Updated on 2026/03/05

写真a

 
MUGURUMA KYOHEI
 
Organization
Institute of Integrated Research Laboratory for Chemistry and Life Science Assistant Professor
Title
Assistant Professor
External link

Degree

  • 博士（薬学） ( 2018.3   東京薬科大学 )

Research Areas

  • Life Science / Pharmaceutical chemistry and drug development sciences

Education

  • Tokyo University of Pharmacy and Life Sciences

    2014.4 - 2018.3

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  • Tokyo University of Pharmacy and Life Science

    2008.4 - 2014.3

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Research History

  • Institute of Science Tokyo   Institute of Integrated Research, Laboratory for Chemistry and Life Science   Assistant Professor

    2024.10

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  • Innovation Center of NanoMedicine

    2024.4

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  • Tokyo Institute of Technology   Institute of Innovative Research   Assistant Professor

    2024.3 - 2024.9

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  • RIKEN   Special Postdoctoral Researcher

    2022.4 - 2024.2

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  • RIKEN

    2020.6 - 2022.3

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  • Tokyo Institute of Technology   School of Materials and Chemical Technology   postdoctoral fellow

    2020.4 - 2022.3

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  • 日本学術振興会   特別研究員（PD）

    2019.4 - 2022.3

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  • 理化学研究所   訪問研究員

    2019.4 - 2020.3

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  • Tokyo University of Pharmacy and Life Science   School of Pharmacy

    2018.4 - 2019.3

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  • 日本学術振興会   特別研究員（DC1）

    2015.4 - 2018.3

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Professional Memberships

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Committee Memberships

  •   ファルマシアトピックス小委員会 委員  

    2024.4   

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Papers

  • Tumor-targeted adeno associated virus-loaded complexes comprising tannic acid and phenylboronic acid-polymers for orthotopic glioblastoma therapy. International journal

    Nozomi Matsudaira, Yuto Honda, Hiroaki Kinoh, Xueying Liu, Shuhei Nagao, Shoko Matsutomo-Nitta, Guo Haochen, Hiromi Hayashita-Kinoh, Miho Aizawa, Kyohei Muguruma, Yutaka Miura, Atushi Shishido, Takashi Okada, Nobuhiro Nishiyama

    Journal of controlled release : official journal of the Controlled Release Society   389   114477 - 114477   2026.1

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    Language：English   Publishing type：Research paper (scientific journal)  

    Adeno-associated virus (AAV) vectors have emerged as one of the most promising viral vectors for gene therapy due to their capacity for long-term transgene expression, strong safety profile and low pathogenicity, and have been applied to the treatment of refractory cancer such as glioblastoma (GBM). However, AAV-mediated cancer gene therapy faces significant obstacles, including poor tumor targeting and neutralization by pre-existing antibodies (Abs). In this study, we developed a novel GBM-targeted AAV delivery platform, the cyclic RGD-functionalized ternary complex (cRGD-ternary complex). This complex is constructed through the self-assembly of AAV, tannic acid, and cRGD-conjugated phenylboronic acid polymers. cRGD serves as a ligand targeting αvβ3/αvβ5 integrins, which are highly expressed on GBM cells. In vitro, the cRGD-ternary complex effectively evaded neutralizing Abs due to its polymer shell and maintained high gene transduction efficiency. In an orthotopic GBM mouse model, systemic administration of cRGD-ternary complex significantly enhanced gene transduction in tumors and achieved substantial tumor suppression over 24 days. Furthermore, the cRGD-ternary complex showed therapeutic efficacy comparable to AAV alone at three-fold higher dose, with negligible hepatotoxicity. This platform successfully integrates active tumor targeting, immune evasion, and efficient gene transduction, overcoming critical limitations of AAV and showing significant potential for GBM gene therapy.

    DOI： 10.1016/j.jconrel.2025.114477

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  • Structure–Activity Relationship Study of Affinity Peptides for the Fc Site of Human Immunoglobulin G Reviewed

    Kyohei Muguruma, Akane Fukuda, Hayate Shida, Rento Osawa, Soichiro Harigaya, Mayu Ito, Nana Sato, Aya Kuroda, Atsuki Kobayashi, Satoshi Kishimoto, Akihiro Taguchi, Kentaro Takayama, Atsuhiko Taniguchi, Yuji Ito, Yoshio Hayashi

    Chemical and Pharmaceutical Bulletin   73 ( 12 )   1132 - 1138   2025.12

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    Authorship：Lead author,　Corresponding author   Publishing type：Research paper (scientific journal)   Publisher：Pharmaceutical Society of Japan  

    DOI： 10.1248/cpb.c25-00637

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  • Polyzwitterion-Based pH-Responsive Shell of Polymeric Micelle: Evaluation of Physicochemical Properties and In Vivo Functionalities

    Wanphiwat Chintrakulchai, Aziz Awaad, Motoaki Kobayashi, Koki Yanagida, Camille Lindley Tiu, Masahiro Toyoda, Kyohei Muguruma, Yuto Honda, Hiroyasu Takemoto, Nobuhiro Nishiyama, Yutaka Miura

    Biomacromolecules   2025.12

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    Publishing type：Research paper (scientific journal)  

    DOI： 10.1021/acs.biomac.5c01343

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  • Metal-phenolic network-based polymeric nanocarriers facilitating antibody cytoplasmic delivery and anti-tumor effects to orthotopic breast tumors. International journal

    Yuto Honda, Haruna Haraguchi, Takeru Tsuda, Rui Ko, Kyohei Muguruma, Haochen Guo, Takahiro Nomoto, Yutaka Miura, Nobuhiro Nishiyama

    Journal of controlled release : official journal of the Controlled Release Society   384   113929 - 113929   2025.8

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    Language：English   Publishing type：Research paper (scientific journal)  

    Intracellular delivery of antibodies holds great promise for targeting cytosolic antigens involved in various diseases, particularly cancer because many key signal-inducing antigens are localized intracellularly. However, the clinical application of intracellular antibodies is hindered by their poor cellular uptake and inefficient endosomal escape owing to their large molecular weight, hydrophilicity, and overall negative charge. To address these challenges, we developed a metal-phenolic network (MPN)-based polymeric nanocarrier for cytosolic antibody delivery. This carrier was composed of a polyphenol-conjugated polymer and metal ions. Upon simple mixing with antibodies, polyphenol-conjugated polymers and metal ions form polymeric MPN complex-encapsulating antibodies with a core-shell structure. The complex, with a diameter of approximately 30 nm and a relatively neutral charge, demonstrated excellent pharmacokinetics and tumor accumulation following intravenous administration. Within tumor cells, the polymeric MPN complex facilitated endosomal escape through a buffering effect triggered by coordination bond dissociation of MPN in the acidic endosomal environment; simultaneously, the antibodies were released from the polymeric MPN complex, leading to binding to the antigen in the cytoplasm. The polymeric MPN complex enhanced the therapeutic effect of cytoplasmic antigen-binding antibodies against orthotopic breast tumors in mice. This study demonstrated the potential of MPN-based polymeric nanocarriers without cationic molecules as a platform for intracellular antibody delivery, enabling systemic administration and cytosolic release in tumors, thus expanding the therapeutic landscape of antibody-based treatments.

    DOI： 10.1016/j.jconrel.2025.113929

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  • Catalytic Activity Alternation of an Artificial Metalloenzyme by Switchable Binding to the Proteins

    Kyohei Muguruma, Kyosuke Imai, Katsunori Tanaka

    ChemCatChem   17 ( 13 )   2025.4

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    Authorship：Lead author,　Corresponding author   Publishing type：Research paper (scientific journal)   Publisher：Wiley  

    Abstract

    An artificial metalloenzyme (ArM) utilizing a human serum albumin (HSA) scaffold exhibits remarkable catalytic stability due to the presence of a catalytic center within the deep hydrophobic pocket, demonstrating potential in vivo applicability for disease treatment via a prodrug activation strategy. Additionally, the development of latent catalysts is an important consideration for catalyst therapy to suppress the undesired activation of prodrugs. In this study, we developed a catalytic activity control system using a bispecific artificial metallopeptide, composed of a CpRu catalyst, an Fc‐binding peptide, and an albumin‐binding ligand. This metallopeptide individually interacted with both HSA and IgG, exhibiting catalytic activity change depending on the binding protein. The catalytic activity was enhanced when the metallopeptide was displaced from the pocket by interaction with IgG compared to the ArM formed with HSA, whereas no activity change was observed in the traditional ArM lacking the Fc‐binding peptide unit. This is the first report of the activity switching in an ArM by changing the binding place of the metal catalyst. We anticipated that this system could lead to further development of the concept for in vivo synthesis of drug molecules, termed “therapeutic in vivo synthetic chemistry” realizing the disease therapy without side effects of drugs.

    DOI： 10.1002/cctc.202500154

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  • Preclinical evaluation of the therapeutic potential of 211-At-rabiolabeled 2,6-diisoproplyphenyl azide in mouse models for human lung cancer treatment Invited Reviewed

    Y. Ode, A. R. Pradipta, P. Ahmadi, A. Ishiwata, A. Nakamura, Y. Egawa, Y. Kusakari, K. Muguruma, Y. Wang, X. Yin, N. Sato, H. Haba, K. Tanaka

    RIKEN Accelerator Progress Report   57   S44   2024.12

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    DOI： 10.34448/RIKEN.APR.57-024

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  • In vivo synthetic anticancer approach by resourcing mouse blood albumin as a biocompatible artificial metalloenzyme International journal

    Kyosuke Imai, Kyohei Muguruma, Akiko Nakamura, Yuriko Kusakari, Tsung-Che Chang, Ambara R. Pradipta, Katsunori Tanaka

    Angewandte Chemie International Edition   63 ( 43 )   e202411225   2024.7

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    Authorship：Corresponding author   Language：English   Publishing type：Research paper (scientific journal)   Publisher：Wiley  

    Methods for producing drugs directly at the cancer site, particularly using bioorthogonal metal catalysts, are being explored to mitigate the side effects of therapy. Albumin‐based artificial metalloenzymes (ArMs) catalyze reactions in living mice while protecting the catalyst in the hydrophobic pocket. Here, we describe the in situ preparation and application of biocompatible tumor‐targeting ArMs using circulating albumin, which is abundant in the bloodstream. The ArM was formed using blood albumin through the intravenous injection of ruthenium conjugated with an albumin‐binding ligand; the tumor‐targeting unit was conjugated to the ArM using its catalytic activity, and the ArM was transported to the cancer site. The delivered ArM catalyzed a second tagging reaction of the proapoptotic peptide on the cancer surface, successfully suppressing cancer proliferation. This approach, which efficiently leveraged the persisting reactivity twice in vivo, holds promise for future in vivo metal‐catalyzed drug synthesis utilizing endogenous albumin.

    DOI： 10.1002/anie.202411225

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  • Structure Derivatization of IgG-Binding Peptides and Analysis of Their Secondary Structure by Circular Dichroism Spectroscopy.

    Kyohei Muguruma, Akane Fukuda, Hayate Shida, Akihiro Taguchi, Kentaro Takayama, Atsuhiko Taniguchi, Yuji Ito, Yoshio Hayashi

    Chemical & pharmaceutical bulletin   72 ( 9 )   831 - 837   2024

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    Authorship：Lead author,　Corresponding author   Language：English   Publishing type：Research paper (scientific journal)  

    Mid-sized cyclic peptides are a promising modality for modern drug discovery. Their larger interaction area coupled with an appropriate secondary structure is more suitable than small molecules for binding to the target protein. In this study, we conducted a structure derivatization of an immunoglobulin G (IgG)-binding peptide (15-IgBP), a β-hairpin-like cyclic peptide with a twisted β-strand and assessed the effect of the secondary structure on IgG-binding activity using circular dichroism (CD) spectra analysis. As a result, derivatization at the Ala5 and Gly9 positions affected the secondary structure of 15-IgBP, in particular the appearance of a small positive peak in the 220-240 nm region characteristic of 15-IgBP in the CD spectrum. Maintaining this peak at a moderate level may be important for the expression of IgG binding activity. We found the small methyl group at Ala5 to be crucial for retaining the preferred secondary structure; we also found Gly9 could be replaced by D-amino acids. By integrating these findings with previous results of the structure-activity relationship, we obtained four potent affinity peptides for IgG binding (Kd = 4.24-5.85 nM). Furthermore, we found the Gly9 position can be substituted for D-Lys. This is a new potential site for attaching functional units for conjugation with IgG for the preparation of homogeneous antibody-drug conjugates.

    DOI： 10.1248/cpb.c24-00430

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  • X-Ray Conformation and Structure-Activity Relationships of MA026, a Reversible Tight Junction Opener. International journal

    Minagi Mukaiyama, Chihiro Uchiyama, Akane Fukuda, Yoshiki Nakazawa, Yuka Kuramochi, Yudai Shibata, Sho Konno, Kyohei Muguruma, Naohiro Matsugaki, Tomo Asari, Kazuyoshi Ogawa, Akihiro Taguchi, Kentaro Takayama, Atsuhiko Taniguchi, Yoko Nagumo, Toshiya Senda, Yoshio Hayashi, Takeo Usui

    Journal of medicinal chemistry   66 ( 13 )   8717 - 8724   2023.6

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    Language：English   Publishing type：Research paper (scientific journal)  

    MA026, a cyclic lipodepsipeptide, opens the tight junction (TJ) probably via binding to claudin-1. We reported that (1) TJ-opening activity is dependent on the amino acid sequence order at Glu10-Leu11; (2) an epimer at the C3 position of the N-terminal acyl tail decreased the TJ-opening activity; and (3) the epimers D-Leu1/L-Gln6 and L-Leu1/D-Gln6 showed more potent TJ-opening activity than natural MA026, although no systematic structure-activity relationship (SAR) study was conducted. Here, we report the three-dimensional structure and systematic SAR study of MA026. X-Ray crystallography and circular dichroism analysis of MA026 revealed that MA026 forms a left-handed α-helical structure, and hydrophobic amino acids are clustered on one side. Furthermore, the SAR results clearly showed that the hydrophobic region of MA026 is important for TJ-opening activity. These results suggest that MA026 interacts with claudin-1 via the hydrophobic cluster region and provide novel structural insights toward the development of a TJ opener targeting claudin-1.

    DOI： 10.1021/acs.jmedchem.3c00365

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  • Therapeutic efficacy of 211At-radiolabeled 2,6-diisopropylphenyl azide in mouse models of human lung cancer Reviewed International journal

    Yudai Ode, Ambara R. Pradipta, Peni Ahmadi, Akihiro Ishiwata, Akiko Nakamura, Yasuko Egawa, Yuriko Kusakari, Kyohei Muguruma, Yang Wang, Xiaojie Yin, Nozomi Sato, Hiromitsu Haba, Katsunori Tanaka

    Chemical Science   14 ( 30 )   8054 - 8060   2023

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    Language：English   Publishing type：Research paper (scientific journal)  

    Targeted α-particle therapy (TAT) is an attractive alternative to conventional therapy for cancer treatment. Among the available radionuclides considered for TAT, astatine-211 (211At) attached to a cancer-targeting molecule appears very promising. Previously, we demonstrated that aryl azide derivatives could react selectively with the endogenous acrolein generated by cancer cells to give a diazo compound, which subsequently forms a covalent bond with the organelle of cancer cells in vivo. Herein, we synthesized 211At-radiolabeled 2,6-diisopropylphenyl azide (ADIPA), an α-emitting molecule that can selectively target the acrolein of cancer cells, and investigated its antitumor effect. Our results demonstrate that a single intratumor or intravenous administration of this simple α-emitting molecule to the A549 (human lung cancer) cell-bearing xenograft mouse model, at a low dose (70 kBq), could suppress tumor growth without inducing adverse effects. Furthermore, because acrolein is generally overproduced by most cancer cells, we believe ADIPA is a simple TAT compound that deserves further investigation for application in animal models and humans with various cancer types and stages.

    DOI： 10.1039/D3SC02513F

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  • Evaluation of acute toxicity of cancer-targeting albumin-based artificial metalloenzymes Reviewed

    Tsung-Che Chang, Igor Nasibullin, Kyohei Muguruma, Yuriko Kusakari, Taiji Shimoda, Katsunori Tanaka

    Bioorganic & Medicinal Chemistry   73   117005 - 117010   2022.11

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    Language：English   Publishing type：Research paper (scientific journal)   Publisher：Elsevier BV  

    DOI： 10.1016/j.bmc.2022.117005

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  • In vivo metal-catalyzed SeCT therapy by a proapoptotic peptide

    Peni Ahmadi, Kyohei Muguruma, Tsung-Che Chang, Satoru Tamura, Kazuki Tsubokura, Yasuko Egawa, Takehiro Suzuki, Naoshi Dohmae, Yoichi Nakao, Katsunori Tanaka

    Chemical Science   12 ( 37 )   12266 - 12273   2021.9

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    Authorship：Lead author   Publishing type：Research paper (scientific journal)   Publisher：Royal Society of Chemistry (RSC)  

    The combination of a proapoptotic peptide with covalent tagging and a carrier-Ru-complex inhibited tumor growth in mice after a single injection.

    DOI： 10.1039/d1sc01784e

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  • Structural Revision of Natural Cyclic Depsipeptide MA026 Established by Total Synthesis and Biosynthetic Gene Cluster Analysis International journal

    Chihiro Uchiyama, Akane Fukuda, Minagi Mukaiyama, Yoshiki Nakazawa, Yuka Kuramochi, Kyohei Muguruma, Mitsue Arimoto, Akihiro Ninomiya, Koichiro Kako, Yohei Katsuyama, Sho Konno, Akihiro Taguchi, Kentaro Takayama, Atsuhiko Taniguchi, Yoko Nagumo, Takeo Usui, Yoshio Hayashi

    Angewandte Chemie International Edition   60 ( 16 )   8792 - 8797   2021.4

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    Language：English   Publishing type：Research paper (scientific journal)   Publisher：Wiley  

    A revised structure of natural 14-mer cyclic depsipeptide MA026, isolated from Pseudomonas sp. RtlB026 in 2002 was established by physicochemical analysis with HPLC, MS/MS, and NMR and confirmed by total solid-phase synthesis. The revised structure differs from that previously reported in that two amino acid residues, assigned in error, have been replaced. Synthesized MA026 with the revised structure showed a tight junction (TJ) opening activity like that of the natural one in a cell-based TJ opening assay. Bioinformatic analysis of the putative MA026 biosynthetic gene cluster (BGC) of RtIB026 demonstrated that the stereochemistry of each amino acid residue in the revised structure can be reasonably explained. Phylogenetic analysis with xantholysin BGC indicates an exceptionally high homology (ca. 90 %) between xantholysin and MA026. The TJ opening activity of MA026 when binding to claudin-1 is a key to new avenues for transdermal administration of large hydrophilic biologics.

    DOI： 10.1002/anie.202015193

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    Other Link： https://onlinelibrary.wiley.com/doi/full-xml/10.1002/anie.202015193

  • Targeted 1,3-dipolar cycloaddition with acrolein for cancer prodrug activation.

    Pradipta AR, Ahmadi P, Terashima K, Muguruma K, Fujii M, Ichino T, Maeda S, Tanaka K

    Chemical science   12 ( 15 )   5438 - 5449   2021.4

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    Publishing type：Research paper (scientific journal)   Publisher：Royal Society of Chemistry (RSC)  

    <p>Prodrug activation strategy by utilizing the reaction between aryl azide and endogenous acrolein that is generally overproduced by cancer cells.</p>

    DOI： 10.1039/d0sc06083f

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  • Development of a High-Affinity Antibody-Binding Peptide for Site-Specific Modification.

    Muguruma K, Osawa R, Fukuda A, Ishikawa N, Fujita K, Taguchi A, Takayama K, Taniguchi A, Ito Y, Hayashi Y

    ChemMedChem   16 ( 11 )   1814 - 1821   2021.3

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    Authorship：Lead author   Publishing type：Research paper (scientific journal)   Publisher：Wiley  

    DOI： 10.1002/cmdc.202000977

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    Other Link： https://onlinelibrary.wiley.com/doi/full-xml/10.1002/cmdc.202000977

  • “On‐Resin” Disulfide Peptide Synthesis with Methyl 3‐Nitro‐2‐pyridinesulfenate

    Kiyotaka Kobayashi, Akihiro Taguchi, Yan Cui, Hayate Shida, Kyohei Muguruma, Kentaro Takayama, Atsuhiko Taniguchi, Yoshio Hayashi

    European Journal of Organic Chemistry   2021 ( 6 )   956 - 963   2021.2

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    Publishing type：Research paper (scientific journal)   Publisher：Wiley  

    DOI： 10.1002/ejoc.202001517

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    Other Link： https://onlinelibrary.wiley.com/doi/full-xml/10.1002/ejoc.202001517

  • Synthesis and biological evaluation of a monocyclic Fc-binding antibody-recruiting molecule for cancer immunotherapy Reviewed International journal

    Koichi Sasaki, Kyohei Muguruma, Rento Osawa, Akane Fukuda, Atsuhiko Taniguchi, Akihiro Kishimura, Yoshio Hayashi, Takeshi Mori, Yoshiki Katayama

    RSC Medicinal Chemistry   12 ( 3 )   406 - 409   2021

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    Language：English   Publishing type：Research paper (scientific journal)   Publisher：Royal Society of Chemistry (RSC)  

    <p>A monocyclic Fc-binding peptide “15-Lys8Leu” enables simple preparation of a Fc-binding antibody-recruiting molecule (Fc-ARM), which induces potent cytotoxicity against folate receptor positive cancer cells <italic>via</italic> NK cell-mediated immune response.</p>

    DOI： 10.1039/d0md00337a

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  • Disease-associated acrolein: A possible diagnostic and therapeutic substrate for in vivo synthetic chemistry. International journal

    Kyohei Muguruma, Ambara R Pradipta, Yudai Ode, Kazuki Terashima, Hiroyuki Michiba, Motoko Fujii, Katsunori Tanaka

    Bioorganic & medicinal chemistry   28 ( 24 )   115831 - 115831   2020.12

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    Acrolein, a highly reactive α,β-unsaturated aldehyde, is a compound to which humans are exposed in many different situations and often causes various human diseases. This paper summarizes the reports over the past twenty-five years regarding disease-associated acrolein detected in clinical patients and the role acrolein plays in various diseases. In several diseases, it was found that the increased acrolein acts as a pathogenetic factor. Thus, we propose the utility of over-produced acrolein as a substrate for a promising therapeutic or diagnostic method applicable to a wide range of diseases based on an in vivo synthetic chemistry strategy.

    DOI： 10.1016/j.bmc.2020.115831

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  • Basic research in antibody-dependent drug delivery technology based on IgG-binding peptide

    Yoshio Hayashi, Kyohei Muguruma

    Drug Delivery System   35 ( 3 )   191 - 199   2020

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    Language：Japanese   Publishing type：Research paper (scientific journal)   Publisher：Japan Society of Drug Delivery System  

    DOI： 10.2745/dds.35.191

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  • Synthesis and structure-activity relationship studies of IgG-binding peptides focused on the C-terminal histidine residue. Reviewed International journal

    Kyohei Muguruma, Mayu Ito, Akane Fukuda, Satoshi Kishimoto, Akihiro Taguchi, Kentaro Takayama, Atsuhiko Taniguchi, Yuji Ito, Yoshio Hayashi

    MedChemComm   10 ( 10 )   1789 - 1795   2019.10

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    Currently, IgG-binding peptides are widely utilized as a research tool, as molecules that guide substrates to the Fc site for site-selective antibody modification, leading to preparation of a homogeneous antibody-drug conjugate. In this study, a structure-activity relationship study of an IgG-binding peptide, 15-IgBP, that is focused on its C-terminal His residue was performed in an attempt to create more potent peptides. A peptide with a substitution of His17 by 2-pyridylalanine (2-Pya) showed a good binding affinity (15-His17(2-Pya), Kd = 75.7 nM). In combination with a previous result, we obtained 15-Lys8Leu/His17(2-Pya)-OH that showed a potent binding affinity (Kd = 2.48 nM) and avoided three synthetic problems concerning the p-hydroxybenzyl amidation at the C-terminus, the difficulty associated with coupling at the His7 position and the racemization of 2-Pya.

    DOI： 10.1039/c9md00294d

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  • Kinetics-Based Structural Requirements of Human Immunoglobulin G Binding Peptides. Reviewed International journal

    Kyohei Muguruma, Konomi Fujita, Akane Fukuda, Satoshi Kishimoto, Soichiro Sakamoto, Risako Arima, Mayu Ito, Mayu Kawasaki, Shogo Nakano, Sohei Ito, Kanade Shimizu, Akihiro Taguchi, Kentaro Takayama, Atsuhiko Taniguchi, Yuji Ito, Yoshio Hayashi

    ACS omega   4 ( 11 )   14390 - 14397   2019.9

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    Language：English   Publishing type：Research paper (scientific journal)  

    Currently, antibodies are widely used not only in research but also in therapy. Hence, peptides that selectively bind to the fragment crystallizable site of an antibody have been extensively utilized in various research efforts such as the preparation of antibody-drug conjugates (ADC). Consequently, appropriate peptides that bind to immunoglobulin G (IgG) with a specific Kd value and also kon and koff values will be useful in different applications, and these kinetic parameters have been perhaps overlooked but are key to development of peptide ligands with advantageous binding properties. We prepared structural derivatives of IgG-binding peptide 1 and evaluated the binding affinity and kinetic rates of the products by surface plasmon resonance assay and isothermal titration calorimetry to obtain novel peptides with beneficial antibody binding properties. In this way, 15-Lys8Leu with fast-binding and slow-release features was obtained through a shortened peptide 15-IgBP. On the other hand, we successfully obtained distinctive peptide, 15-Lys8Tle, with a similar Kd value but with kon and koff values that were as much as six-fold different from those of 15-IgBP. These new peptides are useful for the elucidation of kinetic effects on the function of IgG-binding peptides and various applications of antibody or antibody-drug interactions, such as immunoliposome, ADC, or half-life extension strategy, by using a peptide with the appropriate kinetic features.

    DOI： 10.1021/acsomega.9b01104

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  • An Efficient Method for the Conjugation of Hydrophilic and Hydrophobic Components by Solid-Phase-Assisted Disulfide Ligation Reviewed

    Kyohei Muguruma, Takuya Shirasaka, Daichi Akiyama, Kentarou Fukumoto, Akihiro Taguchi, Kentaro Takayama, Atsuhiko Taniguchi, Yoshio Hayashi

    Angewandte Chemie - International Edition   57 ( 8 )   2170 - 2173   2018.2

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    Language：English   Publishing type：Research paper (scientific journal)   Publisher：Wiley-VCH Verlag  

    DOI： 10.1002/anie.201712324

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  • 抗体部位特異的修飾法を用いた放射性医薬品の開発

    伊東祐二, 金山洋介, 林良雄, 六車共平

    Isotope News (Web)   ( 755 )   22‐24 (WEB ONLY)   2018.2

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    Language：Japanese  

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  • Development of Potent Myostatin Inhibitory Peptides through Hydrophobic Residue-Directed Structural Modification Reviewed

    Kentaro Takayama, Cedric Rentier, Tomo Akari, Akari Nakamura, Yusuke Saga, Takahiro Shimada, Kei Nirasawa, Eri Sasaki, Kyohei Muguruma, Akihiro Taguchi, Atsuhiko Taniguchi, Yoichi Negish, Yoshio Hayashi

    ACS MEDICINAL CHEMISTRY LETTERS   8 ( 7 )   751 - 756   2017.7

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    Language：English   Publishing type：Research paper (scientific journal)  

    DOI： 10.1021/acsmedchemlett.7b00168

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  • Click strategy using disodium salts of amino acids improves the water solubility of plinabulin and KPU-300 Reviewed

    Fumika Yakushiji, Kyohei Muguruma, Yoshiki Hayashi, Takuya Shirasaka, Ryosuke Kawamata, Hironari Tanaka, Yushi Yoshiwaka, Akihiro Taguchi, Kentaro Takayama, Yoshio Hayashi

    BIOORGANIC & MEDICINAL CHEMISTRY   25 ( 14 )   3623 - 3630   2017.7

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    Language：English   Publishing type：Research paper (scientific journal)  

    DOI： 10.1016/j.bmc.2017.04.024

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  • 3-Nitro-2-pyridinesulfenates as Efficient Solution- and Solid-Phase Disulfide Bond Forming Agents Reviewed

    Akihiro Taguchi, Kiyotaka Kobayashi, Akira Kotani, Kyohei Muguruma, Misaki Kobayashi, Kentarou Fukumoto, Kentaro Takayama, Hideki Hakamata, Yoshio Hayashi

    CHEMISTRY-A EUROPEAN JOURNAL   23 ( 34 )   8262 - 8267   2017.6

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    Language：English   Publishing type：Research paper (scientific journal)  

    DOI： 10.1002/chem.201700952

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  • Novel Hybrid Compound of a Plinabulin Prodrug with an IgG Binding Peptide for Generating a Tumor Selective Noncovalent-Type Antibody-Drug Conjugate Reviewed

    Kyohei Muguruma, Fumika Yakushiji, Ryosuke Kawamata, Daichi Akiyama, Risako Arirna, Takuya Shirasaka, Yamato Kikkawa, Akihiro Taguchi, Kentaro Takayama, Takeshi Fukuhara, Tetsuro Watabe, Yuji Ito, Yoshio Hayashi

    BIOCONJUGATE CHEMISTRY   27 ( 7 )   1606 - 1613   2016.7

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    Language：English   Publishing type：Research paper (scientific journal)  

    DOI： 10.1021/acs.bioconjchem.6b00149

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  • チューブリン重合阻害剤Plinabulinの非共有結合型抗体-薬物複合体創製研究

    有間 理沙子, 六車 共平, 川俣 亮介, 秋山 大地, 吉川 大和, 田口 晃弘, 高山 健太郎, 薬師寺 文華, 福原 武志, 渡部 徹郎, 林 良雄

    日本薬学会年会要旨集   136年会 ( 2 )   127 - 127   2016.3

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  • Development of a New Benzophenone-Diketopiperazine-Type Potent Antimicrotubule Agent Possessing a 2-Pyridine Structure Reviewed

    Yoshiki Hayashi, Haruka Takeno, Takumi Chinen, Kyohei Muguruma, Kohei Okuyama, Akihiro Taguchi, Kentaro Takayama, Fumika Yakushiji, Masahiko Miura, Takeo Usui, Yoshio Hayashi

    ACS MEDICINAL CHEMISTRY LETTERS   5 ( 10 )   1094 - 1098   2014.10

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    DOI： 10.1021/ml5001883

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  • Prodrug Study of Plinabulin Using a Click Strategy Focused on the Effects of a Replaceable Water-Solubilizing Moiety Reviewed

    Fumika Yakushiji, Hironari Tanaka, Kyohei Muguruma, Takahiro Iwahashi, Yuri Yamazaki, Yoshio Hayashi

    CHEMICAL & PHARMACEUTICAL BULLETIN   60 ( 7 )   877 - 881   2012.7

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    DOI： 10.1248/cpb.c12-00216

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  • Water-Soluble Prodrug of Antimicrotubule Agent Plinabulin: Effective Strategy with Click Chemistry Reviewed

    Fumika Yakushiji, Hironari Tanaka, Kyohei Muguruma, Takahiro Iwahashi, Yuri Yamazaki, Yoshio Hayashi

    CHEMISTRY-A EUROPEAN JOURNAL   17 ( 45 )   12587 - 12590   2011.11

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    DOI： 10.1002/chem.201102293

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Books

  • Pharmacia

    Kyohei Muguruma（ Role： Contributor）

    2023.2 

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  • Adv. Carbohydr. Chem. Biochem. Special Volume in Memory of Hidetoshi Yamada Part 2

    Kenshiro Yamada, Kyohei Muguruma, Katsunori Tanaka（ Role： ContributorChapter 2: Therapeutic in vivo Synthetic Chemistry using an Artificial Metalloenzyme with Glycosylated Human Serum Albumin）

    Elsevier  2022.12  （ ISBN:9780323985970 ）

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  • 化学

    六車共平, 田中克典（ Role： Contributor「最新のトピックス」 遷移金属触媒の力で病気を治す −体の中での薬物合成に向けて）

    化学同人  2022.7 

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  • 有機合成のための新触媒反応101

    六車共平, 張宗哲, 田中克典（ Role： Contributor42 クリック反応、79 グリコシド化）

    東京化学同人  2021.11  （ ISBN:9784807920051 ）

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    Total pages：x, 212p   Language：Japanese  

    CiNii Books

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  • Biophilia電子版21号, 特集 論理薬科学－創薬の基盤

    六車共平, 林良雄（ Role： Contributorペプチド-薬物複合体の効率的な合成法の開発）

    2017.4 

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  • 抗体薬物複合体(ADC)の設計開発

    六車共平, 林良雄（ Role： Contributor第4章 抗体結合ペプチドを用いた抗体-薬物複合体の創製）

    シーエムシー出版  2016.5  （ ISBN:9784781311593 ）

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    Total pages：vi, 194p   Language：Japanese  

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MISC

  • Cas9-sgRNA RNP delivery systems comprising tannic acid and fine-tuned boronic acid-conjugated polymers for tissue-selective in vivo genome editing

    千野利純, 千野利純, 松尾拓海, 松尾拓海, 本田雄士, 本田雄士, 本田雄士, 刑部祐里子, GUO Haochen, 六車共平, 六車共平, 三浦裕, 三浦裕, 西山伸宏, 西山伸宏, 西山伸宏

    日本薬学会年会要旨集(Web)   145th   2025

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  • Development of high-affinity antibody-binding peptide applicable to site-specific antibody modification

    大澤錬人, 六車共平, 福田茜, 藤田好珠, 石川直到, 田口晃弘, 高山健太郎, 谷口敦彦, 伊東裕二, 林良雄

    日本薬学会年会要旨集(Web)   141st   2021

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  • 9残基目グリシンに着目をしたヒトIgG抗体結合ペプチドの構造活性相関研究

    福田茜, 六車共平, 大澤錬人, 岸本聡, 田口晃弘, 高山健太郎, 谷口敦彦, 伊東祐二, 林良雄

    メディシナルケミストリーシンポジウム講演要旨集   37th   2019

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  • 抗体-薬物複合体への応用をめざした微小管重合阻害剤Plinabulinのジスルフィド型プロドラッグ創製研究

    佐藤菜那, 福田茜, 六車共平, 黒田綾, 遠藤京弥, 田口晃弘, 高山健太郎, 谷口敦彦, 伊東祐二, 林良雄

    メディシナルケミストリーシンポジウム講演要旨集   37th   2019

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  • NPYS化学を基盤とするペプチド合成化学から創薬までの研究展開

    林良雄, 田口晃弘, 六車共平, YAN Cui, 小林清孝

    日本薬学会関東支部大会講演要旨集   63rd   2019

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  • ヒトIgG抗体Fc部位結合ペプチドのC末端残基に着目をした構造活性相関研究

    福田茜, 六車共平, 伊藤真由, 藤田好珠, 坂本宗一郎, 岸本聡, 田口晃弘, 高山健太郎, 谷口敦彦, 伊東祐二, 林良雄

    創薬懇話会講演要旨集   2019   2019

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  • 抗体薬物複合体への適用を指向した抗体結合ペプチドの構造活性相関研究

    六車共平, 藤田好珠, 福田茜, 岸本聡, 有間理沙子, 田口晃弘, 高山健太郎, 谷口敦彦, 伊東祐二, 林良雄

    メディシナルケミストリーシンポジウム講演要旨集   36th   119   2018.11

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  • C末端ヒスチジン残基に着目した抗体結合ペプチドの構造活性相関研究

    伊藤真由, 六車共平, 坂本宗一郎, 福田茜, 岸本聡, 藤田好珠, 田口晃弘, 高山健太郎, 谷口敦彦, 伊東祐二, 林良雄

    日本薬学会関東支部大会講演要旨集   62nd   105   2018.9

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  • A New Aspect of Npys-based Solid Phase Disulfide Peptide Synthesis Reviewed

    Taguchi Akihiro, Muguruma Kyohei, Kobayashi Kiyotaka, Cui Yan, Rentier Cedric, Takayama Kentaro, Taniguchi Atsuhiko, Hayashi Yoshio

    JOURNAL OF PEPTIDE SCIENCE   24   S56 - S56   2018.9

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  • 効率的な抗体薬物複合体調製に向けた抗体Fc部位結合ペプチドの初期的構造活性相関研究

    福田茜, 六車共平, 藤田好珠, 坂本宗一郎, 岸本聡, 伊藤真由, 田口晃弘, 高山健太郎, 谷口敦彦, 伊東祐二, 林良雄

    創薬懇話会講演要旨集   2018   20   2018.6

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  • 抗体薬物複合体への適用を指向した抗体結合ペプチドの構造活性相関研究

    藤田好珠, 六車共平, 坂本宗一郎, 岸本聡, 伊藤真由, 田口晃弘, 高山健太郎, 谷口敦彦, 伊東祐二, 林良雄

    日本薬学会年会要旨集(CD-ROM)   138th   ROMBUNNO.26X‐pm14   2018

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  • 固相ジスルフィド架橋法による難水溶性薬物-水溶性ペプチド架橋体の合成

    六車共平, 田口晃弘, 高山健太郎, 谷口敦彦, 林良雄

    反応と合成の進歩シンポジウム講演要旨集   44th   2018

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  • 抗体Fc部結合ペプチドの構造活性相関研究

    六車共平, 坂本宗一郎, 藤田好珠, 伊藤真由, 田口晃弘, 高山健太郎, 谷口敦彦, 伊東祐二, 林良雄

    日本薬学会年会要旨集(CD-ROM)   138th   ROMBUNNO.S54‐4   2018

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  • 固相ジスルフィド化試薬によるペプチド‐薬物架橋体の合成と非共有結合型抗体薬物複合体への応用

    六車共平, 白坂拓也, 秋山大地, 田口晃弘, 高山健太郎, 谷口敦彦, 伊東祐二, 林良雄

    メディシナルケミストリーシンポジウム講演要旨集   35th   193   2017.10

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  • ヒトIgG結合ペプチドの初期的構造活性相関研究

    坂本宗一郎, 六車共平, 白坂拓也, 岸本聡, 藤田好珠, 有間理沙子, 田口晃弘, 高山健太郎, 谷口敦彦, 伊東祐二, 林良雄

    日本薬学会関東支部大会講演要旨集   61st   113   2017.9

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  • 3-ニトロ-2-ピリジンスルフェニル(Npys)構造を基盤とした新規ジスルフィド架橋試薬の創製研究

    小林清孝, 田口晃弘, 小谷明, 六車共平, 小林美咲, 崔岩, 福元謙太郎, 福元謙太郎, 高山健太郎, 谷口敦彦, 袴田秀樹, 林良雄

    日本薬学会関東支部大会講演要旨集   61st   2017

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  • 環状ジスルフィドペプチドの効率的合成を指向した新規ジスルフィド架橋試薬の創製

    小林清孝, 田口晃弘, 小谷明, 六車共平, 小林美咲, CUI Yan, 福元謙太郎, 福元謙太郎, 高山健太郎, 谷口敦彦, 袴田秀樹, 林良雄

    メディシナルケミストリーシンポジウム講演要旨集   35th   2017

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  • 固相担持型ジスルフィド化試薬を応用したPlinabulinプロドラッグの創製研究

    白坂拓也, 六車共平, 秋山大地, 田口晃弘, 高山健太郎, 谷口敦彦, 林良雄

    創薬懇話会講演要旨集   2017   2017

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  • 微小管重合阻害剤KPU-300を基盤とした構造活性相関研究

    林良樹, 久保木里衣, 佐久間千尋, 中澤大輝, 六車共平, 知念拓実, 田口晃弘, 高山健太郎, 薬師寺文華, 谷口敦彦, 臼井健郎, 林良雄

    メディシナルケミストリーシンポジウム講演要旨集   35th   2017

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  • 固相ジスルフィド架橋試薬を用いたペプチド-薬物架橋体の合成

    六車共平, 白坂拓也, 秋山大地, 田口晃弘, 高山健太郎, 谷口敦彦, 林良雄

    反応と合成の進歩シンポジウム講演要旨集   43rd   2017

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  • SPECIFIC CHEMICAL MODIFICATION OF HUMAN ANTIBODIES BY A REAGENT BASED ON FC-SPECIFIC AFFINITY PEPTIDE

    Y. Ito, S. Kishimoto, Y. Hayashi, K. Takayama, K. Muguruma, Y. Kanayama, N. Takahashi, R. Nakano, S. Takagi

    JOURNAL OF PEPTIDE SCIENCE   22   S16 - S18   2016.9

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  • APPLICATION OF FC-SELECTIVE Z33-PEPTIDE TO THE PREPARATION OF NON-COVALENT-TYPE ANTIBODY-ANTIMICROTUBULE PLINABULIN CONJUGATE

    K. Muguruma, R. Kawamata, D. Akiyama, R. Arima, T. Shirasaka, Y. Kikkawa, A. Taguchi, K. Takayama, T. Fukuhara, Y. Ito, Y. Hayashi

    JOURNAL OF PEPTIDE SCIENCE   22   S18 - S18   2016.9

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  • 固相担持型ジスルフィド化試薬を応用した腫瘍指向性ペプチド-Plinabulin架橋体の創生研究

    白坂拓也, 六車共平, 秋山大地, 田口晃弘, 高山健太郎, 林良雄

    創薬懇話会講演要旨集   2016   2016

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  • 3-ニトロ-2-ピリジンスルフェニル基を基盤とした新規ジスルフィド形成手法の創製とその応用

    田口晃弘, 小林清孝, 福元謙太郎, 福元謙太郎, 小林美咲, 六車共平, 浜田圭佑, 高山健太郎, 林良雄

    反応と合成の進歩シンポジウム講演要旨集   42nd   2016

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  • 固相反応を応用した新規Plinabulinプロドラッグ合成法の創製研究

    白坂拓也, 六車共平, 秋山大地, 田口晃弘, 高山健太郎, 薬師寺文華, 林良雄

    日本薬学会年会要旨集(CD-ROM)   136th   2016

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  • 3-ニトロ-2-ピリジンスルフェニル(Npys)を基盤とした新規ジスルフィド形成試薬の開発

    小林清孝, 田口晃弘, 小林美咲, 六車共平, 福元謙太郎, 福元謙太郎, 高山健太郎, 林良雄

    創薬懇話会講演要旨集   2016   2016

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  • 抗体結合ペプチドZ33を用いたチューブリン重合阻害剤Plinabulinの抗体-薬物複合体創製研究

    六車共平, 福原武志, 渡部徹郎, 林良雄

    日本がん分子標的治療学会学術集会プログラム・抄録集   19th   2015

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  • 固相担持型ジスルフィド化試薬を用いたチューブリン重合阻害剤Plinabulinのプロドラッグ合成研究

    秋山大地, 六車共平, 川俣亮介, 有間理沙子, 田口晃弘, 高山健太郎, 薬師寺文華, 林良雄

    日本薬学会関東支部大会講演要旨集   58th   2014

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  • Development of water-soluble prodrug of diketopiperazine-type antitumor agent "Plinabulin" by a skeletal transformation to monolactim

    Fumika Yakushiji, Kyohei Muguruma, Hironari Tanaka, Takehiro Iwahashi, Yuri Yamazaki, Yoshio Hayashi

    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY   244   2012.8

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  • An effective click strategy for water-soluble prodrug of the antimicrotubule agent ‘plinabulin’ Reviewed

    Yakushiji, Fumika, Tanaka, Hironari, Muguruma, Kyohei, Kawamata, Ryosuke, Yamazaki, Yuri, Takayama, Kentaro, Hayashi, Yoshio

    Peptide Science   7 - 8   2012

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  • Plinabulinの水溶性プロドラッグ合成研究:水溶性置換基の寄与について

    六車共平, 薬師寺文華, 田中達也, 山崎有理, 林良雄

    日本薬学会年会要旨集   132nd ( 2 )   2012

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  • クリックケミストリーを用いたチューブリン重合阻害剤Plinabulinの水溶性プロドラッグ合成研究

    田中達也, 薬師寺文華, 六車共平, 岩橋孝祐, 山崎有理, 林良雄

    日本薬学会年会要旨集   132nd ( 2 )   2012

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  • ジケトピペラジン型微小管重合阻害剤‘Plinabulin’の水溶性プロドラッグ合成研究

    薬師寺文華, 田中達也, 六車共平, 岩橋孝祐, 山崎有理, 林良雄

    反応と合成の進歩シンポジウム講演要旨集   37th   2011

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Industrial property rights

  • ペプチド、およびペプチドを用いる抗体の修飾

    林良雄, 六車共平, 福田茜, 浜地格, 田村朋則

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    Application no：特願2020-172768  Date applied：2020.10

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  • 複合体

    林良雄, 六車共平, 吉川大和, 伊東祐二

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    Application no：特願2019-096155  Date applied：2019.5

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Awards

  • JPS excellent poster presentation award

    2018.12   55th Japanese Peptide Symposium/10th International Peptide Symposium,  

    Kyohei Muguruma

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  • 富山学生ポスター賞

    2017.11   第43回 反応と合成の進歩シンポジウム,  

    六車共平

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  • Good Stone Award

    2016.10   53rd Japanese Peptide Symposium,  

    Kyohei Muguruma

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  • Poster Prize

    2016.7   14th Chinese International Peptide Symposium/5th Asia-pacific International Peptide Symposium,  

    六車共平

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  • Student Poster winner

    2015.12   Antibody engineering & therapeutics 2015,  

    六車共平

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  • 2015 Young Scientist Award

    2015.7  

    六車共平

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Research Projects

  • 金属錯体の配置制御による環境応答性 MRI造影剤の創製

    2026.2 - 2027.4

    公益財団法人 上原記念生命科学財団  2025年度 研究奨励金（A）領域 

    六車共平

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    Authorship：Principal investigator 

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  • フォールディング効果に基づく緩和性能の向上とグリーン造影剤の創製

    Grant number：25K03462  2025.4 - 2028.3

    日本学術振興会  科学研究費助成事業  基盤研究(B)

    三浦 裕, 六車 共平

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    Grant amount：\18980000 （ Direct Cost: \14600000 、 Indirect Cost：\4380000 ）

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  • Biodistribution control of IgG by selective inhibition of FcRn interaction

    Grant number：24K18258  2024.4 - 2027.3

    Japan Society for the Promotion of Science  Grants-in-Aid for Scientific Research  Grant-in-Aid for Early-Career Scientists

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    Grant amount：\4680000 （ Direct Cost: \3600000 、 Indirect Cost：\1080000 ）

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  • Temporary production of toxin for cancer stem cell treatment

    2023.8 - 2024.2

    RIKEN  Incentive research project 

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  • Catalytic activity regulation system with a bispecific metallopeptide

    Grant number：202201061014  2022.4 - 2025.3

    RIKEN 

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  • ペプチドを用いた触媒活性制御機構の開発

    Grant number：20K15968  2020.4 - 2023.3

    日本学術振興会  科学研究費助成事業 若手研究  若手研究

    六車 共平

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    Grant amount：\4160000 （ Direct Cost: \3200000 、 Indirect Cost：\960000 ）

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  • Ｆｃ 受容体への親和性改変を指向した生体内抗体修飾反応の開発

    Grant number：19J00396  2019.4 - 2022.3

    日本学術振興会  科学研究費助成事業 特別研究員奨励費 PD  特別研究員奨励費

    六車 共平

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    Grant amount：\4030000 （ Direct Cost: \3100000 、 Indirect Cost：\930000 ）

    抗体Fc部位を選択的に化学修飾することにより、抗体のFc受容体への親和性の改変に基づいた生体内抗体の機能制御を目的とし、生体内に適用可能な抗体修飾反応の開発をめざした。2021年度は、ヒト血清アルブミン（HSA）を核とするキャリアー分子とルテニウム触媒との複合体およびp-アミノベンジルフルオリド構造を有する反応基質を利用したがん細胞修飾反応をマウス体内で行い、本結果を研究成果として学術誌（Chem. Sci. 2021, 12, 12266）に報告した。この報告は、比較的不安定なルテニウム触媒をHSAと複合体を形成させることにより安定化し、生体内で利用できることを示したものであることに加え、ルテニウム触媒ーp-アミノベンジルフルオリドの触媒系が、抗体修飾反応に利用可能であることを示唆した。次に、抗体修飾に利用するために抗体結合ペプチド構造をルテニウム触媒に導入した化合物を合成した。10ステップの合成経路で、複数種類の誘導体を合成することに成功した。合成した触媒ペプチドはヒト血清アルブミンに対する結合能を示し、HSA複合体を形成することによって触媒の安定化作用が発揮されることが示唆された。また、単純な基質を用いたモデル実験では有意な基質変換能力を示した。すなわち、昨年度開発したp-アミノベンジルフルオリド構造を有する反応基質を用いたタンパク修飾反応により抗体修飾に利用できるものであり、生体内抗体修飾反応の基盤を確立することに成功した。

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  • 難修飾性抗がん剤の標的指向化に資する新規抗体修飾ペプチドの創製

    Grant number：15J09551  2015.4 - 2018.3

    日本学術振興会  科学研究費助成事業 特別研究員奨励費 DC1  特別研究員奨励費

    六車 共平

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    Authorship：Principal investigator  Grant type：Competitive

    Grant amount：\2500000 （ Direct Cost: \2500000 ）

    本研究課題では、抗体Fc部位に親和性を有するペプチドとしてZ33を用い抗体修飾ペプチドの創出をめざしてきた。しかし、Z33以外にも多くの抗体結合ペプチドが報告されていることから、平成29年度では、抗体結合能の評価系を再度検討し直し、他のペプチド誘導体の評価にも適応できるスクリーニング系を立ち上げた。本評価系は短時間での評価が可能であり、得られた数値もKd値と良好に相関する結果が得られた。結果として、当初の目的である抗体結合ペプチドZ33の構造誘導による共有結合型の抗体修飾ペプチドの獲得には至っていないが、本成果は今後の構造-抗体結合能相関研究および抗体修飾ペプチドの創出を加速させるものであると考える。
    また、昨年度の研究成果である固相ジスルフィド架橋法（solid-phase-assisted disulfide ligation, SPDSL）の汎用性の拡大をめざし、種々のPlinabulin-水溶性化合物の架橋体合成を行なった。本反応は、薬物（Plinabuin, 難水溶性）と抗体結合ペプチド（水溶性）のように溶解性の大きく異なる化合物間の架橋体を効率的に合成できるものである。結果として、通常の液相系での架橋反応による合成が困難なペプチド-薬物架橋体を中程度の単離収率で合成することに成功した。また、糖と薬物の架橋体合成も達成しており、本反応はペプチドのみならず、様々な化合物間の架橋反応に適応できるものであることが示唆された。本結果をまとめた報告が、原著論文として掲載に至っている（K. Muguruma et al., Angew. Chem. Int. Ed., 2018, 57, 2170）。

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Teaching Experience

  • 生命理工学基礎実験・演習第二

    2024.4 Institution：東京工業大学

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