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

ID,URL

• J-Global ID

  201901020086443879

researchmap URL

• https://researchmap.jp/hiroseh

Research

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

Papers

• 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

  YAKUGAKU ZASSHI-JOURNAL OF THE PHARMACEUTICAL SOCIETY OF JAPAN, 2008, Peer-reviewed

  
• 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

  

Presentations

• 高分子細胞内送達ペプチドの設計と送達機序

  広瀬久昭

  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