Details of the Researcher

PHOTO

Minoru Ishikawa
Section
Graduate School of Life Sciences
Job title
Professor
Degree

  • 博士（薬学）（東京大学）

  • 修士（工学）（東京工業大学）

Research History 9

  • 2019/04 - Present
    Tohoku University　Graduate School of Life Sciences

  • 2019 - 2021
    理化学研究所　客員研究員（兼務）

  • 2018/04 - 2019/03
    The University of Tokyo

  • 2013/04 - 2018/03
    The University of Tokyo　Institute of Molecular and Cellular Biosciences

  • 2014/04 - 2015/03
    The University of Tokyo

  • 2012/10 - 2013/03
    The University of Tokyo　Institute of Molecular and Cellular Biosciences

  • 2008/07 - 2012/09
    The University of Tokyo　Institute of Molecular and Cellular Biosciences

  • 1996/04 - 2008/06
    明治製菓株式会社（現Meiji Seikaファルマ株式会社）　創薬研究所　研究員

  • 2021 -
    東京大学 大学院薬学系研究科 非常勤講師（兼務）

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Education 3

  • Tokyo Institute of Technology　Graduate School of Bioscience and Biotechnology

    1994/04 - 1996/03

  • Tokyo Institute of Technology　School of Bioscience and Biotechnology

    1991/04 - 1994/03

  • Tokyo Institute of Technology

    1990/04 - 1991/03

Committee Memberships 21

  • 日本薬学会医薬化学部会　MEDCHEM NEWS編集委員長

    2025 - Present

  • 日本薬学会医薬化学部会　常任世話人

    2024 - Present

  • 有機合成化学協会　「ニューモダリティと有機合成化学」研究部会幹事

    2022 - Present

  • 日本薬学会医薬化学部会　MEDCHEM NEWS編集委員

    2017/04 - Present

  • American Chemical Society　Journal of Medicinal Chemistry Editorial Advisory Board

    2020 - 2023

  • 日本学術振興会　科学研究費委員会専門委員

    2015/04 - 2017/03

  • 日本薬学会　ファルマシアトピックス小委員

    2007/04 - 2010/03

  • 日本農芸化学会　東北支部宮城県参与

    2024 - Present

  • 有機合成化学協会東北支部　常任幹事

    2020 - Present

  • 日本薬学会医薬化学部会　創薬ニューフロンティア検討会 委員

    2018/04 - 2025/03

  • 日本薬学会医薬化学部会　日本薬学会医薬化学部会, 第41回メディシナルケミストリーシンポジウム実行委員

    2024 -

  • 日本薬学会医薬化学部会　第39回メディシナルケミストリーシンポジウム実行委員

    2022 -

  • 日本農芸化学会　日本農芸化学会2021年度大会 実行委員

    2021 -

  • 日本薬学会 医薬化学部会　第38回メディシナルケミストリーシンポジウム実行委員

    2020 -

  • The Fourth A3 Roundtable Meeting on Asia Chemical Probe Research Hub実行委員

    2019 -

  • 日本化学会生体機能関連化学部会・日本化学会バイオテクノロジー部会　第13回バイオ関連化学シンポジウム実行委員

    2019 -

  • 日本薬学会医薬化学部会　第37回メディシナルケミストリーシンポジウム実行委員

    2019 -

  • 日本薬学会　代議員（関東支部）

    2019 -

  • 日本化学会医農薬化学ディビジョン　アジア国際シンポジウム実行委員

    2014 -

  • 日本薬学会医薬化学部会　第28回メディシナルケミストリーシンポジウム 世話人

    2009 -

  • 日本薬学会　第128年会 組織委員会プログラム委員

    2008 -

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Professional Memberships 8

  • THE CHEMICAL SOCIETY OF JAPAN

  • JAPANESE SOCIETY FOR CHEMICAL BIOLOGY

  • 日本薬学会医薬化学部会

  • 日本農芸化学会

  • 日本レチノイド研究会

  • American chemical society

  • THE SOCIETY OF SYNTHETIC ORGANIC CHEMISTRY, JAPAN

  • THE PHARMACEUTICAL SOCIETY OF JAPAN

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Research Interests 8

  • 水溶性

  • ユビキチン

  • druglike

  • 核内受容体

  • タンパク質分解

  • 生物有機化学

  • Chemical Biology

  • Medicinal Chemistry

Research Areas 3

  • Nanotechnology/Materials / Chemical biology /

  • Nanotechnology/Materials / Biochemistry /

  • Life sciences / Pharmaceuticals - chemistry and drug development /

Awards 9

  1. 2023年度日本薬学会メディシナルケミストリーシンポジウム優秀賞

    2023/11　日本薬学会医薬化学部会

  2. 平成29年度日本薬学会医薬化学部会メディシナルケミストリーシンポジウム優秀賞

    2017/10　日本薬学会医薬化学部会

  3. レチノイド研究会第26回学術集会奨励賞（首藤賞）

    2015/10　レチノイド研究会

  4. 10th AFMC International Medicinal Chemistry Symposium (AIMECS2015) Poster Presentation Prize

    2015/10　AIMECS

  5. Journal of Medicinal Chemistry Highly Cited Perspective of 2011

    2013/02　American Chemical Society

  6. Journal of Medicinal Chemistry Highly Read Perspective of 2011

    2013/02　American Chemical Society

  7. 2010年度（第23回）有機合成化学協会研究企画賞 （武田薬品工業研究企画賞）

    2011/02　有機合成化学協会

  8. 薬品総合研究所所長賞

    2001　明治製菓株式会社

  9. 第８回日本薬学会医薬化学部会年会ポスター賞

    1999/11　日本薬学会医薬化学部会

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Papers 91

  1. Photo-Enhanced Aqueous Solubilization of Azobenzene-Incorporated Lipids Peer-reviewed

    Shusuke Tomoshige, Yushi Kawasaki, Junki Morimoto, Naohiro Sato, Yuichi Hashimoto, Minoru Ishikawa

    Chemical and Pharmaceutical Bulletin　73　(6)　568-573　2025/06/28

    Publisher: Pharmaceutical Society of Japan

    DOI： 10.1248/cpb.c25-00252 　

    ISSN： 0009-2363

    eISSN： 1347-5223

  2. Laccase-catalyzed tyrosine click reaction with 1-methyl-4-arylurazole: rapid labeling on protein surfaces. International-journal Peer-reviewed

    Keita Nakane, Chizu Fujimura, Shogo Miyano, Zhengyi Liu, Tatsuya Niwa, Hafumi Nishi, Tetsuya Kadonosono, Hideki Taguchi, Shusuke Tomoshige, Minoru Ishikawa, Shinichi Sato

    Chemical communications (Cambridge, England)　2024/11/12

    DOI： 10.1039/d4cc03802a 　

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    Our study demonstrates the exceptional efficiency of 1-methyl-4-arylurazole (MAUra) for tyrosine labeling, optimized with laccase under mild conditions, achieving a high efficiency (kcat/Km = 7.88 × 104 M-1 s-1) with minimal oxidative side reactions and selective labeling of highly exposed tyrosine sites on proteins.

  3. Tyrosine Bioconjugation Using Stably Preparable Urazole Radicals Peer-reviewed

    Shinichi Sato, Shogo Miyano, Keita Nakane, Zhengyi Liu, Munehiro Kumashiro, Tomohide Saio, Yuya Tanaka, Akira Shigenaga, Chizu Fujimura, Eri Koyanagi, Hafumi Nishi, Shusuke Tomoshige, Minoru Ishikawa

    Tetrahedron Chem　100111-100111　2024/11

    Publisher: Elsevier BV

    DOI： 10.1016/j.tchem.2024.100111 　

    ISSN： 2666-951X

  4. ［特集］新しいモダリティとして注目を浴びる分解創薬 分解創薬の特集にあたって Invited Peer-reviewed

    石川稔

    MEDCHEM NEWS　34　(4)　201-205　2024/11

  5. Targeted protein degradation in the mitochondrial matrix and its application to chemical control of mitochondrial morphology Peer-reviewed

    Wakana Yamada, Shusuke Tomoshige, Sho Nakamura, Shinichi Sato, Minoru Ishikawa

    Chemical Science　15　14625-14634　2024/09

    Publisher: Royal Society of Chemistry (RSC)

    DOI： 10.1039/d4sc03145h 　

    ISSN： 2041-6520

    eISSN： 2041-6539

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    Mitochondrial-targeted protein degradation (mitoTPD) is explored using small-molecule degraders that leverage a mitochondria-localized protease. This approach restored mitochondrial morphology and shows potential for drug discovery.

  6. A small-molecule degron with a phenylpropionic acid scaffold Invited Peer-reviewed

    Shusuke Tomoshige, Fumiko Komatsu, Tomoko Kikuchi, Miku Sugiyama, Yushi Kawasaki, Kenji Ohgane, Yuuki Furuyama, Shinichi Sato, Minoru Ishikawa, Kouji Kuramochi

    Bioorganic & Medicinal Chemistry　109　(15)　117789-117789　2024/06

    Publisher: Elsevier BV

    DOI： 10.1016/j.bmc.2024.117789 　

    ISSN： 0968-0896

  7. 標的タンパク質分解誘導化合物 PROTACの開発 Invited

    友重秀介, 石川稔

    PHARM STAGE　24　49-53　2024/05

  8. Allosteric Hsp70 Modulator YM-1 Induces Degradation of BRD4 International-journal Invited Peer-reviewed

    Yugo Mishima, Shusuke Tomoshige, Shinichi Sato, Minoru Ishikawa

    Chemical and Pharmaceutical Bulletin　72　(2)　161-165　2024/02/01

    DOI： 10.1248/cpb.c23-00543 　

  9. ミトコンドリア内タンパク質を標的とするタンパク質分解誘導薬の開発 Invited Peer-reviewed

    MEDCHEM NEWS　34　(3)　145-149　2024

    DOI： 10.14894/medchem.34.3_145 　

  10. 標的タンパク質分解薬PROTAC Invited Peer-reviewed

    石川稔, 友重秀介

    PEPTIDE NEWSLETTER JAPAN　128　7-10　2023/04

  11. Near-Infrared-Light-Activatable Proximity Labeling of Bead-Binding Proteins

    Shinichi Sato, Keita Nakane, Yuki Hoshino, Kosuke Dodo, Shusuke Tomoshige, Minoru Ishikawa, Taniyuki Furuyama

    2023/03/21

    Publisher: American Chemical Society (ACS)

    DOI： 10.26434/chemrxiv-2023-443cj 　

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    Photocatalytic proximity labeling has recently undergone significant advances as a valuable tool for understanding protein–protein and cell–cell interactions. This paper reports the first photocatalytic protein-labeling approach in which the reaction can be controlled using near-infrared (NIR) light (810 nm). Magnetic affinity beads with encapsulated sulfur-substituted silicon (IV) phthalocyanine, which produces singlet oxygen upon NIR irradiation, were prepared. We have developed a method in which the histidine residues of proteins bound to the ligands on the beads are selectively oxidized and labeled by the nucleophilic labeling reagent while minimizing nonspecific adsorption to the dye. Beads with aryl sulfamide, lactose, or CZC-8004 ligands immobilized on their surface can be used to label proteins that bind these ligands, as well as their protein–protein interaction partners.

  12. Switching of Photocatalytic Tyrosine/Histidine Labeling and Application to Photocatalytic Proximity Labeling

    Keita Nakane, Haruto Nagasawa, Chizu Fujimura, Eri Koyanagi, Shusuke Tomoshige, Minoru Ishikawa, Shinichi Sato

    International Journal of Molecular Sciences　23　(19)　11622-11622　2022/10/02

    Publisher: MDPI AG

    DOI： 10.3390/ijms231911622 　

    eISSN： 1422-0067

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    Weak and transient protein interactions are involved in dynamic biological responses and are an important research subject; however, methods to elucidate such interactions are lacking. Proximity labeling is a promising technique for labeling transient ligand–binding proteins and protein–protein interaction partners of analytes via an irreversible covalent bond. Expanding chemical tools for proximity labeling is required to analyze the interactome. We developed several photocatalytic proximity-labeling reactions mediated by two different mechanisms. We found that numerous dye molecules can function as catalysts for protein labeling. We also identified catalysts that selectively modify tyrosine and histidine residues and evaluated their mechanisms. Model experiments using HaloTag were performed to demonstrate photocatalytic proximity labeling. We found that both ATTO465, which catalyzes labeling by a single electron transfer, and BODIPY, which catalyzes labeling by singlet oxygen, catalyze proximity labeling in cells.

  13. 標的タンパク質分解薬による創薬パラダイムシフト -低分子リガンドの活躍 Invited

    友重秀介, 石川稔

    月刊細胞　54　(9)　504-507　2022/07

  14. Improvement in Aqueous Solubility of Bioactive Molecules by Decreasing Intermolecular Interaction Invited Peer-reviewed

    Minoru Ishikawa

    YAKUGAKU ZASSHI　142　(4)　365-379　2022/04

    Publisher: Pharmaceutical Society of Japan

    DOI： 10.1248/yakushi.21-00185-3 　

    ISSN： 0031-6903

    eISSN： 1347-5231

  15. Conversion of a PROTAC Mutant Huntingtin Degrader into Small-Molecule Hydrophobic Tags Focusing on Drug-like Properties International-journal Peer-reviewed

    Keigo Hirai, Hiroko Yamashita, Shusuke Tomoshige, Yugo Mishima, Tatsuya Niwa, Kenji Ohgane, Mayumi Ishii, Kayoko Kanamitsu, Yui Ikemi, Shinsaku Nakagawa, Hideki Taguchi, Shinichi Sato, Yuichi Hashimoto, Minoru Ishikawa

    ACS Medicinal Chemistry Letters　13　(3)　396-402　2022/03

    Publisher: American Chemical Society (ACS)

    DOI： 10.1021/acsmedchemlett.1c00500 　

    ISSN： 1948-5875

    eISSN： 1948-5875

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    The onset of neurodegenerative disorders (NDs), such as Alzheimer's disease, is associated with the accumulation of aggregates of misfolded proteins. We previously showed that chemical knockdown of ND-related aggregation-prone proteins can be achieved by proteolysis targeting chimeras (PROTACs). However, hetero-bifunctional PROTACs generally show poor permeability into the central nervous system, where NDs are located. Here, we document the conversion of one of our PROTACs into hydrophobic tags (HyTs), another class of degraders bearing hydrophobic degrons. This conversion decreases the molecular weight and the number of hydrogen bond donors/acceptors. All the developed HyTs lowered the level of mutant huntingtin, an aggregation-prone protein, with potency comparable to that of the parent PROTAC. Through IAM chromatography analysis and in vivo brain penetration assay of the HyTs, we discovered a brain-permeable HyT. Our results and mechanistic analysis indicate that conversion of protein degraders into HyTs could be a useful approach to improve their drug-like properties.

  16. BODIPY Catalyzes Proximity‐Dependent Histidine Labelling Peer-reviewed

    Keita Nakane, Tatsuya Niwa, Michihiko Tsushima, Shusuke Tomoshige, Hideki Taguchi, Hiroyuki Nakamura, Minoru Ishikawa, Shinichi Sato

    ChemCatChem　14　(9)　e202200077　2022/02/20

    Publisher: Wiley

    DOI： 10.1002/cctc.202200077 　

    ISSN： 1867-3880

    eISSN： 1867-3899

  17. Functionalization of Human Serum Albumin by Tyrosine Click Peer-reviewed

    Satsuki Obara, Keita Nakane, Chizu Fujimura, Shusuke Tomoshige, Minoru Ishikawa, Shinichi Sato

    International Journal of Molecular Sciences　22　(16)　8676-8676　2021/08

    Publisher: MDPI AG

    DOI： 10.3390/ijms22168676 　

    eISSN： 1422-0067

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    Human serum albumin (HSA) is a promising drug delivery carrier. Although covalent modification of Cys34 is a well-established method, it is desirable to develop a novel covalent modification method that targets residues other than cysteine to introduce multiple functions into a single HSA molecule. We developed a tyrosine-selective modification of HSA. Three tyrosine selective modification methods, hemin-catalyzed, horseradish peroxidase (HRP)-catalyzed, and laccase-catalyzed reactions were performed, and the modification efficiencies and modification sites of the modified HSAs obtained by these methods were evaluated and compared. We found that the laccase-catalyzed method could efficiently modify the tyrosine residue of HSA under mild reaction conditions without inducing oxidative side reactions. An average of 2.2 molecules of functional groups could be introduced to a single molecule of HSA by the laccase method. Binding site analysis using mass spectrometry suggested Y84, Y138, and Y401 as the main modification sites. Furthermore, we evaluated binding to ibuprofen and found that, unlike the conventional lysine residue modification, the inhibition of drug binding was minimal. These results suggest that tyrosine-residue selective chemical modification is a promising method for covalent drug attachment to HSA.

  18. 医薬リード化合物の体内動態改善法 –水溶性・脂溶性のアウフヘーベン– Invited Peer-reviewed

    石川稔

    ファルマシア　57　620-624　2021/07

  19. Improvement in aqueous solubility of achiral symmetric cyclofenil by modification to a chiral asymmetric analog Peer-reviewed

    Junki Morimoto, Kazunori Miyamoto, Yuki Ichikawa, Masanobu Uchiyama, Makoto Makishima, Yuichi Hashimoto, Minoru Ishikawa

    Scientific Reports　11　12697　2021/06

  20. Proximity Histidine Labeling by Umpolung Strategy Using Singlet Oxygen International-journal Peer-reviewed

    Keita Nakane, Shinichi Sato, Tatsuya Niwa, Michihiko Tsushima, Shusuke Tomoshige, Hideki Taguchi, Minoru Ishikawa, Hiroyuki Nakamura

    Journal of the American Chemical Society　143　(20)　7726-7731　2021/05/26

    Publisher: American Chemical Society (ACS)

    DOI： 10.1021/jacs.1c01626 　

    ISSN： 0002-7863

    eISSN： 1520-5126

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    While electrophilic reagents for histidine labeling have been developed, we report an umpolung strategy for histidine functionalization. A nucleophilic small molecule, 1-methyl-4-arylurazole, selectively labeled histidine under singlet oxygen (1O2) generation conditions. Rapid histidine labeling can be applied for instant protein labeling. Utilizing the short diffusion distance of 1O2 and a technique to localize the 1O2 generator, a photocatalyst in close proximity to the ligand-binding site, we demonstrated antibody Fc-selective labeling on magnetic beads functionalized with a ruthenium photocatalyst and Fc ligand, ApA. Three histidine residues located around the ApA binding site were identified as labeling sites by liquid chromatography-mass spectrometry analysis. This result suggests that 1O2-mediated histidine labeling can be applied to a proximity labeling reaction on the nanometer scale.

  21. In Vivo Synthetic Chemistry of Proteolysis Targeting Chimeras (PROTACs) Invited Peer-reviewed

    Shusuke Tomoshige, Minoru Ishikawa

    Bioorganic & Medicinal Chemistry　41　116221-116221　2021/05

    Publisher: Elsevier BV

    DOI： 10.1016/j.bmc.2021.116221 　

    ISSN： 0968-0896

  22. PROTACs and Other Chemical Protein Degradation Technologies for the Treatment of Neurodegenerative Disorders Peer-reviewed

    Shusuke Tomoshige, Minoru Ishikawa

    Angewandte Chemie International Edition　60　3346-3354　2021/02

    Publisher: Wiley

    DOI： 10.1002/anie.202004746 　

    ISSN： 1433-7851

    eISSN： 1521-3773

  23. meta-Non-flat substituents: a novel molecular design to improve aqueous solubility in small molecule drug discovery International-journal Peer-reviewed

    Yuki Ichikawa, Michiaki Hiramatsu, Yusuke Mita, Makoto Makishima, Yotaro Matsumoto, Yui Masumoto, Atsuya Muranaka, Masanobu Uchiyama, Yuichi Hashimoto, Minoru Ishikawa

    Organic & Biomolecular Chemistry　19　(2)　446-456　2021/01

    Publisher: Royal Society of Chemistry (RSC)

    DOI： 10.1039/d0ob02083d 　

    ISSN： 1477-0520

    eISSN： 1477-0539

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    <p>We found a novel molecular design for improvement in the aqueous solubility of small molecule drugs.</p>

  24. Image-based screen capturing misfolding status of Niemann-Pick type C1 identifies potential candidates for chaperone drugs Peer-reviewed

    Ryuta Shioi, Fumika Karaki, Hiromasa Yoshioka, Tomomi Noguchi-Yachide, Minoru Ishikawa, Kosuke Dodo, Yuichi Hashimoto, Mikiko Sodeoka, Kenji Ohgane

    PLOS ONE　15　(12)　e0243746-e0243746　2020/12

    Publisher: Public Library of Science (PLoS)

    DOI： 10.1371/journal.pone.0243746 　

    eISSN： 1932-6203

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    Niemann-Pick disease type C is a rare, fatal neurodegenerative disorder characterized by massive intracellular accumulation of cholesterol. In most cases, loss-of-function mutations in the <italic>NPC1</italic> gene that encodes lysosomal cholesterol transporter NPC1 are responsible for the disease, and more than half of the mutations are considered to interfere with the biogenesis or folding of the protein. We previously identified a series of oxysterol derivatives and phenanthridine-6-one derivatives as pharmacological chaperones, i.e., small molecules that can rescue folding-defective phenotypes of mutated NPC1, opening up an avenue to develop chaperone therapy for Niemann-Pick disease type C. Here, we present an improved image-based screen for NPC1 chaperones and we describe its application for drug-repurposing screening. We identified some azole antifungals, including itraconazole and posaconazole, and a kinase inhibitor, lapatinib, as probable pharmacological chaperones. A photo-crosslinking study confirmed direct binding of itraconazole to a representative folding-defective mutant protein, NPC1-I1061T. Competitive photo-crosslinking experiments suggested that oxysterol-based chaperones and itraconazole share the same or adjacent binding site(s), and the sensitivity of the crosslinking to P691S mutation in the sterol-sensing domain supports the hypothesis that their binding sites are located near this domain. Although the azoles were less effective in reducing cholesterol accumulation than the oxysterol-derived chaperones or an HDAC inhibitor, LBH-589, our findings should offer new starting points for medicinal chemistry efforts to develop better pharmacological chaperones for NPC1.

  25. 神経変性疾患治療に向けたタンパク質分解アプローチ Invited Peer-reviewed

    友重秀介、石川稔

    実験医学　38　(14)　2326-2330　2020/08

  26. 疾患疾患原因タンパク質の寿命を短縮する分子の創製と医薬応用への課題 Invited Peer-reviewed

    石川稔

    Drug Delivery System　35　(3)　229-239　2020/07

  27. 生細胞内の疾患関連タンパク質を 減少させる低分子創薬手法の開発 Invited Peer-reviewed

    石川稔, 橋本祐一

    有機合成化学協会誌　78　(5)　402-413　2020/05

  28. Selective Degradation of Target Proteins by Chimeric Small-Molecular Drugs, PROTACs and SNIPERs. International-journal Peer-reviewed

    Minoru Ishikawa, Shusuke Tomoshige, Yosuke Demizu, Mikihiko Naito

    Pharmaceuticals (Basel, Switzerland)　13　(4)　74　2020/04/21

    DOI： 10.3390/ph13040074 　

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    New therapeutic modalities are needed to address the problem of pathological but undruggable proteins. One possible approach is the induction of protein degradation by chimeric drugs composed of a ubiquitin ligase (E3) ligand coupled to a ligand for the target protein. This article reviews chimeric drugs that decrease the level of specific proteins such as proteolysis targeting chimeric molecules (PROTACs) and specific and nongenetic inhibitor of apoptosis protein (IAP)-dependent protein erasers (SNIPERs), which target proteins for proteasome-mediated degradation. We cover strategies for increasing the degradation activity induced by small molecules, and their scope for application to undruggable proteins.

  29. Application of protein knockdown strategy targeting β-sheet structure to multiple disease-associated polyglutamine proteins. International-journal Peer-reviewed

    Hiroko Yamashita, Shusuke Tomoshige, Sayaka Nomura, Kenji Ohgane, Yuichi Hashimoto, Minoru Ishikawa

    Bioorganic & medicinal chemistry　28　(1)　115175-115175　2020

    DOI： 10.1016/j.bmc.2019.115175 　

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    Polyglutamine diseases are a class of neurodegenerative diseases associated with the accumulation of aggregated mutant proteins. We previously developed a class of degradation-inducing agents targeting the β-sheet-rich structure typical of such aggregates, and we showed that these agents dose-, time-, and proteasome-dependently decrease the intracellular level of mutant huntingtin with an extended polyglutamine tract, which correlates well with the severity of Huntington's disease. Here, we demonstrate that the same agents also deplete other polyglutamine disease-related proteins: mutant ataxin-3 and ataxin-7 in cells from spino-cerebellar ataxia patients, and mutant atrophin-1 in cells from dentatorubral-pallidoluysian atrophy patients. Targeting cross-β-sheet structure could be an effective design strategy to develop therapeutic agents for multiple neurodegenerative diseases.

  30. Efficient Lead Finding, Activity Enhancement and Preliminary Selectivity Control of Nuclear Receptor Ligands Bearing a Phenanthridinone Skeleton Peer-reviewed

    Yuko Nishiyama, Shinya Fujii, Makoto Makishima, Yuichi Hashimoto, Minoru Ishikawa

    International Journal of Molecular Sciences　2018/07

    DOI： 10.3390/ijms19072090 　

  31. Structural development of tetrachlorophthalimides as liver X receptor β (LXRβ)-selective agonists with improved aqueous solubility Peer-reviewed

    Sayaka Nomura, Kaori Endo-Umeda, Shinya Fujii, Makoto Makishima, Yuichi Hashimoto, Minoru Ishikawa

    Bioorganic and Medicinal Chemistry Letters　28　(4)　796-801　2018/02/15

    Publisher: Elsevier Ltd

    DOI： 10.1016/j.bmcl.2017.12.024 　

    ISSN： 1464-3405 0960-894X

  32. Degradation of huntingtin mediated by a hybrid molecule composed of IAP antagonist linked to phenyldiazenyl benzothiazole derivative Peer-reviewed

    Shusuke Tomoshige, Sayaka Nomura, Kenji Ohgane, Yuichi Hashimoto, Minoru Ishikawa

    Bioorganic and Medicinal Chemistry Letters　28　(4)　707-710　2018/02/15

    Publisher: Elsevier Ltd

    DOI： 10.1016/j.bmcl.2018.01.012 　

    ISSN： 1464-3405 0960-894X

  33. 神経変性疾患原因タンパク質のケミカルノックダウン Invited

    石川稔, 友重秀介, 野村さやか, 山下博子, 大金賢司

    MEDCHEM NEWS　28　88-92　2018

  34. Unexpected emergence of luciferase-inhibitory activity during structural development study of phenyloxadiazole-based PPAR ligands Peer-reviewed

    hioi R, Toyota Y, Noguchi-Yachide T, Ishikawa M, Yamaguchi T, Makishima M, Hashimoto Y, Ohgane K

    Heterocycles　97　(2)　854-864　2018

  35. Novel Nonsteroidal Progesterone Receptor (PR) Antagonists with a Phenanthridinone Skeleton Peer-reviewed

    Nishiyama Y, Mori S, Makishima M, Fujii S, Kagechika H, Hashimoto Y, Ishikawa M

    ACS Medicinal Chemistry Letters　9　(7)　641-645　2018

    DOI： 10.1021/acsmedchemlett.8b00058 　

  36. Photo-enhanced Aqueous Solubilization of an Azo-compound Peer-reviewed

    Minoru Ishikawa, Takuya Ohzono, Takao Yamaguchi, Yasuo Norikane

    Scientific Reports　7　6909　2017/12/01

    Publisher: Nature Publishing Group

    DOI： 10.1038/s41598-017-06947-w 　

    ISSN： 2045-2322

  37. Structural development studies of pyrazoloketone-derived acetyl-CoA carboxylase inhibitors Peer-reviewed

    Heterocycles　2017/12

  38. Structural basis for specific cleavage of Lys6-linked polyubiquitin chains by USP30. International-journal Peer-reviewed

    Yusuke Sato, Kei Okatsu, Yasushi Saeki, Koji Yamano, Noriyuki Matsuda, Ai Kaiho, Atsushi Yamagata, Sakurako Goto-Ito, Minoru Ishikawa, Yuichi Hashimoto, Keiji Tanaka, Shuya Fukai

    Nature structural & molecular biology　24　(11)　911-919　2017/11

    DOI： 10.1038/nsmb.3469 　

  39. Discovery of Small Molecules that Induce the Degradation of Huntingtin Peer-reviewed

    Shusuke Tomoshige, Sayaka Nomura, Kenji Ohgane, Yuichi Hashimoto, Minoru Ishikawa

    ANGEWANDTE CHEMIE-INTERNATIONAL EDITION　56　(38)　11530-11533　2017/09

    DOI： 10.1002/anie.201706529 　

    ISSN： 1433-7851

    eISSN： 1521-3773

  40. 1 alpha-Hydroxy derivatives of 7-dehydrocholesterol are selective liver X receptor modulators Peer-reviewed

    Kaori Endo-Umeda, Atsushi Aoyama, Masato Shimizu, Minoru Ishikawa, Yuichi Hashimoto, Sachiko Yamada, Makoto Makishima

    JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY　172　136-148　2017/09

    DOI： 10.1016/j.jsbmb.2017.07.014 　

    ISSN： 0960-0760

  41. Specific fluorescence labeling of target proteins by using a ligand-4-azidophthalimide conjugate Peer-reviewed

    Kosuke Chiba, Miwako Asanuma, Minoru Ishikawa, Yuichi Hashimoto, Kosuke Dodo, Mikiko Sodeoka, Takao Yamaguchi

    CHEMICAL COMMUNICATIONS　53　(62)　8751-8754　2017/08

    DOI： 10.1039/c7cc03252h 　

    ISSN： 1359-7345

    eISSN： 1364-548X

  42. Switching subtype-selectivity: Fragment replacement strategy affords novel class of peroxisome proliferator-activated receptor alpha/delta (PPAR alpha/delta) dual agonists Peer-reviewed

    Ryuta Shioi, Shogo Okazaki, Tomomi Noguchi-Yachide, Minoru Ishikawa, Makoto Makishima, Yuichi Hashimoto, Takao Yamaguchi

    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS　27　(14)　3131-3134　2017/07

    DOI： 10.1016/j.bmcl.2017.05.037 　

    ISSN： 0960-894X

    eISSN： 1464-3405

  43. Structure-activity relationships of rosiglitazone for peroxisome proliferator-activated receptor gamma transrepression Peer-reviewed

    Yosuke Toyota, Sayaka Nomura, Makoto Makishima, Yuichi Hashimoto, Minoru Ishikawa

    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS　27　(12)　2776-2780　2017/06

    DOI： 10.1016/j.bmcl.2017.04.061 　

    ISSN： 0960-894X

    eISSN： 1464-3405

  44. Phenanthridin-6-one derivatives as the first class of non-steroidal pharmacological chaperones for Niemann-Pick disease type C1 protein Peer-reviewed

    Hiromitsu Fukuda, Fumika Karaki, Kosuke Dodo, Tomomi Noguchi-Yachide, Minoru Ishikawa, Yuichi Hashimoto, Kenji Ohgane

    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS　27　(12)　2781-2787　2017/06

    DOI： 10.1016/j.bmcl.2017.04.062 　

    ISSN： 0960-894X

    eISSN： 1464-3405

  45. Targeted degradation of proteins localized in subcellular compartments by hybrid small molecules Peer-reviewed

    Keiichiro Okuhira, Takuji Shoda, Risa Omura, Nobumichi Ohoka, Takayuki Hattori, Norihito Shibata, Yosuke Demizu, Ryo Sugihara, Asato Ichino, Haruka Kawahara, Yukihiro Itoh, Minoru Ishikawa, Yuichi Hashimoto, Masaaki Kurihara, Susumu Itoh, Hiroyuki Saito, Mikihiko Naito

    Molecular Pharmacology　91　(3)　159-166　2017/03

    DOI： 10.1124/mol.116.105569 　

    ISSN： 0026-895X

    eISSN： 1521-0111

  46. Structure-activity relationship studies of non-carboxylic acid peroxisome proliferator-activated receptor alpha/delta (PPAR alpha/delta) dual agonists Peer-reviewed

    Shogo Okazaki, Ryuta Shioi, Tomomi Noguchi-Yachide, Minoru Ishikawa, Makoto Makishima, Yuichi Hashimoto, Takao Yamaguchi

    BIOORGANIC & MEDICINAL CHEMISTRY　24　(21)　5455-5461　2016/11

    DOI： 10.1016/j.bmc.2016.08.067 　

    ISSN： 0968-0896

    eISSN： 1464-3391

  47. Discovery of N-(1-(3-(4-phenoxyphenyl)-1,2,4-oxadiazol-5-yl)ethyl)acetamides as novel acetyl-CoA carboxylase 2 (ACC2) inhibitors with peroxisome proliferator-activated receptor alpha/delta (PPAR alpha/delta) dual agonistic activity Peer-reviewed

    Shogo Okazaki, Tomomi Noguchi-Yachide, Taki Sakai, Minoru Ishikawa, Makoto Makishima, Yuichi Hashimoto, Takao Yamaguchi

    BIOORGANIC & MEDICINAL CHEMISTRY　24　(21)　5258-5269　2016/11

    DOI： 10.1016/j.bmc.2016.08.045 　

    ISSN： 0968-0896

    eISSN： 1464-3391

  48. Development of Tetrachlorophthalimides as Liver X Receptor beta (LXR beta)-Selective Agonists Peer-reviewed

    Sayaka Nomura, Kaori Endo-Umeda, Makoto Makishima, Yuichi Hashimoto, Minoru Ishikawa

    CHEMMEDCHEM　11　(20)　2347-2360　2016/10

    DOI： 10.1002/cmdc.201600305 　

    ISSN： 1860-7179

    eISSN： 1860-7187

  49. Improvement in Aqueous Solubility of Retinoic Acid Receptor (RAR) Agonists by Bending the Molecular Structure Peer-reviewed

    Michiaki Hiramatsu, Yuki Ichikawa, Shusuke Tomoshige, Makoto Makishima, Atsuya Muranaka, Masanobu Uchiyama, Takao Yamaguchi, Yuichi Hashimoto, Minoru Ishikawa

    CHEMISTRY-AN ASIAN JOURNAL　11　(15)　2210-2217　2016/08

    DOI： 10.1002/asia.201600744 　

    ISSN： 1861-4728

    eISSN： 1861-471X

  50. Efficient protein knockdown of HaloTag-fused proteins using hybrid molecules consisting of IAP antagonist and HaloTag ligand Peer-reviewed

    Shusuke Tomoshige, Yuichi Hashimoto, Minoru Ishikawa

    BIOORGANIC & MEDICINAL CHEMISTRY　24　(14)　3144-3148　2016/07

    DOI： 10.1016/j.bmc.2016.05.035 　

    ISSN： 0968-0896

    eISSN： 1464-3391

  51. Improving the Water-Solubility of Compounds By Molecular Modification to Disrupt Crystal Packing Peer-reviewed

    Minoru Ishikawa, Yuichi Hashimoto

    The Practice of Medicinal Chemistry: Fourth Edition　747-765　2015/08/28

    Publisher: Elsevier Inc.

    DOI： 10.1016/B978-0-12-417205-0.00031-6 　

  52. Styrylphenylphthalimides as Novel Transrepression-Selective Liver X Receptor (LXR) Modulators Peer-reviewed

    Sayaka Nomura, Kaori Endo-Urneda, Atsushi Aoyama, Makoto Makishima, Yuichi Hashimoto, Minoru Ishikawa

    ACS MEDICINAL CHEMISTRY LETTERS　6　(8)　902-907　2015/08

    DOI： 10.1021/acsmedchemlett.5b00170 　

    ISSN： 1948-5875

  53. Design and synthesis of silicon-containing fatty acid amide derivatives as novel peroxisome proliferator-activated receptor (PPAR) agonists Peer-reviewed

    Daisuke Kajita, Masaharu Nakamura, Yotaro Matsumoto, Minoru Ishikawa, Yuichi Hashimoto, Shinya Fujii

    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS　25　(16)　3350-3354　2015/08

    DOI： 10.1016/j.bmcl.2015.05.045 　

    ISSN： 0960-894X

    eISSN： 1464-3405

  54. Structure-activity relationships of benzhydrol derivatives based on 1 '-acetoxychavicol acetate (ACA) and their inhibitory activities on multiple myeloma cell growth via inactivation of the NF-kappa B pathway Peer-reviewed

    Takashi Misawa, Kosuke Dodo, Minoru Ishikawa, Yuichi Hashimoto, Morihiko Sagawa, Masahiro Kizaki, Hiroshi Aoyama

    BIOORGANIC & MEDICINAL CHEMISTRY　23　(9)　2241-2246　2015/05

    DOI： 10.1016/j.bmc.2015.02.039 　

    ISSN： 0968-0896

    eISSN： 1464-3391

  55. Design, synthesis and structure-activity relationship studies of novel sirtuin 2 (SIRT2) inhibitors with a benzamide skeleton Peer-reviewed

    Taki Sakai, Yotaro Matsumoto, Minoru Ishikawa, Kazuyuki Sugita, Yuichi Hashimoto, Nobuhiko Wakai, Akio Kitao, Era Morishita, Chikashi Toyoshima, Tomoatsu Hayashi, Tetsu Akiyama

    BIOORGANIC & MEDICINAL CHEMISTRY　23　(2)　328-339　2015/01

    DOI： 10.1016/j.bmc.2014.11.027 　

    ISSN： 0968-0896

    eISSN： 1464-3391

  56. Degradation of HaloTag-fused nuclear proteins using bestatin-HaloTag ligand hybrid molecules Peer-reviewed

    Shusuke Tomoshige, Mikihiko Naito, Yuichi Hashimoto, Minoru Ishikawa

    ORGANIC & BIOMOLECULAR CHEMISTRY　13　(38)　9746-9750　2015

    DOI： 10.1039/c5ob01395j 　

    ISSN： 1477-0520

    eISSN： 1477-0539

  57. Structure-activity relationship-guided development of retinoic acid receptor-related orphan receptor gamma (ROR gamma)-selective inverse agonists with a phenanthridin-6(5H)-one skeleton from a liver X receptor ligand Peer-reviewed

    Yuko Nishiyama, Masahiko Nakamura, Takashi Misawa, Madoka Nakagomi, Makoto Makishima, Minoru Ishikawa, Yuichi Hashimoto

    BIOORGANIC & MEDICINAL CHEMISTRY　22　(9)　2799-2808　2014/05

    DOI： 10.1016/j.bmc.2014.03.007 　

    ISSN： 0968-0896

    eISSN： 1464-3391

  58. 7-Dehydrocholesterol metabolites produced by sterol 27-hydroxylase (CYP27A1) modulate liver X receptor activity Peer-reviewed

    Kaori Endo-Umeda, Kaori Yasuda, Kazuyuki Sugita, Akira Honda, Miho Ohta, Minoru Ishikawa, Yuichi Hashimoto, Toshiyuki Sakaki, Makoto Makishima

    JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY　140　7-16　2014/03

    DOI： 10.1016/j.jsbmb.2013.11.010 　

    ISSN： 0960-0760

  59. Structure-activity relationships of bisphenol a analogs at estrogen receptors (ERs): Discovery of an ERα-selective antagonist Peer-reviewed

    Keisuke Maruyama, Masaharu Nakamura, Shusuke Tomoshige, Kazuyuki Sugita, Makoto Makishima, Yuichi Hashimoto, Minoru Ishikawa

    Bioorganic and Medicinal Chemistry Letters　23　(14)　4031-4036　2013/07/15

    DOI： 10.1016/j.bmcl.2013.05.067 　

    ISSN： 0960-894X 1464-3405

  60. Improvement in Solubility in Small Molecule Drug Discovery Programs Focusing on Dihedral Angle and Symmetry Peer-reviewed

    Minoru Ishikawa, Yuichi Hashimoto

    JOURNAL OF SYNTHETIC ORGANIC CHEMISTRY JAPAN　71　(6)　625-636　2013/06

    DOI： 10.5059/yukigoseikyokaishi.71.625 　

    ISSN： 0037-9980

    eISSN： 1883-6526

  61. Structure-activity relationship of benzodiazepine derivatives as LXXLL peptide mimetics that inhibit the interaction of vitamin D receptor with coactivators Peer-reviewed

    Yusuke Mita, Kosuke Dodo, Tomomi Noguchi-Yachide, Yuichi Hashimoto, Minoru Ishikawa

    BIOORGANIC & MEDICINAL CHEMISTRY　21　(4)　993-1005　2013/02

    DOI： 10.1016/j.bmc.2012.11.042 　

    ISSN： 0968-0896

  62. Small-molecular, non-peptide, non-ATP-competitive polo-like kinase 1 (Plk1) inhibitors with a terphenyl skeleton Peer-reviewed

    Yusuke Mita, Tomomi Noguchi-Yachide, Minoru Ishikawa, Yuichi Hashimoto

    Bioorganic and Medicinal Chemistry　21　(3)　608-617　2013/02/01

    DOI： 10.1016/j.bmc.2012.11.054 　

    ISSN： 0968-0896 1464-3391

  63. Design, Synthesis, and Biological Evaluation of Novel Transrepression-Selective Liver X Receptor (LXR) Ligands with 5,11-Dihydro-5-methyl-11-methylene-6H-dibenz[b,e]azepin-6-one Skeleton Peer-reviewed

    Atsushi Aoyama, Kaori Endo-Umeda, Kenji Kishida, Kenji Ohgane, Tomomi Noguchi-Yachide, Hiroshi Aoyama, Minoru Ishikawa, Hiroyuki Miyachi, Makoto Makishima, Yuichi Hashimoto

    JOURNAL OF MEDICINAL CHEMISTRY　55　(17)　7360-7377　2012/09

    DOI： 10.1021/jm3002394 　

    ISSN： 0022-2623

    eISSN： 1520-4804

  64. Double protein knockdown of cIAP1 and CRABP-II using a hybrid molecule consisting of ATRA and IAPs antagonist Peer-reviewed

    Yukihiro Itoh, Minoru Ishikawa, Risa Kitaguchi, Keiichiro Okuhira, Mikihiko Naito, Yuichi Hashimoto

    Bioorganic and Medicinal Chemistry Letters　22　(13)　4453-4457　2012/07/01

    DOI： 10.1016/j.bmcl.2012.04.134 　

    ISSN： 0960-894X

    eISSN： 1464-3405

  65. Design, synthesis and biological evaluation of nuclear receptor-degradation inducers Peer-reviewed

    Yukihiro Itoh, Risa Kitaguchi, Minoru Ishikawa, Mikihiko Naito, Yuichi Hashimoto

    Bioorganic and Medicinal Chemistry　19　(22)　6768-6778　2011/11/15

    DOI： 10.1016/j.bmc.2011.09.041 　

    ISSN： 0968-0896

    eISSN： 1464-3391

  66. CONFIRMATION OF MOLECULAR PLANARITY DISRUPTION.. EFFECT ON AQUEOUS SOLUBILITY IMPROVEMENT OF beta-NAPHTHOFLAVONE ANALOGS Peer-reviewed

    Yuji Fujita, Mitsuhiro Yonehara, Katsushi Kitahara, Jun Shimokawa, Yuichi Hashimoto, Minoru Ishikawa

    HETEROCYCLES　83　(11)　2563-2575　2011/11

    DOI： 10.3987/COM-11-12352 　

    ISSN： 0385-5414

  67. Inhibition of Restriction Enzymes EcoRI, BamHI and HindIII by Phenethylphenylphthalimides Derived from Thalidomide Peer-reviewed

    Kazunori Motoshima, Minoru Ishikawa, Yuichi Hashimoto, Kazuyuki Sugita

    CHEMICAL & PHARMACEUTICAL BULLETIN　59　(7)　880-884　2011/07

    DOI： 10.1248/cpb.59.880 　

    ISSN： 0009-2363

  68. Development of target protein-selective degradation inducer for protein knockdown Peer-reviewed

    Yukihiro Itoh, Minoru Ishikawa, Risa Kitaguchi, Shinichi Sato, Mikihiko Naito, Yuichi Hashimoto

    Bioorganic and Medicinal Chemistry　19　(10)　3229-3241　2011/05/15

    DOI： 10.1016/j.bmc.2011.03.057 　

    ISSN： 0968-0896

    eISSN： 1464-3391

  69. Peroxisome proliferator-activated receptor agonists with phenethylphenylphthalimide skeleton derived from thalidomide-related liver X receptor antagonists: Relationship between absolute configuration and subtype selectivity Peer-reviewed

    Kazunori Motoshima, Minoru Ishikawa, Yuichi Hashimoto, Kazuyuki Sugita

    BIOORGANIC & MEDICINAL CHEMISTRY　19　(10)　3156-3172　2011/05

    DOI： 10.1016/j.bmc.2011.03.065 　

    ISSN： 0968-0896

  70. Non-competitive and selective dipeptidyl peptidase IV inhibitors with phenethylphenylphthalimide skeleton derived from thalidomide-related alpha-glucosidase inhibitors and liver X receptor antagonists Peer-reviewed

    Kazunori Motoshima, Kazuyuki Sugita, Yuichi Hashimoto, Minoru Ishikawa

    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS　21　(10)　3041-3045　2011/05

    DOI： 10.1016/j.bmcl.2011.03.026 　

    ISSN： 0960-894X

  71. Specific degradation of CRABP-II via cIAP1-mediated ubiquitylation induced by hybrid molecules that crosslink cIAP1 and the target protein Peer-reviewed

    Keiichiro Okuhira, Nobumichi Ohoka, Kimie Sai, Tomoko Nishimaki-Mogami, Yukihiro Itoh, Minoru Ishikawa, Yuichi Hashimoto, Mikihiko Naito

    FEBS Letters　585　(8)　1147-1152　2011/04

    DOI： 10.1016/j.febslet.2011.03.019 　

    ISSN： 0014-5793

  72. FURTHER APPLICATION OF THE MULTI-TEMPLATE APPROACH FOR CREATION OF BIOLOGICAL RESPONSE MODIFIERS: DISCOVERY OF A NEW CLASS OF MULTIFUNCTIONAL ANTI-DIABETIC AGENTS Peer-reviewed

    Kazunori Motoshima, Tomomi Noguchi-Yachide, Minoru Ishikawa, Yuichi Hashimoto, Kazuyuki Sugita

    HETEROCYCLES　82　(2)　1083-+　2011/03

    DOI： 10.3987/REV-10-SR(E)7 　

    ISSN： 0385-5414

  73. Improvement in Aqueous Solubility in Small Molecule Drug Discovery Programs by Disruption of Molecular Planarity and Symmetry Peer-reviewed

    Minoru Ishikawa, Yuichi Hashimoto

    JOURNAL OF MEDICINAL CHEMISTRY　54　(6)　1539-1554　2011/03

    DOI： 10.1021/jm101356p 　

    ISSN： 0022-2623

  74. Novel selective anti-androgens with a diphenylpentane skeleton Peer-reviewed

    Keisuke Maruyama, Tomomi Noguchi-Yachide, Kazuyuki Sugita, Yuichi Hashimoto, Minoru Ishikawa

    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS　20　(22)　6661-6666　2010/11

    DOI： 10.1016/j.bmcl.2010.09.011 　

    ISSN： 0960-894X

  75. Improvement of water-solubility of biarylcarboxylic acid peroxisome proliferator-activated receptor (PPAR) delta-selective partial agonists by disruption of molecular planarity/symmetry Peer-reviewed

    Jun-ichi Kasuga, Minoru Ishikawa, Mitsuhiro Yonehara, Makoto Makishima, Yuichi Hashimoto, Hiroyuki Miyachi

    BIOORGANIC & MEDICINAL CHEMISTRY　18　(20)　7164-7173　2010/10

    DOI： 10.1016/j.bmc.2010.08.041 　

    ISSN： 0968-0896

  76. Development of tryptase inhibitors derived from thalidomide Peer-reviewed

    Masashi Tetsuhashi, Minoru Ishikawa, Mariko Hashimoto, Yuichi Hashimoto, Hiroshi Aoyama

    BIOORGANIC & MEDICINAL CHEMISTRY　18　(14)　5323-5338　2010/07

    DOI： 10.1016/j.bmc.2010.05.037 　

    ISSN： 0968-0896

  77. Anti-influenza activity of phenethylphenylphthalimide analogs derived from thalidomide Peer-reviewed

    Yuma Iwai, Hitoshi Takahashi, Dai Hatakeyama, Kazunori Motoshima, Minoru Ishikawa, Kazuyuki Sugita, Yuichi Hashimoto, Yuichi Harada, Shigeyuki Itamura, Takato Odagiri, Masato Tashiro, Yoshihisa Sei, Kentaro Yamaguchi, Takashi Kuzuhara

    BIOORGANIC & MEDICINAL CHEMISTRY　18　(14)　5379-5390　2010/07

    DOI： 10.1016/j.bmc.2010.05.035 　

    ISSN： 0968-0896

    eISSN： 1464-3391

  78. Protein knockdown using methyl bestatin-ligand hybrid molecules: Design and synthesis of inducers of ubiquitination-mediated degradation of cellular retinoic acid-binding proteins Peer-reviewed

    Yukihiro Itoh, Minoru Ishikawa, Mikihiko Naito, Yuichi Hashimoto

    Journal of the American Chemical Society　132　(16)　5820-5826　2010/04

    DOI： 10.1021/ja100691p 　

    ISSN： 0002-7863

    eISSN： 1520-5126

  79. LXXLL peptide mimetics as inhibitors of the interaction of vitamin D receptor with coactivators Peer-reviewed

    Yusuke Mita, Kosuke Dodo, Tomomi Noguchi-Yachide, Hiroyuki Miyachi, Makoto Makishima, Yuichi Hashimoto, Minoru Ishikawa

    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS　20　(5)　1712-1717　2010/03

    DOI： 10.1016/j.bmcl.2010.01.079 　

    ISSN： 0960-894X

  80. beta-Naphthoflavone analogs as potent and soluble aryl hydrocarbon receptor agonists: Improvement of solubility by disruption of molecular planarity Peer-reviewed

    Yuji Fujita, Mitsuhiro Yonehara, Masashi Tetsuhashi, Tomomi Noguchi-Yachide, Yuichi Hashimoto, Minoru Ishikawa

    BIOORGANIC & MEDICINAL CHEMISTRY　18　(3)　1194-1203　2010/02

    DOI： 10.1016/j.bmc.2009.12.036 　

    ISSN： 0968-0896

  81. Glycogen Phosphorylase a Inhibitors with a Phenethylphenylphthalimide Skeleton Derived from Thalidomide-Related alpha-Glucosidase Inhibitors and Liver X Receptor Antagonists Peer-reviewed

    Kazunori Motoshima, Minoru Ishikawa, Kazuyuki Sugita, Yuichi Hashimoto

    BIOLOGICAL & PHARMACEUTICAL BULLETIN　32　(9)　1618-1620　2009/09

    DOI： 10.1248/bpb.32.1618 　

    ISSN： 0918-6158

  82. Separation of alpha-glucosidase-inhibitory and liver X receptor-antagonistic activities of phenethylphenyl phthalimide analogs and generation of LXR alpha-selective antagonists Peer-reviewed

    Kazunori Motoshima, Tomomi Noguchi-Yachide, Kazuyuki Sugita, Yuichi Hashimoto, Minoru Ishikawa

    BIOORGANIC & MEDICINAL CHEMISTRY　17　(14)　5001-5014　2009/07

    DOI： 10.1016/j.bmc.2009.05.066 　

    ISSN： 0968-0896

  83. Pseurotin A and its analogues as inhibitors of immunoglobuline E production Peer-reviewed

    Minoru Ishikawa, Tomohisa Ninomiya, Hirotomo Akabane, Nobuaki Kushida, Go Tsujiuchi, Makoto Ohyama, Shuichi Gomi, Keiko Shito, Takashi Murata

    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS　19　(5)　1457-1460　2009/03

    DOI： 10.1016/j.bmcl.2009.01.029 　

    ISSN： 0960-894X

  84. Synthesis of Potent alpha(v)beta(3)/alpha(IIb)beta(3) Dual Antagonists Tricyclic Pharmaeophore-based Molecules and Their Selectivity Control Peer-reviewed

    Minoru Ishikawa, Dai Kubota, Keiichi Ajito

    JOURNAL OF SYNTHETIC ORGANIC CHEMISTRY JAPAN　66　(11)　1093-1104　2008/11

    ISSN： 0037-9980

  85. Chemical Modification of Pseurotin A: One-pot Synthesis of Synerazol and Pseurotin E and Determination of Absolute Stereochemistry of Pseurotin E Peer-reviewed

    Minoru Ishikawa, Tomohisa Ninomiya

    JOURNAL OF ANTIBIOTICS　61　(11)　692-695　2008/11

    DOI： 10.1038/ja.2008.99 　

    ISSN： 0021-8820

  86. A scalable synthesis of MN-447, an antagonist for integrins alpha(v)beta(3) and alpha(IIb)beta(3) Peer-reviewed

    Minoru Ishikawa, Masaki Tsushima, Dai Kubota, Yumiko Yanagisawa, Yukiko Hiraiwa, Yasuo Kojima, Kojima Ajito, Naomichi Anzai

    ORGANIC PROCESS RESEARCH & DEVELOPMENT　12　(4)　596-602　2008/07

    DOI： 10.1021/op800073z 　

    ISSN： 1083-6160

  87. Enantioselective total synthesis of (+)-sarcodictyenone Peer-reviewed

    Takako Yamazaki, Minoru Ishikawa, Miki Uemura, Yuko Kanda, Hisashi Takei, Morio Asaoka

    TETRAHEDRON　64　(8)　1895-1900　2008/02

    DOI： 10.1016/j.tet.2007.11.088 　

    ISSN： 0040-4020

  88. Tricyclic pharmacophore-based molecules as novel integrin alpha(v)beta(3) antagonists. Part IV: Preliminary control of alpha(v)beta(3) selectivity by meta-oriented substitution Peer-reviewed

    D Kubota, M Ishikawa, M Ishikawa, N Yahata, S Murakami, K Fujishima, M Kitakaze, K Ajito

    BIOORGANIC & MEDICINAL CHEMISTRY　14　(12)　4158-4181　2006/06

    DOI： 10.1016/j.bmc.2006.01.062 　

    ISSN： 0968-0896

  89. Tricyclic pharmacophore-based molecules as novel integrin alpha(v)beta(3) antagonists. Part III: Synthesis of potent antagonists with alpha(v)beta(3)/alpha(IIb)beta(3) dual activity and improved water solubility Peer-reviewed

    M Ishikawa, Y Hiraiwa, D Kubota, M Tsushima, T Watanabe, S Murakami, S Ouchi, K Ajito

    BIOORGANIC & MEDICINAL CHEMISTRY　14　(7)　2131-2150　2006/04

    DOI： 10.1016/j.bmc.2005.10.055 　

    ISSN： 0968-0896

  90. Tricyclic pharmacophore-based molecules as novel integrin alpha(v)beta(3) antagonists. Part 2: Synthesis of potent alpha(v)beta(3)/alpha(IIb)beta(3) dual antagonists Peer-reviewed

    M Ishikawa, D Kubota, M Yamamoto, C Kuroda, M Iguchi, A Koyanagi, S Murakami, K Ajito

    BIOORGANIC & MEDICINAL CHEMISTRY　14　(7)　2109-2130　2006/04

    DOI： 10.1016/j.bmc.2005.10.061 　

    ISSN： 0968-0896

  91. Tricyclic pharmacophore-based molecules as novel integrin alpha(v)beta(3) antagonists. Part 1: Design and synthesis of a lead compound exhibiting alpha(v)beta(3)/alpha(IIb)beta(3) dual antagonistic activity Peer-reviewed

    D Kubota, M Ishikawa, M Yamamoto, S Murakami, M Hachisu, K Katano, K Ajito

    BIOORGANIC & MEDICINAL CHEMISTRY　14　(7)　2089-2108　2006/04

    DOI： 10.1016/j.bmc.2005.10.060 　

    ISSN： 0968-0896

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    ファルマシア　61　(8)　761-761　2025/08

    DOI： 10.14894/faruawpsj.61.8_761 　

  2. 標的タンパク質分解薬 Invited Peer-reviewed

    石川稔, 伊藤拓水, 伊藤幸裕, 友重秀介

    現代化学　643　51-57　2024/09

  3. 脳移行性を示す神経変性タンパク質分解薬 Invited Peer-reviewed

    石川稔

    化学と工業　77　493　2024/07

  4. Development of practical fluorescent probes by improving water solubility

    神保大地, 友重秀介, 佐藤伸一, 佐藤伸一, 花岡健二郎, 宮本和範, 松本洋太郎, 石川稔

    メディシナルケミストリーシンポジウム講演要旨集　39th (CD-ROM)　2022

    ISSN： 0919-214X

  5. 標的タンパク質を分解する低分⼦ 〜疾患関連タンパク質をゴミ箱へ〜 Invited Peer-reviewed

    石川稔

    生命化学研究レター　62　(4)　9-14　2021/04

  6. 標的タンパク質分解薬の動向ーPROTACsの先を見据えて Invited

    石川稔, 友重秀介

    月刊化学　75　(12)　70-71　2020/11

  7. Excellence in Medicinal Chemistry Research from Japan Peer-reviewed

    Shaomeng Wang、Gunda Georg、Minoru Ishikawa、Tomohiko Ohwada、Satoshi Shuto、Takayoshi Suzuki

    Journal of Medicinal Chemistry　63　(17)　8877-8879　2020/08

  8. 高活性なリガンド創出に向けたユビキチンリガーゼcIAP1-BIR3ドメインの結晶構造解析

    岡部真琴, 佐藤伸一, 佐藤伸一, 横山武司, 友重秀介, 石川稔, 田中良和

    日本分子生物学会年会プログラム・要旨集(Web)　43rd　2020

  9. Cover Picture: Improvement in Aqueous Solubility of Retinoic Acid Receptor (RAR) Agonists by Bending the Molecular Structure (Chem. Asian J. 15/2016)

    Michiaki Hiramatsu, Yuki Ichikawa, Shusuke Tomoshige, Makoto Makishima, Atsuya Muranaka, Masanobu Uchiyama, Takao Yamaguchi, Yuichi Hashimoto, Minoru Ishikawa

    Chemistry - An Asian Journal　11　(15)　2086　2016/08/05

    Publisher: John Wiley and Sons Ltd

    DOI： 10.1002/asia.201600924 　

    ISSN： 1861-471X 1861-4728

  10. Liver X Receptor(LXR)リガンドの構造展開によるTransrepression作用選択的リガンドの創製

    青山惇, 梅田(遠藤)香織, 谷内出(野口)友美, 石川稔, 宮地弘幸, 槇島誠, 橋本祐一

    日本薬学会年会要旨集　132nd　(2)　2012

    ISSN： 0918-9823

  11. LXXLL peptide mimetics as inhibitors of the interaction of vitamin D recceptor with coactivators Invited

    Mita Yusuke, Hashimoto Yuichi, Ishikawa Minoru

    VITAMINS　85　(1)　25-26　2011

    Publisher: THE VITAMIN SOCIETY OF JAPAN

    DOI： 10.20632/vso.85.1_25 　

    ISSN： 0006-386X

  12. 2-I-18 LXXLL配列を模倣したビタミンD受容体-コアクチベーター相互作用阻害物質の創製(一般演題,日本ビタミン学会第62回大会発表要旨)

    三田 裕介, 〓〓 孝介, 谷内出 友美, 宮地 弘幸, 橋本 祐一, 石川 稔

    ビタミン　84　(4)　175-175　2010

    Publisher: 公益社団法人 日本ビタミン学会

    DOI： 10.20632/vso.84.4_175_2 　

    ISSN： 0006-386X

  13. インテグリンαvβ3/αIIbβ3デュアル拮抗作用を有するRGDペプチド等価体の創製 Invited

    石川 稔

    ペプチドニュースレター　77　4-6　2010

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Books and Other Publications 8

  1. 医療工学研究の最前線 ～近未来のバイオ医用機器, 生体材料, 創薬科学～

    石川稔, 友重秀介

    シーエムシー出版　2024/11

    ISBN: 9784781318219

  2. 創薬化学のすゝめ

    日本薬学会医薬化学部会　2023/06

  3. 研究開発の俯瞰報告書 ライフサイエンス・臨床医学分野（2023年）

    石川稔

    国立研究開発法人科学技術振興機構　2023/04

  4. 創薬科学・医薬化学

    橘高, 敦史

    化学同人　2022/10

    ISBN: 9784759823325

  5. 研究開発の俯瞰報告書 ライフサイエンス・臨床医学分野（2021年）

    石川稔

    国立研究開発法人科学技術振興機構　2021/04

  6. The Practice of Medicinal Chemistry, 4th edition

    Minoru Ishikawa, Yuichi Hashimoto

    2015

  7. 生体有機化学

    石川 稔

    東京化学同人　2012

  8. 創薬支援研究の展望

    石川稔, 味戸慶一

    シーエムシー出版　2008

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Presentations 60

  1. 神経変性疾患治療を指向した創薬化学研究 Invited

    石川稔

    九州大学薬学研究院セミナー　2025/07/10

  2. Targeted Protein Degradation in Mitochondria

    Sho NAKAMURA, Wakana YAMADA, Shusuke TOMOSHIGE, Minoru ISHIKAWA

    The 29th French-Japanese Symposium on Medical and Fine Chemistry　2025/05/19

  3. Novel drug discovery strategies for neurodegenerative disorders Invited

    Minoru Ishikawa

    Frontiers in Medicinal Chemistry 2025　2025/04/04

  4. 神経変性疾患治療を目指したケミカルバイオロジー Invited

    石川稔

    2024年度分子研異分野技術交流セミナー（第6回）　2024/11/29

  5. ミトコンドリア内タンパク質を標的とするタンパク質分解誘導薬の開発 Invited

    山田若菜, 佐藤伸一, 石川稔, 友重秀介

    第41回メディシナルケミストリーシンポジウム　2024/11/22

  6. Novel drug discovery for neurodegenerative disorders Invited

    石川稔

    令和6年度化学系学協会東北大会　2024/09/15

  7. 神経変性疾患治療を指向した創薬モダリティの提案 Invited

    石川稔

    星薬科大学学長セミナー　2024/04/26

  8. 標的タンパク質分解薬の創薬研究 Invited

    石川稔

    第９回 医薬品開発研究センターシンポジウム　2024/03/15

  9. 神経変性疾患治療を目指した有機化学的アプローチ Invited

    石川稔

    ニューモダリティと有機合成化学」研究部会 第10回勉強会　2023/11/27

  10. タンパク質分解薬の概要 Invited

    石川稔

    第40回メディシナルケミストリーシンポジウム つながり醸成企画ー未来を切り拓く創薬技術ー　2023/11/14

  11. Medicinal chemistry for neurodegenerative disorders Invited

    Minoru Ishikawa

    Tohoku University Chemistry Summer School 2023　2023/08/09

  12. PROTACs for neurodegenerative disorders Invited

    Minoru Ishikawa

    2nd Targeted Protein Degradation Conference in Japan　2023/07/26

  13. 新創薬モダリティを指向した創薬化学研究 Invited

    石川稔

    東京工業大学大学院ライフエンジニアリング特別講義第四- 低分子創薬の革新的モダリティーと最前線 -　2023/06/30

  14. 神経変性疾患治療に対する創薬手法 Invited

    石川稔

    日本薬学会東海支部特別講演会　2023/06/13

  15. 神経変性疾患治療を目指した有機化学的アプローチ Invited

    石川稔

    有機合成化学協会東北支部＿仙台地区春の講演会　2023/05/20

  16. Novel drug discovery for neurodegenerative disorders Invited

    Minoru Ishikawa

    日本薬学会第143年会 Frontiers in Synthetic Medicinal Chemistry 2023　2023/03/27

  17. 標的タンパク質を分解する低分子PROTACの創製 Invited

    石川稔

    日本農芸化学会2023年度広島大会シンポジウム ケモテクノロジーが拓くユビキチン研究の新潮流　2023/03/15

  18. Medicinal chemistry for neurodegenerative disorders Invited

    Minoru Ishikawa

    8th Seoul National University Symposium on Medicinal Chemistry　2023/01/13

  19. PROTACs for neurodegenerative disorders Invited

    Minoru Ishikawa

    the international symposium "Ubiquitin New Frontier ~from Neo-Biology to Targeted Protein Degradation~"　2022/12/04

  20. タンパク質分解薬の創製研究 Invited

    石川稔

    第54回若手ペプチド夏の勉強会　2022/08/08

  21. タンパク質分解の創薬 Invited

    石川稔

    東京薬科大学 生命科学部 公開講義　2022/07/05

  22. 細胞内の標的タンパク質を分解誘導する低分子 Invited

    石川稔

    第74回日本細胞生物学会大会 シンポジウム[新学術] ユビキチン研究のニューフロンティア　2022/06/28

  23. 標的タンパク質を分解誘導する低分子 Invited

    石川稔

    日本ケミカルバイオロジー学会第16回年会 新学術領域研究「ケモテクノロジーが拓くユビキチンニューフロンティア」共催ミニシンポジウム　2022/06/01

  24. 疾患関連タンパク質を分解誘導する低分子 Invited

    石川稔

    令和3年度第四回東名産学官・医連携研究会　2022/02/01

  25. Chemical biology of bioactive molecules Invited

    石川稔

    International Symposium for Interface Oral Health Science 2022　2022/01/15

  26. 凝集性タンパク質を分解するストラテジー Invited

    石川稔

    第40回日本認知症学会学術集会 オンラインシンポジウム新しいケミカルバイオロジー手法の開発と神経変性疾患への展開　2021/11

  27. 神経変性疾患の原因タンパク質分解薬の創製 Invited

    石川稔

    CBI学会 第424回研究講演会「プロテインノックダウン法による創薬パラダイムシフト」　2021/06/25

  28. 細胞内で標的タンパク質を減少させる機能性分子 Invited

    石川稔

    日本薬学会第141回年会シンポジウム 薬学における生命指向型化学（機能性分子を基軸とした生命現象の可視化・解明）　2021/03/29

  29. 分子間相互作用低下による生物活性物質の水溶性向上策 Invited

    石川稔

    日本薬学会第141回年会シンポジウム 薬学領域に貢献するメディシナルケミストリー最前線　2021/03/27

  30. 標的タンパク質を分解誘導するケミカルバイオロジー手法 Invited

    石川稔

    第93回日本生化学会大会 シンポジウム「化学で攻める新しい創薬のカタチ」　2020/09/15

  31. 細胞内の標的タンパク質を減少させる低分子 Invited

    石川稔

    日本薬学会第140年会 シンポジウム 薬学における生命指向型化学（革新的ケミカルツールを用いた生命科学研究の最前線）　2020/03/26

  32. 疾患関連タンパク質のケミカルノックダウンと神経変性疾患への展開 Invited

    石川 稔

    大正製薬株式会社講演会　2020/02/07

  33. 細胞内の疾患関連タンパク質を減少させる有機化学的手法 Invited

    石川 稔

    2019年度 後期（秋季）有機合成化学講習会 有機合成化学が切り拓く新しい世界－独創的アプローチの最前線－　2019/11/21

  34. ワルなタンパク質をぶっ壊す小柄な薬 Invited

    石川 稔

    第9回CSJ化学フェスタ2019 文科省科研費新学術領域研究「ケモテクノロジーが拓くユビキチンニューフロンティア」特別企画 ユビキチンは令和の新創薬ターゲット　2019/10/16

  35. 細胞内の標的タンパク質の寿命を短縮する低分子 Invited

    石川 稔

    第13回バイオ関連化学シンポジウム フォーカスドセッション「最先端合成化学を駆使したバイオ関連化学最前線」　2019/09/06

  36. Degradation of target proteins by small molecules Invited

    Minoru Ishikawa

    17th Annual Congress of International Drug Discovery Science & Technology　2019/07/25

  37. 低分子によるタンパク質ノックダウン Invited

    石川 稔

    日本ケミカルバイオロジー学会第14回年会 新学術領域研究「ケモユビキチン」共催ミニシンポジウム　2019/06/11

  38. 低分子創薬の守備範囲を拡げる有機化学的戦略：標的タンパク質のケミカルノックダウンと、水溶性を向上させる分子設計 Invited

    石川 稔

    東京理科大学理工学部生物有機化学特別セミナー　2019/05/24

  39. 標的タンパク質のケミカルノックダウンと応用展開 Invited

    石川 稔

    日本薬学会第139年会 シンポジウム 選択的タンパク質分解医薬品開発の最前線　2019/03/23

  40. 低分子創薬の守備範囲を拡げる戦略：標的タンパク質のケミカルノックダウンと、水溶性を向上させる分子設計 Invited

    石川 稔

    第23回神戸ポートアイランド創薬フォーラム　2018/12

  41. 標的タンパク質のケミカルノックダウン Invited

    石川 稔

    大塚創薬化学シンポジウム2018　2018/11

  42. Selective degradation of target proteins by small molecules Invited

    石川 稔

    The Third A3 Roundtable Meeting on Chemical Probe Research Hub　2018/11

  43. 標的タンパク質のケミカルノックダウン Invited

    石川 稔

    理化学研究所 Pioneering Project: Chemical Probe（生命現象探索分子）第一回合同合宿セミナー　2018/10

  44. 疾患関連タンパク質の寿命を縮める低分子 Invited

    石川 稔

    熊本大学工学部物質生命化学科 第７回生命化学セミナー　2018/10

  45. 薬らしい物性を指向した核内受容体リガンドの創製研究 Invited

    石川 稔

    日本レチノイド研究会第29回学術集会 若手シンポジウム　2018/10

  46. 低分子創薬の守備範囲を拡げる戦略：標的タンパク質のケミカルノックダウンと、水溶性を向上させる分子設計 Invited

    石川 稔

    名古屋大学大学院創薬科学研究科 第79回創薬科学セミナー　2018/07

  47. Selective degradation of target proteins by small molecules Invited

    石川 稔

    第2回A3若手研究者ミーティング　2018/07

  48. 低分子創薬のフィールドを拡げる手法開発：タンパク質分解誘導薬と水溶性向上策 Invited

    石川 稔

    大阪大学 新適塾「未来創薬への誘い」第42回　2018/04

  49. ユビキチン化により標的タンパク質を分解する低分子 Invited

    石川 稔

    第１回ユビキチン研究会　2018/01

  50. 「匠の化合物」で生命を操れるか？ Invited

    石川 稔

    第6回CSJ化学フェスタ2016 テーマ企画 私たちの生活に欠かせない有機合成化学！～「匠の技」で豊かな分子と社会を生み出そう！～　2016/11

  51. 低分子創薬のふたつの新戦略：タンパク質分解と、水溶性向上 Invited

    石川 稔

    第1回先端ケミカルバイオロジー研究会　2016/06

  52. タンパク質を特異的に分解する低分子の新展開 Invited

    石川 稔

    第30回バイオテクノロジー懇談会　2016/02

  53. 低分子によりタンパク質を特異的に減少させる「タンパク質ノックダウン法」の開発と応用 Invited

    石川 稔

    アステラス製薬株式会社講演会　2014/04

  54. タンパク質を特異的に分解誘導する低分子を利用した新治療戦略と低分子の標的タンパク質同定法 Invited

    石川 稔

    第86回日本生化学会大会 シンポジウム ケミカルライブラリースクリーニング再考 アカデミアで意味あるケミカルライブラリースクリーニングを実現するために　2013/09

  55. 細胞内レチノイン酸結合タンパク質（CRABP）を特異的に分解誘導する低分子の創製と新治療戦略 Invited

    石川 稔

    日本レチノイド研究会第24回学術集会 若手シンポジウム　2013/08

  56. タンパク質を特異的に分解する低分子の創製と応用 Invited

    石川 稔

    東京大学 第17回分生研シンポジウム　2012/10

  57. 親水性置換基導入に頼らない水溶性向上策：平面性・対称性の崩壊を目指した分子設計 Invited

    石川 稔

    田辺三菱製薬株式会社講演会　2011/08

  58. 新しい創薬戦略：タンパク質間相互作用の制御と親水性置換基導入に頼らない水溶性向上策 Invited

    石川 稔

    明治薬科大学 平成22年度第２回化学系若手研究者講話　2011/02

  59. 水溶性の優れた非ペプチド性インテグリンαvβ3/αIIbβ3デュアル拮抗薬の創製 Invited

    石川 稔

    日本薬学会第130年会 シンポジウム 有機化学を基盤とする実践的創薬　2010/03

  60. 新しい創薬手法の開発：タンパク質相互作用の制御と水溶性向上策 Invited

    石川 稔

    三井化学株式会社講演会　2010/02

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Industrial Property Rights 9

  1. インテグリンαvβ3拮抗剤としてのアミノピペリジン誘導体

    石川 稔, 村上 省一, 山本 幹夫, 窪田 大, 蜂須 貢, 片野 清昭, 味戸 慶一

    Property Type: Patent

  2. インテグリンαvβ3拮抗作用を有するα-ヒドロキシカルボン酸類新規化合物

    味戸 慶一, 八幡 直和, 石川 稔, 窪田 大, 村上 省一, 山本幹 夫, 藤島 和幸, 五味 修一, 大内 章吉

    Property Type: Patent

  3. インテグリンαvβ3拮抗作用を有するメタ置換安息香酸誘導体

    味戸 慶一, 石川 稔, 窪田 大, 村上 省一, 山本 幹夫, 八幡 直和, 藤島 和幸, 大山 真

    Property Type: Patent

  4. インテグリンαvβ3拮抗剤としての3-アミノピペリジン誘導体

    石川 稔, 窪田 大, 平岩 由紀子, 津島 正樹, 山本 幹夫, 八幡 直和, 黒田 千津子, 安部 允泰, 藤島 和幸, 村上 省一, 味戸 慶一

    Property Type: Patent

  5. インテグリンαvβ3拮抗物質を含んでなる再灌流障害治療剤

    藤島 和幸, 村上 省一, 山本 幹夫, 安部 允泰, 石川 稔, 大内 章吉, 味戸 慶一

    Property Type: Patent

  6. (4-オキソピペリジン-1-イル)安息香酸誘導体を用いたインテグリンαvβ3阻害剤の製造法

    石川 稔, 津島 正樹, 山田 拓, 窪田 大, 柳沢 由美子, 平岩 由起子, 大内 章吉, 安西 直道, 味戸 慶一

    Property Type: Patent

  7. ２位チエニルカルバペネム誘導体

    勢津 文仁, 塩川 宗二郎, 川野 愛美, 狩野 ゆうこ, 佐藤 晋也, 佐藤 悦子, 古内 剛, 石川 誠, 石川 稔, 金田 香織, 坂巻 儀晃, 馬場 信吉, 是澤 友和

    Property Type: Patent

  8. インテグリンαvβ3拮抗剤としてのフェニルピペラジン誘導体

    味戸 慶一, 村上 省一, 石川 稔, 山本 幹夫, 窪田 大, 五味 修一, 蜂須 貢, 片野 清昭

    Property Type: Patent

  9. 抗血小板凝集阻害作用を有するカルボン酸誘導体

    太田 和美, 磯村 泰子, 石川 稔, 奥平 典子, 鈴木 尚, 相澤 一雅, 片野 清昭

    Property Type: Patent

Show all Show first 5

Research Projects 13

  1. プロテオスタシスの異常を是正するネオユビキチンコードの解明

    大竹史明

    Offer Organization: 日本医療研究開発機構

    System: 革新的先端研究開発支援事業（AMED-CREST)

    2021 - 2026

  2. 疾患関連タンパク質の近接制御を基盤とした新しい創薬化学

    Offer Organization: Japan Society for the Promotion of Science

    System: Grants-in-Aid for Scientific Research Grant-in-Aid for Scientific Research (A)

    Category: Grant-in-Aid for Scientific Research (A)

    Institution: Tohoku University

    2022/04 - 2025/03

  3. Chemical protein knockdown technology and cell regulation

    Offer Organization: Japan Society for the Promotion of Science

    System: Grants-in-Aid for Scientific Research

    Category: Grant-in-Aid for Scientific Research on Innovative Areas (Research in a proposed research area)

    2018/06/29 - 2023/03/31

  4. 疾患関連タンパク質のタグ化を誘導する新創薬モダリティ Competitive

    石川 稔

    System: 科学研究費補助金（薬系化学および創薬科学関連）、基盤研究（B）

    2018 - 2022

  5. ケモテクノロジーが拓くユビキチンニューフロンティア Competitive

    内藤 幹彦

    System: 科学研究費補助金 新学術領域研究（研究領域提案型）（複合領域）

    2018 - 2022

  6. 細胞内アミロイドβのケミカルバイオロジー Competitive

    石川 稔

    System: 科学研究費補助金（創薬化学）、挑戦的研究（萌芽）

    2017 - 2018

  7. Polypharmacology based on dynamism of the target protein

    Hashimoto Yuichi, ISHIKAWA Minoru, FUJII Shinya, YACHIDE Tomomi

    Offer Organization: Japan Society for the Promotion of Science

    System: Grants-in-Aid for Scientific Research

    Category: Grant-in-Aid for Scientific Research (B)

    Institution: The University of Tokyo

    2014/04/01 - 2017/03/31

    More details Close

    One of novel strategy in the drug development would be "polypharmacology" (or "shot-gun approach"). It focuses on the robust biological functions and captures the actions of drug from wide and various aspects. Therefore, it stands in contrast to the conventional one-drug-one-target approach. Polypharmacology drug candidates involve bio-active compounds with multiple targets, i.e., multiple pathological/pathophysiological proteins and/or genes, in drug design. The limited success of one-molecular targeted drug discovery nowadays and clarification of robustness of biological system prompt us to develop polypharmacological strategy-based new drugs. Also, functional multiplicity in addition to the multiplicity of the target proteins, i.e., protein-knockdown activity and/or pharmacological chaperon activity, were also pursued in this study.

  8. 化合物が導くリバース翻訳後修飾プロテオミクス Competitive

    石川 稔

    System: 科学研究費補助金（創薬化学）、基盤研究（B）

    2013 - 2017

  9. Chemical control of protein dramatype

    HASHIMOTO Yuichi, ISHIKAWA Minoru, AOYAMA Hiroshi, SUGITA Kazuyuki, KOBAYASHI Hisayoshi, YACHIDE Tomomi, MATSUMOTO Yotaro, MISAWA Takashi

    Offer Organization: Japan Society for the Promotion of Science

    System: Grants-in-Aid for Scientific Research

    Category: Grant-in-Aid for Scientific Research (A)

    Institution: The University of Tokyo

    2010/04/01 - 2014/03/31

    More details Close

    Function, expression, stability and cellular localization of proteins are determined by their three dimensional structure. Therefore, control of the conformation of proteins results on regulation of their function/stability/localization. Abnormal conformation of specific proteins results in various incurable diseases. This research projects resulted in creation of: (1) various nuclear receptor ligands which control the function of the receptors by regulating their conformation, (2) small molecules (pharmacological chaperons) which correct abnormal trafficking of mutated proteins (ex. mutated rhodopsin which causes retinitis pigmentosa, NPC1 which caused Niemann-Pick type 1 disease), and (3) small molecules (SNIPERS) which induce degradation of target proteins in living cells.

  10. 多重薬理作用によるC型肝炎の治療戦略 Competitive

    石川 稔

    System: 科学研究費補助金（創薬化学）、挑戦的萌芽研究

    2013 - 2014

  11. タンパク質の特異的分解手法が切り拓く創薬化学の新カテゴリー Competitive

    石川 稔

    System: 科学研究費補助金（創薬化学）、若手研究（B）

    2011 - 2012

  12. Protein Knockdown Approach : Hybrid Small Molecules which Induce Proteasome Degradation of Target Proteins

    HASHIMOTO Yuichi, ISHIKAWA Minoru

    Offer Organization: Japan Society for the Promotion of Science

    System: Grants-in-Aid for Scientific Research

    Category: Grant-in-Aid for Challenging Exploratory Research

    Institution: The University of Tokyo

    2009 - 2011

    More details Close

    Protein knockdown can be achieved by the use of a small molecule that possesses affinity for both the target protein and ubiquitin ligase. As the ubiquitin ligase, we selected cIAP1 which specifically binds methylbestatin. Several hybrid molecules consisting of methylbestatin and a ligand for various proteins were designed and synthesized. These hybrid molecules induced selective decomposition of the target proteins.

  13. 多次元同時阻害作用を有する核内受容体機能阻害薬の創製研究 Competitive

    石川 稔

    System: 科学研究費補助金（創薬化学）、若手研究（B）

    2009 - 2010

Show all Show first 5

Teaching Experience 5

  1. 細胞機能工学　東京大学大学院農学系研究科

  2. 全学体験ゼミナール　東京大学教養学部

  3. 医薬化学II　東京大学薬学部

  4. 基礎薬科学特論II　東京大学大学院薬学系研究科

  5. ケミカルバイオロジー特論　東京大学大学院薬学系研究科

Media Coverage 2

  1. ミトコンドリア局在タンパク質の分解誘導技術mitoTPDを開発 新しい創薬方法論やミトコンドリア研究技術への展開に期待

    東北大学　https://www.tohoku.ac.jp/japanese/2024/08/press20240829-03-mitoTPD.html

    2024/08

    Type: Internet

  2. 特集：細胞の清掃工場を薬に 病原タンパク質を狙って分解

    日経サイエンス

    2022/09

    Type: Newspaper, magazine