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Hirose, Hisaaki

Institute for Chemical Research (ICR) Program-Specific Associate Professor

Hirose, Hisaaki
    Last Updated :2023/09/22

    Basic Information

    Professional Memberships

    • 日本分子生物学会
    • 日本生物物理学会
    • 日本薬学会
    • 日本生化学会

    Academic Degree

    • 修士(薬学)(京都大学)
    • 博士(薬学)(京都大学)

    Research History

    • From Feb. 2019, To Present
      Kyoto University, Institute for Chemical Research, 特定准教授
    • From Apr. 2015, To Jan. 2019
      The University of Tokyo, Graduate School of Science, 博士研究員
    • From Jun. 2012, To Mar. 2015
      Institute de Pharmacologie Moleculaire et Cellulaire, CNRS., Postdoctoral Fellow
    • From Apr. 2012, To May 2012
      Kyoto University, Institute for Chemical Research, 博士研究員


    researchmap URL

      Last Updated :2023/09/22


      Research Interests

      • 細胞内送達
      • イメージング
      • ペプチド化学
      • 細胞外小胞
      • エンドサイトーシス

      Research Areas

      • Nanotechnology/Materials, Molecular biochemistry
      • Life sciences, Pharmaceuticals - chemistry and drug development


      • Macropinoscope: Real-Time Simultaneous Tracking of pH and Cathepsin B Activity in Individual Macropinosomes
        Hisaaki Hirose; Eiji Nakata; Zhengxiao Zhang; Yuya Shibano; Masashi Maekawa; Takashi Morii; Shiroh Futaki
        Analytical Chemistry, 19 Jul. 2023, Peer-reviewed, Lead author
      • Structural Dissection of Epsin-1 N-Terminal Helical Peptide: The Role of Hydrophobic Residues in Modulating Membrane Curvature.
        Motoki Nishimura; Yoshimasa Kawaguchi; Kakeru Kuroki; Yuna Nakagawa; Toshihiro Masuda; Takayuki Sakai; Kenichi Kawano; Hisaaki Hirose; Miki Imanishi; Tomoka Takatani-Nakase; Sergii Afonin; Anne S Ulrich; Shiroh Futaki
        Chemistry (Weinheim an der Bergstrasse, Germany), 06 Mar. 2023
      • A noncanonical endocytic pathway is involved in the internalization of 3 μm polystyrene beads into HeLa cells
        Hisaaki Hirose; Masashi Maekawa; Hiroki Ida; Masashi Kuriyama; Yasufumi Takahashi; Shiroh Futaki
        Biomaterials Science, Dec. 2022, Peer-reviewed, Lead author, Corresponding author
      • Quantitative Analysis of Extracellular Vesicle Uptake and Fusion with Recipient Cells.
        Hisaaki Hirose; Yusuke Hirai; Michihito Sasaki; Hirofumi Sawa; Shiroh Futaki
        Bioconjugate chemistry, 04 Oct. 2022, Peer-reviewed, Lead author, Corresponding author
      • Split luciferase-based estimation of cytosolic cargo concentration delivered intracellularly via attenuated cationic amphiphilic lytic peptides
        Syusuke Okano; Yoshimasa Kawaguchi; Kenichi Kawano; Hisaaki Hirose; Miki Imanishi; Shiroh Futaki
        Bioorganic & Medicinal Chemistry Letters, Jul. 2022
      • The formation of particle-like structure on cell membranes accompanies direct influx of arginine-rich peptides into cells
        H. Hirose; T. Takeuchi; I. Nakase; S. Futaki
        BIOPOLYMERS, 2011, Peer-reviewed
      • Evaluation of effective membrane penetration by FHV peptide
        Ikuhiko Nakase; Hisaaki Hirose; Shiroh Futaki
      • Peptide-assisted intracellular delivery of biomacromolecules
        Futaki, S.; Arafiles, J.V.V.; Hirose, H.
        Chemistry Letters, 2020, Last author
      • Stearylated Macropinocytosis-Inducing Peptides Facilitating the Cellular Uptake of Small Extracellular Vesicles
        Yuna Nakagawa; Jan Vincent V. Arafiles; Yoshimasa Kawaguchi; Ikuhiko Nakase; Hisaaki Hirose; Shiroh Futaki
        Bioconjugate Chemistry, 04 May 2022, Peer-reviewed
      • Piezo1 activation using Yoda1 inhibits macropinocytosis in A431 human epidermoid carcinoma cells
        Masashi Kuriyama; Hisaaki Hirose; Toshihiro Masuda; Masachika Shudou; Jan Vincent Arafiles; Miki Imanishi; Masashi Maekawa; Yuji Hara; Shiroh Futaki
        Scientific Reports, Apr. 2022, Peer-reviewed, Lead author, Corresponding author
      • Grafting Hydrophobic Amino Acids Critical for Inhibition of Protein–Protein Interactions on a Cell-Penetrating Peptide Scaffold
        Yuki Nagano; Jan Vincent V. Arafiles; Keiko Kuwata; Yoshimasa Kawaguchi; Miki Imanishi; Hisaaki Hirose; Shiroh Futaki
        Molecular Pharmaceutics, 07 Feb. 2022, Peer-reviewed
      • Cytosolic protein delivery using pH-responsive, charge-reversible lipid nanoparticles.
        Yusuke Hirai; Hisaaki Hirose; Miki Imanishi; Tomohiro Asai; Shiroh Futaki
        Scientific reports, 06 Oct. 2021, Peer-reviewed
      • Liquid droplet formation and facile cytosolic translocation of IgG in the presence of attenuated cationic amphiphilic lytic peptides.
        Takahiro Iwata; Hisaaki Hirose; Kentarou Sakamoto; Yusuke Hirai; Jan Vincent V Arafiles; Misao Akishiba; Miki Imanishi; Shiroh Futaki
        Angewandte Chemie (International ed. in English), 11 Jun. 2021, Peer-reviewed
      • A facile combinatorial approach to construct a ratiometric fluorescent sensor: application for the real-time sensing of cellular pH changes.
        Eiji Nakata; Hisaaki Hirose; Khongorzul Gerelbaatar; Jan Vincent V Arafiles; Zhengxiao Zhang; Shiroh Futaki; Takashi Morii
        Chemical science, 08 May 2021, Peer-reviewed
      • Nanoscale Visualization of Morphological Alteration of Live-Cell Membranes by the Interaction with Oligoarginine Cell-Penetrating Peptides.
        Hiroki Ida; Yasufumi Takahashi; Akichika Kumatani; Hitoshi Shiku; Tomo Murayama; Hisaaki Hirose; Shiroh Futaki; Tomokazu Matsue
        Analytical chemistry, 06 Apr. 2021, Peer-reviewed
      • Discovery of a Macropinocytosis-Inducing Peptide Potentiated by Medium-Mediated Intramolecular Disulfide Formation.
        Jan Vincent V Arafiles; Hisaaki Hirose; Yusuke Hirai; Masashi Kuriyama; Maxwell Mamfe Sakyiamah; Wataru Nomura; Kazuhiro Sonomura; Miki Imanishi; Akira Otaka; Hirokazu Tamamura; Shiroh Futaki
        Angewandte Chemie (International ed. in English), 24 Feb. 2021, Peer-reviewed
      • Effect of Surface Modifications on Cellular Uptake of Gold Nanorods in Human Primary Cells and Established Cell Lines.
        Yuxiang Xiao; Wei Xu; Yoshihiro Komohara; Yukio Fujiwara; Hisaaki Hirose; Shiroh Futaki; Takuro Niidome
        ACS omega, 22 Dec. 2020, Peer-reviewed
      • Improved cytosolic delivery of macromolecules through dimerization of attenuated lytic peptides.
        Yohei Nomura; Kentarou Sakamoto; Misao Akishiba; Takahiro Iwata; Hisaaki Hirose; Shiroh Futaki
        Bioorganic & medicinal chemistry letters, 01 Sep. 2020, Peer-reviewed
      • An Artificial Amphiphilic Peptide Promotes Endocytic Uptake by Inducing Membrane Curvature
        Toshihiro Masuda; Hisaaki Hirose; Kentarou Baba; Astrid Walrant; Sandrine Sagan; Naoyuki Inagaki; Toyoshi Fujimoto; Shiroh Futaki
        Bioconjugate Chemistry, 17 Jun. 2020, Peer-reviewed
      • Enhancing the activity of membrane remodeling epsin-peptide by trimerization
        Hsu, W.-Y.; Masuda, T.; Afonin, S.; Sakai, T.; Arafiles, J.V.V.; Kawano, K.; Hirose, H.; Imanishi, M.; Ulrich, A.S.; Futaki, S.
        Bioorganic and Medicinal Chemistry Letters, 2020, Peer-reviewed
      • Conversion of cationic amphiphilic lytic peptides to cell-penetration peptides
        Yu, H.-H.; Sakamoto, K.; Akishiba, M.; Tamemoto, N.; Hirose, H.; Nakase, I.; Imanishi, M.; Madani, F.; Gräslund, A.; Futaki, S.
        Peptide Science, 2020, Peer-reviewed
      • Stimulating Macropinocytosis for Intracellular Nucleic Acid and Protein Delivery: A Combined Strategy with Membrane-Lytic Peptides to Facilitate Endosomal Escape
        Arafiles, J.V.V.; Hirose, H.; Akishiba, M.; Tsuji, S.; Imanishi, M.; Futaki, S.
        Bioconjugate Chemistry, 2020, Peer-reviewed
      • A Case Study on the Keap1 Interaction with Peptide Sequence Epitopes Selected by the Peptidomic mRNA Display
        Hirose, H.; Hideshima, T.; Katoh, T.; Suga, H.
        ChemBioChem, 2019, Peer-reviewed, Lead author
      • Oligoarginine-Bearing Tandem Repeat Penetration-Accelerating Sequence Delivers Protein to Cytosol via Caveolae-Mediated Endocytosis
        Okuda, A.; Tahara, S.; Hirose, H.; Takeuchi, T.; Nakase, I.; Ono, A.; Takehashi, M.; Tanaka, S.; Futaki, S.
        Biomacromolecules, 2019, Peer-reviewed
      • In vitro expression of genetically encoded non-standard peptides consisting of exotic amino acid building blocks
        Hirose, H.; Tsiamantas, C.; Katoh, T.; Suga, H.
        Current Opinion in Biotechnology, 2019, Peer-reviewed, Lead author
      • Targeting surface voids to counter membrane disorders in lipointoxication-related diseases
        Ferru-Clément, R.; Spanova, M.; Dhayal, S.; Morgan, N.G.; Hélye, R.; Becq, F.; Hirose, H.; Antonny, B.; Vamparys, L.; Fuchs, P.F.J.; Ferreira, T.
        Journal of Cell Science, 2016, Peer-reviewed
      • Effect of amino acid substitution in the hydrophobic face of amphiphilic peptides on membrane curvature and perturbation: N-terminal helix derived from adenovirus internal protein VI as a model
        Murayama, T.; Pujals, S.; Hirose, H.; Nakase, I.; Futaki, S.
        Biopolymers, 2016, Peer-reviewed
      • A sub-nanometre view of how membrane curvature and composition modulate lipid packing and protein recruitment
        Vanni, S.; Hirose, H.; Barelli, H.; Antonny, B.; Gautier, R.
        Nature Communications, 2014, Peer-reviewed, Lead author
      • Dynamic amphiphile libraries to screen for the "fragrant" delivery of siRNA into HeLa cells and human primary fibroblasts
        Gehin, C.; Montenegro, J.; Bang, E.-K.; Cajaraville, A.; Takayama, S.; Hirose, H.; Futaki, S.; Matile, S.; Riezman, H.
        Journal of the American Chemical Society, 2013, Peer-reviewed
      • Modeling the endosomal escape of cell-penetrating peptides using a transmembrane pH gradient
        Madani, F.; Abdo, R.; Lindberg, S.; Hirose, H.; Futaki, S.; Langel, Ü.; Gräslund, A.
        Biochimica et Biophysica Acta - Biomembranes, 2013, Peer-reviewed
      • Arginine-rich peptides: Methods of translocation through biological membranes
        Futaki, S.; Hirose, H.; Nakase, I.
        Current Pharmaceutical Design, 2013, Peer-reviewed
      • Curvature engineering: Positive membrane curvature induced by epsin N-terminal peptide boosts internalization of octaarginine
        Pujals, S.; Miyamae, H.; Afonin, S.; Murayama, T.; Hirose, H.; Nakase, I.; Taniuchi, K.; Umeda, M.; Sakamoto, K.; Ulrich, A.S.; Futaki, S.
        ACS Chemical Biology, 2013, Peer-reviewed
      • Effect of the attachment of a penetration accelerating sequence and the influence of hydrophobicity on octaarginine-mediated intracellular delivery
        Takayama, K.; Hirose, H.; Tanaka, G.; Pujals, S.; Katayama, S.; Nakase, I.; Futaki, S.
        Molecular Pharmaceutics, 2012, Peer-reviewed
      • Transient focal membrane deformation induced by arginine-rich peptides leads to their direct penetration into cells
        Hirose, H.; Takeuchi, T.; Osakada, H.; Pujals, S.; Katayama, S.; Nakase, I.; Kobayashi, S.; Haraguchi, T.; Futaki, S.
        Molecular Therapy, 2012, Peer-reviewed, Lead author
      • Transformation of an antimicrobial peptide into a plasma membrane-permeable, mitochondria-targeted peptide via the substitution of lysine with arginine
        Nakase, I.; Okumura, S.; Katayama, S.; Hirose, H.; Pujals, S.; Yamaguchi, H.; Arakawa, S.; Shimizu, S.; Futaki, S.
        Chemical Communications, 2012, Peer-reviewed
      • Acylation of octaarginine: Implication to the use of intracellular delivery vectors
        Katayama, S.; Hirose, H.; Takayama, K.; Nakase, I.; Futaki, S.
        Journal of Controlled Release, 2011, Peer-reviewed
      • Expressed protein ligation for the preparation of fusion proteins with cell penetrating peptides for endotoxin removal and intracellular delivery
        Yu, H.-H.; Nakase, I.; Pujals, S.; Hirose, H.; Tanaka, G.; Katayama, S.; Imanishi, M.; Futaki, S.
        Biochimica et Biophysica Acta - Biomembranes, 2010, Peer-reviewed
      • Elucidating cell-penetrating peptide mechanisms of action for membrane interaction, cellular uptake, and translocation utilizing the hydrophobic counter-anion pyrenebutyrate
        Guterstam, P.; Madani, F.; Hirose, H.; Takeuchi, T.; Futaki, S.; EL Andaloussi, S.; Gräslund, A.; Langel, Ü.
        Biochimica et Biophysica Acta - Biomembranes, 2009, Peer-reviewed
      • Cell-surface accumulation of flock house virus-derived peptide leads to efficient internalization via macropinocytosis
        Nakase, I.; Hirose, H.; Tanaka, G.; Tadokoro, A.; Kobayashi, S.; Takeuchi, T.; Futaki, S.
        Molecular Therapy, 2009, Peer-reviewed


      • 高分子細胞内送達ペプチドの設計と送達機序
        日本薬剤学会第38年会, 18 May 2023, Invited
      • 細胞外物質の細胞内移行様式
        広瀬 久昭
        慶應薬学先端実学(サイヤンス)セミナー, 18 Nov. 2022, Invited