Description
  「研究成果報告書概要(和文)」より
- Data Source
  KAKENHI-PROJECT-15590030
[Journal Article] Effect of the acyl groups on O→N acyl migration in the water-soluble prodrugs of HIV-1 protease inhibitor2003
- Author(s)
  Y.Hamada, H.Matsumoto, T.Kimura, Y.Hayashi, Y.Kiso
- Journal Title
  
  Biorg.Med.Chem.Lett. 13(16)
  
  Pages: 2727-2730
- Description
  「研究成果報告書概要(欧文)」より
- Data Source
  KAKENHI-PROJECT-15590030
[Journal Article] Effect of the acyl groups on O→N acyl migration in the water-soluble prodrugs of HIV-1 protease inhibitor.2003
- Author(s)
  Y.Hamada, H.Matsumoto, T.Kimura, Y.Hayashi, Y.Kiso
- Journal Title
  
  Biorg.Med.Chem.Lett. 13(16)
  
  Pages: 2727-2730
- Description
  「研究成果報告書概要(和文)」より
- Data Source
  KAKENHI-PROJECT-15590030
[Journal Article] KMI-008, a novel β-secretase inhibitor containing a hydroxymethylcarbonyl isostere as a transition-state mimic : design and synthesis of substrate-based octapeptides2003
- Author(s)
  D.Shuto, S.Kasai, T.Kimura, P.Liu, K.Hidaka, T.Hamada, et al.
- Journal Title
  
  Biorg.Med.Chem.Lett. 13(24)
  
  Pages: 4273-4276
- Description
  「研究成果報告書概要(和文)」より
- Data Source
  KAKENHI-PROJECT-15590030
[Journal Article] High affinity inhibition of a family of Plasmodium falciparum proteases by a designed adaptive inhibitor2003
- Author(s)
  A.Nezami, T.Kimura, K.Hidaka, A.Kiso, J.Liu, Y.Kiso, E.Freire, et al.
- Journal Title
  
  Biochemistry 42(28)
  
  Pages: 8459-8464
- Description
  「研究成果報告書概要(和文)」より
- Data Source
  KAKENHI-PROJECT-15590030
[Presentation] "クリックペプチド":水溶性プレカーサーによるアルツハイマー病関連Aβ変異体の産生.2010
- Author(s)
  王惠、柿澤多惠子、谷口敦彦、水口貴章、相馬洋平、向井秀仁、木村徹、木曽良明
- Organizer
  日本薬学会第130年会
- Place of Presentation
  岡山
- Data Source
  KAKENHI-PROJECT-21249007
[Presentation] ロピナビル耐性株由来の変異を導入したHIVプロテアーゼ誘導体の解析.2010
- Author(s)
  日高興士、安達基泰、黒木良太、濱田貴司、Sankara Rajesh、木村徹、木曽良明
- Organizer
  第24回日本エイズ学会学術集会・総会
- Place of Presentation
  東京
- Data Source
  KAKENHI-PROJECT-21249007
[Presentation] Tripeptidic BACE1 inhibitors by confor- mational structure-based design.2010
- Author(s)
  Yoshio Hamada, Harichandra Tagad, Takashi Hamada, Tooru Kimura, Yoshiaki Kiso
- Organizer
  5th Inter- national Peptide Symposium/ 47th Japanese Peptide Symposium
- Place of Presentation
  Kyoto
- Data Source
  KAKENHI-PROJECT-21249007
[Presentation] 新規抗マラリア治療薬を目指したプラスメプシン阻害剤研究:酵素ポケット外での新たな相互作用.2010
- Author(s)
  三浦拓也、日高興士、上村剛史、柏本啓介、Ernesto Freire、木村徹、木曽良明
- Organizer
  日本薬学会第130年会
- Place of Presentation
  岡山
- Data Source
  KAKENHI-PROJECT-21249007
[Presentation] ロピナビル耐性株由来のHIVプロテアーゼ変異体とアロフェニルノルスタチン阻害剤の相互作用解析.2010
- Author(s)
  日高興士、安達基泰、黒木良太、濱田貴司、Rajesh Narayanan、木村徹、木曽良明
- Organizer
  第29回メディシナルケミストリーシンポジウム
- Place of Presentation
  京都
- Data Source
  KAKENHI-PROJECT-21249007
[Presentation] In situ production of Alzheimer's Aβ mutants from water-soluble click peptide precursors.2010
- Author(s)
  Hui Wang, Taeko Kakizawa, Atsuhiko Taniguchi, Takaaki Mizuguchi, Youhei Sohma, Hidehito Mukai, Tooru Kimura, Yoshiaki Kiso
- Organizer
  11th Chinese International Peptide Symposium
- Place of Presentation
  Lanzhou, China
- Data Source
  KAKENHI-PROJECT-21249007
[Presentation] In situ production of Alzheimer's disease-related amyloid s peptide from water- soluble precursor analogs.2009
- Author(s)
  Atsuhiko Taniguchi, Youhei Sohma, Mariusz Skwarczynski, Yuta Hirayama, Takuma Okada, Keisuke Ikeda, Halan Prakash, Hidehito Mukai, Tooru Kimura, Yoshio Hayashi, Shun Hirota, Katsumi Matsuzaki, Yoshiaki Kiso: Click peptide
- Organizer
  238th American Chemical Society National Meeting
- Place of Presentation
  Washington DC, USA
- Data Source
  KAKENHI-PROJECT-21249007
[Presentation] 非ペプチド型BACE1阻害剤の設計と構造活性相関.2009
- Author(s)
  濱田芳男、大田博子、Diganta Sarma、中西智哉、Abdellah Yamani、山口亮司、日高興士、木村徹、石浦章一、木曽良明
- Organizer
  第14回日本病態プロテアーゼ学会
- Place of Presentation
  吹田
- Data Source
  KAKENHI-PROJECT-21249007
[Presentation] Significance of wild-type APP sequence in developing the BACE1 inhibitors.2009
- Author(s)
  Yoshio Hamada, Daisuke Shuto, Ping Liu, Takashi Hamada, Koushi Hidaka, Tooru Kimura, Yoshiaki Kiso
- Organizer
  46th Japanese Peptide Symposium
- Place of Presentation
  Kitakyushu, Japan
- Data Source
  KAKENHI-PROJECT-21249007
[Presentation] プラスメプシンを標的とした新規抗マラリア治療薬の開発:酵素ポケット外へのアミノ置換基の伸長.2009
- Author(s)
  三浦拓也、日高興士、上村剛史、柏本啓介、木村徹、木曽良明、Ernesto Freire
- Organizer
  第28回メディシナルケミストリーシンポジウム
- Place of Presentation
  東京
- Data Source
  KAKENHI-PROJECT-21249007
[Presentation] HIV protease inhibitor design to employ water molecules.2009
- Author(s)
  K. Hidaka, T. Hamada, M. Adachi, R. Kuroki, T. Kimura, Y. Kiso
- Organizer
  Sixth General Meeting of the International Proteo- lysis Society
- Place of Presentation
  Gold Coast, Australia
- Data Source
  KAKENHI-PROJECT-21249007
[Presentation] 架橋水および水和を利用するHIVプロテアーゼ阻害剤研究.2009
- Author(s)
  日高興士、Jeffrey-TriNguyen、濱田貴司、安達基泰、黒木良太、木村徹、木曽良明
- Organizer
  第23回日本エイズ学会学術集会
- Place of Presentation
  名古屋
- Data Source
  KAKENHI-PROJECT-21249007
[Presentation] SAR study of BACE1 inhibitors containing pyridine derivatives2008
- Author(s)
  H. Ohta, Y. Hamada, N. Miyamoto, R. Yamaguchi, A. Yamani, K. Hidaka, T. Kimura, K. Saito, S. Ishiura, Y. Kiso
- Organizer
  45th Japanese Peptide Symposium
- Place of Presentation
  Tokyo, Japan
- Data Source
  KAKENHI-PROJECT-18209005
[Presentation] Road to HTLV-I protease inhibition2008
- Author(s)
  Jeffrey-Tri Nguyen, Meihui Zhang, Ayako Itami, Hikoichiro Maegawa, Keiji Nishiyama, Tooru Kimura, Yoshio Hayashi, Maosheng Cheng, Yoshiaki Kiso
- Organizer
  International Symposium on Integrated Medicinal Science
- Place of Presentation
  Kyoto, Japan
- Data Source
  KAKENHI-PROJECT-18590110
[Presentation] Effect of dipeptidomimetics on malaria parasite proliferation inhibition targeting plasmepsin2008
- Author(s)
  K. Hidaka, T. Kimura, T. Uemura, A. J. Ruben, E. Freire, Y. Kiso
- Organizer
  45th Japanese Peptide Symposium
- Place of Presentation
  Tokyo, Japan
- Data Source
  KAKENHI-PROJECT-18209005
[Presentation] BACE1阻害剤の設計-ペプチドから非ペプチドへ2008
- Author(s)
  濱田芳男、大田博子、宮本奈緒子、山口亮司、A. Yamani、日高興士、木村徹、齋藤一樹、石浦章一、木曽良明
- Organizer
  第13回病態と治療におけるプロテアーゼとインヒビター学会
- Place of Presentation
  吹田
- Data Source
  KAKENHI-PROJECT-18209005
[Presentation] Rational Drug Design of HTLV-I Protease Inhibitors from Octapeptides to Tetrapeptides2007
- Author(s)
  J.-T, Nguyen, M. Zhang, A. Itami, H. Maegawa, K. Nishiyama, T. Kimura, Y. Hayashi, M. Cheng and Y. Kiso
- Organizer
  20th American Peptide Symposium : Peptides for Youth
- Place of Presentation
  Montreal, Canada
- Data Source
  KAKENHI-PROJECT-18590110
[Presentation] Non-peptidic small-sized BACE1 inhibitors : optimazation based on the docked inhibitor's conformer in BACE12007
- Author(s)
  Y. Hamada, N. Miyamoto, R. Yamaguchi, A. Yamani, K. Hidaka, H. Kumada, T. Kimura, K. Saito, Y. Hayashi, S. Ishiura, Y. Kiso
- Organizer
  20th American Peptide Symposium : Peptides for Youth
- Place of Presentation
  Montreal, Canada
- Data Source
  KAKENHI-PROJECT-18209005
[Presentation] HIV protease and malarial plasmepsin inhi bitors with hydroxylmethylcarbonyl isostere2007
- Author(s)
  K. Hidaka, T. Kimura, Y. Tsuchiya, M. Kamiya, E. Freire, B. M. Dunn, Y. Hayashi, Y. Kiso
- Organizer
  5th General Meeting of the International Proteolysis Society
- Place of Presentation
  Patras, Greece
- Data Source
  KAKENHI-PROJECT-18209005
[Presentation] Application of intramolecular migration reaction in peptide chemistry to chemical biology based on "click peptide", and chemical pharmaceutics2006
- Author(s)
  Y. Hayashi, Y. Sohma, A. Taniguchi, M. Skwarczynski, T. Kimura, Y. Kiso
- Organizer
  The 11th Akabori Conf. 2006Japanese-German Symp. Peptide Sci
- Place of Presentation
  Kloster Banz, Germany
- Data Source
  KAKENHI-PROJECT-18209005
[Presentation] Novel thio-derivative of phenylnorstatine and its application to the BACE1 inhibitors design2006
- Author(s)
  Z. Ziora, S. Kasai, K. Hidaka, A. Nagamine, T. Kimura, Y. Hayashi, Y. Kiso
- Organizer
  29th European Peptide Symposium
- Place of Presentation
  Gdansk, Poland
- Data Source
  KAKENHI-PROJECT-18209005

1. KISO Yoshiaki (40089107)

# of Collaborated Projects: 32 results

# of Collaborated Products: 59 results
2. AKAJI Kenichi (60142296)

# of Collaborated Projects: 19 results

# of Collaborated Products: 0 results
3. FUJIWARA Yoichi (60199396)

# of Collaborated Projects: 15 results

# of Collaborated Products: 0 results
4. HAYASHI Yoshio (10322562)

# of Collaborated Projects: 4 results

# of Collaborated Products: 0 results
5. YAMAZAKI Toshimasa (40360458)

# of Collaborated Projects: 4 results

# of Collaborated Products: 0 results
6. HIDAKA Koushi (30445960)

# of Collaborated Projects: 2 results

# of Collaborated Products: 17 results
7. KOBAYASHI Yuji (20127228)

# of Collaborated Projects: 2 results

# of Collaborated Products: 0 results
8. SOHMA Youhei (10565518)

# of Collaborated Projects: 1 results

# of Collaborated Products: 7 results
9. MUKAI Hidehito (20251027)

# of Collaborated Projects: 1 results

# of Collaborated Products: 4 results
10. NOZAKI Tomoyoshi (60198588)

# of Collaborated Projects: 1 results

# of Collaborated Products: 0 results
11. ALI Vahab (20400757)

# of Collaborated Projects: 1 results

# of Collaborated Products: 0 results
12. TAKAHASHI Yasuhiro (10154874)

# of Collaborated Projects: 1 results

# of Collaborated Products: 0 results
13. USSERY Micha

# of Collaborated Projects: 1 results

# of Collaborated Products: 0 results
14. TORCHIA Denn

# of Collaborated Projects: 1 results

# of Collaborated Products: 0 results
15. YARCHOAN Rob

# of Collaborated Projects: 1 results

# of Collaborated Products: 0 results
16. 満屋裕明

# of Collaborated Projects: 1 results

# of Collaborated Products: 0 results
17. 三本勤

# of Collaborated Projects: 1 results

# of Collaborated Products: 0 results

Kimura Tooru 木村 徹

KIMURA Tooru 木村 徹

木村 徹 キムラ トオル

Research Projects

Research Products

Co-Researchers

薬剤耐性HIVプロテアーゼに対する高活性阻害剤の設計研究Principal Investigator

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Synthetic study of membrane permeable inhibitor of HTLV-I proteasePrincipal Investigator

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Study for Synthesis of HTLV-I Protease Analog using Chemical LigationPrincipal Investigator

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ジスルフィド架橋型HIVプロテアーゼダイマー誘導体の合成研究Principal Investigator

Principal Investigator

Project Period (FY)

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Research Institution

Kimura Tooru 木村徹

KIMURA Tooru 木村徹

木村徹キムラトオル