Updated on 2025/09/25

写真a

 
Tanaka Tomohiro
 
Organization
Faculty of Medicine, Dentistry and Pharmaceutical Sciences Associate Professor
Position
Associate Professor
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Degree

  • 医学博士 ( 東京医科歯科大学 )

Research Interests

  • ケミカルバイオロジー

  • 有機合成化学

Research Areas

  • Life Science / Pharmaceutical chemistry and drug development sciences

Education

  • Tokyo Medical and Dental University     医歯学総合研究科博士課程後期

    2008.4 - 2011.3

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  • Tokyo Medical and Dental University     医歯学総合研究科博士課程前期

    2006.4 - 2008.3

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  • Tokyo University of Pharmacy and Life Science   薬学部  

    2002.4 - 2006.3

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Research History

  • Okayama University   学術研究院医歯薬学域   Associate Professor

    2022.10

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    Country:Japan

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  • Tokyo University of Science   Faculty of Pharmaceutical Sciences, Department of Medicinal and Life Science   Assistant Professor

    2019.10 - 2022.9

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  • The Noguchi Institute   糖鎖有機化学研究室   Researcher

    2016.3 - 2019.9

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  • Tokyo University of Science   Faculty of Pharmaceutical Sciences

    2012.10 - 2016.2

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  • ペンシルバニア大学   ポスドク研究員

    2011.5 - 2012.9

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Committee Memberships

  • 日本薬学会   ファルマシアトピックス小委員  

    2022.4 - 2024.3   

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    Committee type:Academic society

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Papers

  • Design, Synthesis, and Anti-SARS-CoV-2 Activity of Amodiaquine Analogs Reviewed

    Shin Aoki, Tomohiro Tanaka, Kenta Yokoi, Azusa Kanbe, Tomoe Morita, Mayuka Nii, Hidetoshi Satoh, Masaki Kakihana, Shotaro Otaki, Saki Sekiguchi, Koki Nakamura, Toshifumi Tojo, Masanori Baba, Mika Okamoto

    Chemical and Pharmaceutical Bulletin   73 ( 4 )   355 - 368   2025.4

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    Publishing type:Research paper (scientific journal)   Publisher:Pharmaceutical Society of Japan  

    DOI: 10.1248/cpb.c24-00647

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  • Synthesis of new functionalized bioactive S-substituted indolyl-triazoles as cytotoxic and apoptotic agents through multi-targeted kinase inhibition Reviewed

    Ahmed T.A. Boraei, Mohamed S. Nafie, Assem Barakat, Tomohiro Tanaka, Koshu Kawano, Toshifumi Tojo, Shin Aoki, Ahmed A.M. Sarhan

    Bioorganic Chemistry   156   108154 - 108154   2025.3

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

    DOI: 10.1016/j.bioorg.2025.108154

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  • Amodiaquine Analogs Are Potent Inhibitors of Interleukin-6 Production Induced by Activation of Toll-Like Receptors Recognizing Pathogen Nucleic Acids Reviewed

    Yohei Takenaka, Tomohiro Tanaka, Shotaro Otaki, Azusa Kanbe, Tomoe Morita, Kenta Yokoi, Saki Sekiguchi, Koki Nakamura, Hidetoshi Satoh, Toshifumi Tojo, Fumiaki Uchiumi, Kazuki Kitabatake, Shin Aoki, Mitsutoshi Tsukimoto

    Biological and Pharmaceutical Bulletin   47 ( 12 )   2101 - 2118   2024.12

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    Publishing type:Research paper (scientific journal)   Publisher:Pharmaceutical Society of Japan  

    DOI: 10.1248/bpb.b24-00639

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  • Detection of Circulating Tumor Cells in Blood Using Two-Step Random Forest Reviewed

    Hua Wei, Takahiro Natori, Tomohiro Tanaka, Shin Aoki, Sho Kuriyama, Takeshi Yamada, Naoyuki Aikawa

    IEEJ Transactions on Electronics, Information and Systems   144 ( 3 )   121 - 126   2024.3

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    Publishing type:Research paper (scientific journal)   Publisher:Institute of Electrical Engineers of Japan (IEE Japan)  

    DOI: 10.1541/ieejeiss.144.121

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  • Design and Synthesis of Poly(2,2′-Bipyridyl) Ligands for Induction of Cell Death in Cancer Cells: Control of Anticancer Activity by Complexation/Decomplexation with Biorelevant Metal Cations Reviewed

    Chandrasekar Balachandran, Masumi Hirose, Tomohiro Tanaka, Jun Jie Zhu, Kenta Yokoi, Yosuke Hisamatsu, Yasuyuki Yamada, Shin Aoki

    Inorganic Chemistry   2023.8

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    Publishing type:Research paper (scientific journal)   Publisher:American Chemical Society (ACS)  

    DOI: 10.1021/acs.inorgchem.3c01738

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  • Post-complexation Functionalization of Cyclometalated Iridium(III) Complexes and Applications to Biomedical and Material Sciences Reviewed

    Shin Aoki, Kenta Yokoi, Yosuke Hisamatsu, Chandrasekar Balachandran, Yuichi Tamura, Tomohiro Tanaka

    Topics in Current Chemistry   380 ( 5 )   2022.10

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    Publishing type:Research paper (scientific journal)   Publisher:Springer Science and Business Media LLC  

    DOI: 10.1007/s41061-022-00401-w

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    Other Link: https://link.springer.com/article/10.1007/s41061-022-00401-w/fulltext.html

  • Design, Synthesis and Biological Evaluation of Boron‐Containing Macrocyclic Polyamine Dimers and Their Zinc(II) Complexes for Boron Neutron Capture Therapy Reviewed

    Hiroki Ueda, Minoru Suzuki, Yoshinori Sakurai, Tomohiro Tanaka, Shin Aoki

    European Journal of Inorganic Chemistry   2022 ( 5 )   2022.2

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

    DOI: 10.1002/ejic.202100949

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    Other Link: https://onlinelibrary.wiley.com/doi/full-xml/10.1002/ejic.202100949

  • The structure of POMGNT2 provides new insights into the mechanism to determine the functional O ‐mannosylation site on α‐dystroglycan Reviewed

    Rieko Imae, Naoyuki Kuwabara, Hiroshi Manya, Tomohiro Tanaka, Masato Tsuyuguchi, Mamoru Mizuno, Tamao Endo, Ryuichi Kato

    Genes to Cells   26 ( 7 )   485 - 494   2021.7

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

    DOI: 10.1111/gtc.12853

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    Other Link: https://onlinelibrary.wiley.com/doi/full-xml/10.1111/gtc.12853

  • Design, Synthesis, and Biological Evaluation of Boron-Containing Macrocyclic Polyamines and Their Zinc(II) Complexes for Boron Neutron Capture Therapy Reviewed

    Hiroki Ueda, Minoru Suzuki, Reiko Kuroda, Tomohiro Tanaka, Shin Aoki

    Journal of Medicinal Chemistry   64 ( 12 )   8523 - 8544   2021.6

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    Publishing type:Research paper (scientific journal)   Publisher:American Chemical Society (ACS)  

    DOI: 10.1021/acs.jmedchem.1c00445

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  • Mefloquine, a Potent Anti-severe Acute Respiratory Syndrome-Related Coronavirus 2 (SARS-CoV-2) Drug as an Entry Inhibitor in vitro Reviewed

    Kaho Shionoya, Masako Yamasaki, Shoya Iwanami, Yusuke Ito, Shuetsu Fukushi, Hirofumi Ohashi, Wakana Saso, Tomohiro Tanaka, Shin Aoki, Kouji Kuramochi, Shingo Iwami, Yoshimasa Takahashi, Tadaki Suzuki, Masamichi Muramatsu, Makoto Takeda, Takaji Wakita, Koichi Watashi

    Frontiers in Microbiology   12   2021.4

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    Publishing type:Research paper (scientific journal)   Publisher:Frontiers Media SA  

    Coronavirus disease 2019 (COVID-19) has caused serious public health, social, and economic damage worldwide and effective drugs that prevent or cure COVID-19 are urgently needed. Approved drugs including Hydroxychloroquine, Remdesivir or Interferon were reported to inhibit the infection or propagation of severe acute respiratory syndrome-related coronavirus 2 (SARS-CoV-2), however, their clinical efficacies have not yet been well demonstrated. To identify drugs with higher antiviral potency, we screened approved anti-parasitic/anti-protozoal drugs and identified an anti-malarial drug, Mefloquine, which showed the highest anti-SARS-CoV-2 activity among the tested compounds. Mefloquine showed higher anti-SARS-CoV-2 activity than Hydroxychloroquine in VeroE6/TMPRSS2 and Calu-3 cells, with IC50 = 1.28 μM, IC90 = 2.31 μM, and IC99 = 4.39 μM in VeroE6/TMPRSS2 cells. Mefloquine inhibited viral entry after viral attachment to the target cell. Combined treatment with Mefloquine and Nelfinavir, a replication inhibitor, showed synergistic antiviral activity. Our mathematical modeling based on the drug concentration in the lung predicted that Mefloquine administration at a standard treatment dosage could decline viral dynamics in patients, reduce cumulative viral load to 7% and shorten the time until virus elimination by 6.1 days. These data cumulatively underscore Mefloquine as an anti-SARS-CoV-2 entry inhibitor.

    DOI: 10.3389/fmicb.2021.651403

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  • Potential anti-COVID-19 agents, cepharanthine and nelfinavir, and their usage for combination treatment Reviewed

    Hirofumi Ohashi, Koichi Watashi, Wakana Saso, Kaho Shionoya, Shoya Iwanami, Takatsugu Hirokawa, Tsuyoshi Shirai, Shigehiko Kanaya, Yusuke Ito, Kwang Su Kim, Takao Nomura, Tateki Suzuki, Kazane Nishioka, Shuji Ando, Keisuke Ejima, Yoshiki Koizumi, Tomohiro Tanaka, Shin Aoki, Kouji Kuramochi, Tadaki Suzuki, Takao Hashiguchi, Katsumi Maenaka, Tetsuro Matano, Masamichi Muramatsu, Masayuki Saijo, Kazuyuki Aihara, Shingo Iwami, Makoto Takeda, Jane A. McKeating, Takaji Wakita

    iScience   24 ( 4 )   102367 - 102367   2021.4

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

    DOI: 10.1016/j.isci.2021.102367

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  • Development of metallosupramolecular phosphatases based on the combinatorial self-assembly of metal complexes and organic building blocks for the catalytic hydrolysis of phosphate monoesters Reviewed

    Shin Aoki, Akib Bin Rahman, Yosuke Hisamatsu, Yuya Miyazawa, Mohd Zulkefeli, Yutaka Saga, Tomohiro Tanaka

    Results in Chemistry   3   100133 - 100133   2021.1

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

    DOI: 10.1016/j.rechem.2021.100133

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  • Crystal structures of fukutin-related protein (FKRP), a ribitol-phosphate transferase related to muscular dystrophy Reviewed

    Naoyuki Kuwabara, Rieko Imae, Hiroshi Manya, Tomohiro Tanaka, Mamoru Mizuno, Hiroki Tsumoto, Motoi Kanagawa, Kazuhiro Kobayashi, Tatsushi Toda, Toshiya Senda, Tamao Endo, Ryuichi Kato

    Nature Communications   11 ( 1 )   2020.1

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    Publishing type:Research paper (scientific journal)   Publisher:Springer Science and Business Media LLC  

    Abstract

    α-Dystroglycan (α-DG) is a highly-glycosylated surface membrane protein. Defects in the O-mannosyl glycan of α-DG cause dystroglycanopathy, a group of congenital muscular dystrophies. The core M3 O-mannosyl glycan contains tandem ribitol-phosphate (RboP), a characteristic feature first found in mammals. Fukutin and fukutin-related protein (FKRP), whose mutated genes underlie dystroglycanopathy, sequentially transfer RboP from cytidine diphosphate-ribitol (CDP-Rbo) to form a tandem RboP unit in the core M3 glycan. Here, we report a series of crystal structures of FKRP with and without donor (CDP-Rbo) and/or acceptor [RboP-(phospho-)core M3 peptide] substrates. FKRP has N-terminal stem and C-terminal catalytic domains, and forms a tetramer both in crystal and in solution. In the acceptor complex, the phosphate group of RboP is recognized by the catalytic domain of one subunit, and a phosphate group on O-mannose is recognized by the stem domain of another subunit. Structure-based functional studies confirmed that the dimeric structure is essential for FKRP enzymatic activity.

    DOI: 10.1038/s41467-019-14220-z

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    Other Link: https://www.nature.com/articles/s41467-019-14220-z

  • Efficient synthesis of N- and O-linked glycopeptides using acid-labile Boc groups for the protection of carbohydrate moieties Reviewed

    Tomohiro Tanaka, Mika Shiraishi, Akio Matsuda, Mamoru Mizuno

    Tetrahedron Letters   60 ( 40 )   151106 - 151106   2019.10

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    DOI: 10.1016/j.tetlet.2019.151106

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  • Design, synthesis and biological evaluation of low molecular weight CXCR4 ligands. Reviewed

    Sakyiamah MM, Kobayakawa T, Fujino M, Konno M, Narumi T, Tanaka T, Nomura W, Yamamoto N, Murakami T, Tamamura H

    Bioorganic & medicinal chemistry   27 ( 6 )   1130 - 1138   2019.3

  • Design, synthesis and biological evaluation of low molecular weight CXCR4 ligands Reviewed

    Sakyiamah MM, Kobayakawa T, Fujino M, KonnoM, Narumi T, Tanaka T, Nomura W, Yamamoto N, Murakami T, Tamamura H

    ChemMedChem   8 ( 1 )   118 - 124   2019

  • Design and synthesis of boron containing monosaccharides by the hydroboration of d-glucal for use in boron neutron capture therapy (BNCT). Reviewed

    Itoh T, Tamura K, Ueda H, Tanaka T, Sato K, Kuroda R, Aoki S

    Bioorganic & medicinal chemistry   26 ( 22 )   5922 - 5933   2018.12

  • CDP-glycerol inhibits the synthesis of the functional O-mannosyl glycan of α-dystroglycan Reviewed

    Rieko Imae, Hiroshi Manya, Hiroki Tsumoto, Kenji Osumi, Tomohiro Tanaka, Mamoru Mizuno, Motoi Kanagawa, Kazuhiro Kobayashi, Tatsushi Toda, Tamao Endo

    Journal of Biological Chemistry   293 ( 31 )   12186 - 12198   2018.8

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

    DOI: 10.1074/jbc.ra118.003197

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  • Bivalent 14-mer peptide ligands of CXCR4 with polyproline linkers with anti-chemotactic activity against Jurkat cells Reviewed

    Tomohiro Tanaka, Toru Aoki, Wataru Nomura, Hirokazu Tamamura

    JOURNAL OF PEPTIDE SCIENCE   23 ( 7-8 )   574 - 580   2017.7

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    DOI: 10.1002/psc.2946

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  • Concise and Versatile Synthesis of Sulfoquinovosyl Acyl Glycerol Derivatives for Biological Applications Reviewed

    Tomohiro Tanaka, Yasuhiro Sawamoto, Shin Aoki

    CHEMICAL & PHARMACEUTICAL BULLETIN   65 ( 6 )   566 - 572   2017.6

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    DOI: 10.1248/cpb.c17-00135

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  • B-11 NMR Probes of Copper(II): Finding and Implications of the Cu2+-Promoted Decomposition of ortho-Carborane Derivatives Reviewed

    Tomohiro Tanaka, Yukiko Nishiura, Rikita Araki, Takaomi Saido, Ryo Abe, Shin Aoki

    EUROPEAN JOURNAL OF INORGANIC CHEMISTRY   ( 12 )   1819 - 1834   2016.4

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    DOI: 10.1002/ejic.201600117

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  • Development of a fluoride-responsive amide bond cleavage device that is potentially applicable to a traceable linker Reviewed

    Yamamoto, J, Maeda, N, Komiya, C, Tanaka, T, Denda, M, Ebisuno, K, Nomura, W, Tamamura, H, Sato, Y, Yamauchi, A, Shigenaga, A, Otaka, A

    Tetrahedron   70   5122 - 5127   2014

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    DOI: 10.1016/j.tet.2014.05.110

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  • Development of a traceable linker containing a thiol-responsive amino acid for the enrichment and selective labelling of target proteins Reviewed

    Jun Yamamoto, Masaya Denda, Nami Maeda, Miku Kita, Chiaki Komiya, Tomohiro Tanaka, Wataru Nomura, Hirokazu Tamamura, Youichi Sato, Aiko Yamauchi, Akira Shigenaga, Akira Otaka

    ORGANIC & BIOMOLECULAR CHEMISTRY   12 ( 23 )   3821 - 3826   2014

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    DOI: 10.1039/c4ob00622d

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  • Cell-permeable stapled peptides based on HIV-1 integrase inhibitors derived from HIV-1 Gene products Reviewed

    Wataru Nomura, Haruo Aikawa, Nami Ohashi, Emiko Urano, Mathieu Métifiot, Masayuki Fujino, Kasthuraiah Maddali, Taro Ozaki, Ami Nozue, Tetsuo Narumi, Chie Hashimoto, Tomohiro Tanaka, Yves Pommier, Naoki Yamamoto, Jun A. Komano, Tsutomu Murakami, Hirokazu Tamamura

    ACS Chemical Biology   8 ( 10 )   2235 - 2244   2013.10

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    Language:English   Publishing type:Research paper (scientific journal)   Publisher:American Chemical Society  

    DOI: 10.1021/cb400495h

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  • Expressed protein ligation at methionine: N-terminal attachment of homocysteine, ligation, and masking. Reviewed International journal

    Tomohiro Tanaka, Anne M Wagner, John B Warner, Yanxin J Wang, E James Petersson

    Angewandte Chemie (International ed. in English)   52 ( 24 )   6210 - 3   2013.6

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    DOI: 10.1002/anie.201302065

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  • Biological Effects of Bivalent-type CXCR4 Ligands with Rigid Linkers Reviewed

    Nomura W, Tanaka T, Aoki T, Narumi T, Tamamura H

    BIOPOLYMERS   100 ( 3 )   296 - 296   2013.5

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  • 腫瘍認識プローブ・HIV阻害剤としてのケモカイン受容体リガンド Reviewed

    野村 渉, 田中 智博, 大橋 南美, 玉村 啓和

    生体材料工学研究所年報   46   28 - 31   2013.3

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    Language:Japanese   Publisher:東京医科歯科大学生体材料工学研究所  

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  • Low-Molecular-Weight CXCR4 Ligands with Variable Spacers Reviewed

    Tetsuo Narumi, Haruo Aikawa, Tomohiro Tanaka, Chie Hashimoto, Nami Ohashi, Wataru Nomura, Takuya Kobayakawa, Hikaru Takano, Yuki Hirota, Tsutomu Murakami, Naoki Yamamoto, Hirokazu Tamamura

    ChemMedChem   8 ( 1 )   118 - 124   2013.1

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

    DOI: 10.1002/cmdc.201200390

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  • Bivalent ligands for the chemokine receptor CXCR4 dimer and their function Reviewed

    Nomura W, Tanaka T, Aikawa H, Narumi T, Tamamura H

    JOURNAL OF PEPTIDE SCIENCE   18   S47 - S47   2012.9

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  • HIV inhibitors targeting entry, fusion, and integrase Reviewed

    Narumi Tetsuo, Tanaka Tomohiro, Nomura Wataru, Aikawa Haruo, Tamamura Hirokazu

    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY   244   2012.8

  • Pharmacophore-based small molecule CXCR4 ligands Reviewed

    Tetsuo Narumi, Tomohiro Tanaka, Chie Hashimoto, Wataru Nomura, Haruo Aikawa, Akira Sohma, Kyoko Itotani, Miyako Kawamata, Tsutomu Murakami, Naoki Yamamoto, Hirokazu Tamamura

    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS   22 ( 12 )   4169 - 4172   2012.6

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    DOI: 10.1016/j.bmcl.2012.04.032

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  • Conjugation of cell-penetrating peptides leads to identification of anti-HIV peptides from matrix proteins Reviewed

    Tetsuo Narumi, Mao Komoriya, Chie Hashimoto, Honggui Wu, Wataru Nomura, Shintaro Suzuki, Tomohiro Tanaka, Joe Chiba, Naoki Yamamoto, Tsutomu Murakami, Hirokazu Tamamura

    BIOORGANIC & MEDICINAL CHEMISTRY   20 ( 4 )   1468 - 1474   2012.2

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    DOI: 10.1016/j.bmc.2011.12.055

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  • A Synthetic C34 Trimer of HIV-1 gp41 Shows Significant Increase in Inhibition Potency Reviewed

    Wataru Nomura, Chie Hashimoto, Aki Ohya, Kosuke Miyauchi, Emiko Urano, Tomohiro Tanaka, Tetsuo Narumi, Toru Nakahara, Jun A. Komano, Naoki Yamamoto, Hirokazu Tamamura

    CHEMMEDCHEM   7 ( 2 )   205 - 208   2012.2

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    DOI: 10.1002/cmdc.201100542

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  • The successes and failures of HIV drug discovery Reviewed

    Chie Hashimoto, Tomohiro Tanaka, Tetsuo Narumi, Wataru Nomura, Hirokazu Tamamura

    EXPERT OPINION ON DRUG DISCOVERY   6 ( 10 )   1067 - 1090   2011.10

  • Azamacrocyclic Metal Complexes as CXCR4 Antagonists Reviewed

    Tomohiro Tanaka, Tetsuo Narumi, Taro Ozaki, Akira Sohma, Nami Ohashi, Chie Hashimoto, Kyoko Itotani, Wataru Nomura, Tsutomu Murakami, Yamamoto B. Naoki, Hirokazu Tamamura

    CHEMMEDCHEM   6 ( 5 )   834 - 839   2011.5

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    DOI: 10.1002/cmdc.201000548

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  • Design and Synthesis of Traceable Linker for Efficient Enrichment and Specific Labeling of Target Proteins Reviewed

    Yamamoto Jun, Tanaka Tomohiro, Denda Masaya, Shigenaga Akira, Nomura Wataru, Tamamura Hirokazu, Otaka Akira

    BIOPOLYMERS   96 ( 4 )   492   2011

  • Development of Bivalent Ligands for CXCR4 with Rigid Linkers and Application to Detection of Cancer Cells Reviewed

    Nomura Wataru, Tomohiro Tanaka, Akemi Masuda, Tetsuo Narumi, Hirokazu Tamamura

    BIOPOLYMERS   96 ( 4 )   510 - 511   2011

  • Synthesis and Application of Fluorescent-labeled Bivalent-type CXCR4 Ligands

    Aikawa Haruo, Nomura Wataru, Narumi Tetsuo, Tanaka Tomohiro, Tamamura Hirokazu

    Proceedings of the Symposium on Progress in Organic Reactions and Syntheses   37   109 - 109   2011

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    Language:Japanese   Publisher:Division of Organic Chemistry, The Pharmaceutical Society of Japan  

    We have synthesized bivalent CXCR4 ligands consisting of two molecules of a cyclic pentapeptide cFC131 connected by poly(L-prolines), and the maximum increase in their binding affinity for CXCR4 was observed when the length of linker were 5.5 to 6.5 nm. Here, we synthesized a bivalent ligand with a cyanine dye which would have a property of light absorption and emission in near infrared (NIR) region. Two molecules of cFC131 were conjugated with proline linker through the reaction between the thiol group of cFC131 and the chloroacetyl moiety of proline linker terminals. The obtained azido-peptide was coupled with alkynylcyanine by copper(I)-catalyzed azido/alkyne cycloaddition (CuAAC) reaction. The fluorescent-labeled bivalent ligand was purified by HPLC and characterized by ESI-MS.

    DOI: 10.14895/hannou.37.0.109.0

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  • Bivalent Ligands of CXCR4 with Rigid Linkers for Elucidation of the Dimerization State in Cells Reviewed

    Tomohiro Tanaka, Wataru Nomura, Tetsuo Narumi, Akemi Masuda, Hirokazu Tamamura

    JOURNAL OF THE AMERICAN CHEMICAL SOCIETY   132 ( 45 )   15899 - 15901   2010.11

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    DOI: 10.1021/ja107447w

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  • HIV-1遺伝子産物由来のインテグラーゼ阻害剤の創出 Reviewed

    橋本 知恵, 田中 智博, 浦野 恵美子, 尾崎 太郎, 新井 啓之, 鳴海 哲夫, 野村 渉, Maddali Kasthuraiah, Pommier Yves, 山本 直樹, 駒野 淳, 玉村 啓和

    日本エイズ学会誌   12 ( 4 )   370 - 370   2010.11

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  • gp120のCD4結合サイトを模倣した新規抗原分子の創製 Reviewed

    尾崎 太郎, 田中 智博, 宮内 浩典, 橋本 知恵, 鳴海 哲夫, 野村 渉, 山本 直樹, 駒野 淳, 玉村 啓和

    日本エイズ学会誌   12 ( 4 )   484 - 484   2010.11

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  • HIV-1侵入過程の動的超分子機構を基にした新規エイズワクチンの創製 Reviewed

    橋本 知恵, 鳴海 哲夫, 野村 渉, 中原 徹, 田中 智博, 大庭 賢二, 相馬 晃, 長谷山 正樹, 村上 努, 山本 直樹, 玉村 啓和

    日本エイズ学会誌   12 ( 4 )   483 - 483   2010.11

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  • CD4 mimics targeting the HIV entry mechanism and their hybrid molecules with a CXCR4 antagonist Reviewed

    Tetsuo Narumi, Chihiro Ochiai, Kazuhisa Yoshimura, Shigeyoshi Harada, Tomohiro Tanaka, Wataru Nomura, Hiroshi Arai, Taro Ozaki, Nami Ohashi, Shuzo Matsushita, Hirokazu Tamamura

    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS   20 ( 19 )   5853 - 5858   2010.10

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    DOI: 10.1016/j.bmcl.2010.07.106

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  • Peptidic HIV integrase inhibitors derived from HIV gene products: Structure-activity relationship studies Reviewed

    Shintaro Suzuki, Kasthuraiah Maddali, Chie Hashimoto, Emiko Urano, Nami Ohashi, Tomohiro Tanaka, Taro Ozaki, Hiroshi Arai, Hiroshi Tsutsumi, Tetsuo Narumi, Wataru Nomura, Naoki Yamamoto, Yves Pommier, Jun A. Komano, Hirokazu Tamamura

    BIOORGANIC & MEDICINAL CHEMISTRY   18 ( 18 )   6771 - 6775   2010.9

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    DOI: 10.1016/j.bmc.2010.07.050

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  • Peptide HIV-1 integrase inhibitors from HIV-1 gene products. Reviewed

    Suzuki S, Urano E, Hashimoto C, Tsutsumi H, Nakahara T, Tanaka T, Nakanishi Y, Maddali K, Han Y, Hamatake M, Miyauchi K, Pommier Y, Beutler JA, Sugiura W, Fuji H, Hoshino T, Itotani K, Nomura W, Narumi T, Yamamoto N, Komano JA, Tamamura H

    Journal of medicinal chemistry   53 ( 14 )   5356 - 5360   2010.7

  • Remodeling of Dynamic Structures of HIV-1 Envelope Proteins Leads to Synthetic Antigen Molecules Inducing Neutralizing Antibodies Reviewed

    Toru Nakahara, Wataru Nomura, Kenji Ohba, Aki Ohya, Tomohiro Tanaka, Chie Hashimoto, Tetsuo Narumi, Tsutomu Murakami, Naoki Yamamoto, Hirokazu Tamamura

    BIOCONJUGATE CHEMISTRY   21 ( 4 )   709 - 714   2010.4

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    DOI: 10.1021/bc900502z

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  • 合成抗原ペプチドによるHIV-1 gp41の三量体構造を認識する抗体の誘導 Reviewed

    野村 渉, 中原 徹, 大矢 亜紀, 大庭 賢二, 田中 智博, 橋本 知恵, 鳴海 哲夫, 村上 努, 山本 直樹, 玉村 啓和

    日本薬学会年会要旨集   130年会 ( 2 )   114 - 114   2010.3

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  • エイズワクチンを指向した宿主受容体CXCR4由来抗原分子の創製 Reviewed

    橋本 知恵, 野村 渉, 田中 智博, 中原 徹, 鳴海 哲夫, 大庭 賢二, 村上 努, 山本 直樹, 玉村 啓和

    日本薬学会年会要旨集   130年会 ( 2 )   71 - 71   2010.3

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  • CD4 mimics targeting the mechanism of HIV entry. Reviewed

    Yamada Y, Ochiai C, Yoshimura K, Tanaka T, Ohashi N, Narumi T, Nomura W, Harada S, Matsushita S, Tamamura H

    Bioorganic & medicinal chemistry letters   20 ( 1 )   354 - 358   2010.1

  • Beyond antibodyという研究領域 ペプチドミメティクを基盤とした阻害剤と新規概念によるワクチン Reviewed

    玉村 啓和, 野村 渉, 鳴海 哲夫, 田中 智博, 駒野 淳, 山本 直樹

    日本生化学会大会プログラム・講演要旨集   82回   1S4a - 4   2009.9

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  • センシングバイオロジーを指向した蛍光性CXCR4プローブの創出とリガンドスクリーニング法の開発 Reviewed

    堤 浩, 野村 渉, 田中 智博, 田部 泰章, 糸谷 恭子, 玉村 啓和

    生体材料工学研究所年報   42   3 - 7   2009.3

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  • Fluorogenically Active Leucine Zipper Peptides as Tag-Probe Pairs for Protein Imaging in Living Cells Reviewed

    Hiroshi Tsutsumi, Wataru Nomura, Seiichiro Abe, Tomoaki Mino, Akemi Masuda, Nami Ohashi, Tomohiro Tanaka, Kenji Ohba, Naoki Yamamoto, Kazunari Akiyoshi, Hirokazu Tamamura

    ANGEWANDTE CHEMIE-INTERNATIONAL EDITION   48 ( 48 )   9164 - 9166   2009

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    DOI: 10.1002/anie.200903183

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  • Development of chemokine receptor CXCR4 antagonists using bio-mimetic strategy. Reviewed

    Tamamura H, Tanaka T, Tsutsumi H, Ohashi N, Hiramatsu K, Araki T, Ojida A, Hamachi I, Wang Z, Peiper SC, Trent JO, Ueda S, Oishi S, Fujii N

    Advances in experimental medicine and biology   611   145 - 146   2009

  • Stereoselective synthesis of peptidomimetics based on acid-catalyzed ring-opening of beta-aziridinyl-alpha,beta-enoates. Reviewed

    Tamamura H, Tanaka T, Tsutsumi H, Nemoto K, Mizokami S, Ohashi N, Oishi S, Fujii N

    Advances in experimental medicine and biology   611   149 - 150   2009

  • Structure-activity relationship study on artificial CXCR4 ligands possessing the cyclic pentapeptide scaffold: the exploration of amino acid residues of pentapeptides by substitutions of several aromatic amino acids Reviewed

    Tomohiro Tanaka, Wataru Nomura, Tetsuo Narumi, Ai Esaka, Shinya Oishi, Nami Ohashi, Kyoko Itotani, Barry J. Evans, Zi-xuan Wang, Stephen C. Peiper, Nobutaka Fujii, Hirokazu Tamamura

    ORGANIC & BIOMOLECULAR CHEMISTRY   7 ( 18 )   3805 - 3809   2009

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    DOI: 10.1039/b908286g

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  • A future perspective on the development of chemokine receptor CXCR4 antagonists Reviewed

    Hirokazu Tamamura, Hiroshi Tsutsumi, Wataru Nomura, Tomohiro Tanaka, Nobutaka Fujii

    EXPERT OPINION ON DRUG DISCOVERY   3 ( 10 )   1155 - 1166   2008.10

  • Fluorophore labeling enables imaging and evaluation of specific CXCR4-ligand interaction at the cell membrane for fluorescence-based screening Reviewed

    Wataru Nomura, Yasuaki Tanabe, Hiroshi Tsutsumi, Tomohiro Tanaka, Kenji Ohba, Naoki Yamamoto, Hirokazu Tamamura

    BIOCONJUGATE CHEMISTRY   19 ( 9 )   1917 - 1920   2008.9

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    DOI: 10.1021/bc800216p

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  • HIV侵入の動的超分子機構を標的としたCD4 mimic small moleculeの創製 Reviewed

    山田 裕子, 吉村 和久, 田中 智博, 堤 浩, 野村 渉, 糸谷 恭子, 増野 弘幸, 柴田 潤二, 畑田 万紀子, 松下 修三, 玉村 啓和

    日本薬学会年会要旨集   128年会 ( 2 )   84 - 84   2008.3

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  • Structure-activity relationship study of CXCR4 antagonists bearing the cyclic pentapeptide scaffold: identification of the new pharmacophore Reviewed

    Tomohiro Tanaka, Hiroshi Tsutsumi, Wataru Nomura, Yasuaki Tanabe, Nami Ohashi, Ai Esaka, Chihiro Ochiai, Jun Sato, Kyoko Itotani, Tsutomu Murakami, Kenji Ohba, Naoki Yamamoto, Nobutaka Fujii, Hirokazu Tamamura

    ORGANIC & BIOMOLECULAR CHEMISTRY   6 ( 23 )   4374 - 4377   2008

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    DOI: 10.1039/b812029c

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  • Versatile use of acid-catalyzed ring-opening of beta-aziridinyl-alpha,beta-enoates to stereoselective synthesis of peptidomimetics Reviewed

    Hirokazu Tamamura, Tomohiro Tanaka, Hiroshi Tsutsumi, Koji Nemoto, Satoko Mizokami, Nami Ohashi, Shinya Oishi, Nobutaka Fujii

    TETRAHEDRON   63 ( 37 )   9243 - 9254   2007.9

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    DOI: 10.1016/j.tet.2007.06.029

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  • Therapeutic potential of the chemokine receptor CXCR4 antagonists as multifunctional agents Invited Reviewed

    Hiroshi Tsutsumi, Tomohiro Tanaka, Nami Ohashi, Hiroyuki Masuno, Hirokazu Tamamura, Kenichi Hiramatsu, Takanobu Araki, Satoshi Ueda, Shinya Oishi, Nobutaka Fujii

    BIOPOLYMERS   88 ( 2 )   279 - 289   2007

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    DOI: 10.1002/bip.20653

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MISC

  • CDP-glycerolはα-ジストログリカンの糖鎖伸長を阻害する

    今江 理恵子, 萬谷 博, 津元 裕樹, 田中 智博, 水野 真盛, 金川 基, 小林 千浩, 戸田 達史, 遠藤 玉夫

    日本生化学会大会プログラム・講演要旨集   91回   [1P - 033]   2018.9

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  • 福山型筋ジストロフィー原因遺伝子産物fukutinのグリセロールリン酸転移活性

    萬谷 博, 今江 理恵子, 津元 裕樹, 田中 智博, 水野 真盛, 金川 基, 小林 千浩, 戸田 達史, 遠藤 玉夫

    日本筋学会学術集会プログラム・抄録集   4回   162 - 162   2018.8

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  • 筋ジストロフィー症原因遺伝子産物フクチンはジストログリカン糖鎖にグリセロールリン酸を導入する活性を有する

    今江 理恵子, 萬谷 博, 津元 裕樹, 田中 智博, 水野 真盛, 金川 基, 小林 千浩, 戸田 達史, 遠藤 玉夫

    日本薬学会年会要旨集   138年会 ( 3 )   105 - 105   2018.3

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  • HIV阻害剤・腫瘍認識プローブとしてのケモカイン受容体リガンド Invited

    野村 渉, 田中智博, 玉村啓和

    ペプチド医薬の最前線,(株)シーエムシー出版   101 - 107   2012.12

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  • Corrigendum: A Synthetic C34 Trimer of HIV-1 gp41 Shows Significant Increase in Inhibition Potency

    Wataru Nomura, Chie Hashimoto, Aki Ohya, Kosuke Miyauchi, Emiko Urano, Tomohiro Tanaka, Tetsuo Narumi, Toru Nakahara, Jun A. Komano, Naoki Yamamoto, Hirokazu Tamamura

    ChemMedChem   7   546 - 546   2012.4

  • Development of Designed Bivalent Ligands for CXCR4 and Their Function on Receptor Binding

    NOMURA Wataru, TANAKA Tomohiro, AOKI Toru, SOHMA Akira, AIKAWA Haruo, NARUMI Tetsuo, TAMAMURA Hirokazu

    2011   79 - 80   2012.3

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  • 最新ペプチド合成技術とその創薬研究への応用. Invited

    野村 渉, 田中智博, 相川春夫, 玉村啓和

    多価結合型GPCRリガンドの合成とがん細胞イメージングへの応用(株式会社 メディカルドゥ   267 - 273   2012

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  • フッ化物イオン応答型アミノ酸の開発と標的タンパク質精製ツールへの応用

    山本純, 田中智博, 傳田将也, 戎野紘司, 重永章, 野村渉, 玉村啓和, 大高章

    日本薬学会年会要旨集   132nd ( 2 )   2012

  • 長さの調節が可能な二価結合型CXCR4リガンドの創製・蛍光ラベル化と応用

    相川春夫, 野村渉, 鳴海哲夫, 田中智博, 玉村啓和

    日本化学会講演予稿集   92nd ( 3 )   2012

  • ジピコリルアミンおよびアザマクロサイクル環を有する二核亜鉛錯体型CXCR4アンタゴニストの構造活性相関研究

    紺野誠, 野村渉, 鳴海哲夫, 相川春夫, 玉村啓和, 田中智博, 橋本知恵, 大橋南美, 尾崎太郎, 相馬晃, 糸谷恭子, 村上努, 山本直樹

    日本化学会講演予稿集   92nd ( 4 )   2012

  • 標的タンパク質の効率的濃縮と同定を指向したトレーサブルリンカーの開発

    山本純, 前田奈美, 田中智博, 傳田将也, 重永章, 野村渉, 玉村啓和, 大高章

    日本薬学会年会要旨集   131st ( 2 )   2011

  • CXCR4二量化状態解析のための2価結合型リガンドの合成

    相馬晃, 野村渉, 田中智博, 鳴海哲夫, 相川春夫, 玉村啓和

    日本薬学会関東支部大会講演要旨集   55th   2011

  • 蛍光ラベル化した二価結合型CXCR4リガンドの創製と応用

    相川春夫, 野村渉, 鳴海哲夫, 田中智博, 玉村啓和

    反応と合成の進歩シンポジウム講演要旨集   37th   2011

  • HIV-gp41の三量体構造に特異的な中和抗体を誘導する人工抗原ペプチド

    野村渉, 相馬晃, 中原徹, 中原徹, 大庭賢二, 田中智博, 橋本知恵, 橋本知恵, 鳴海哲夫, 山本直樹, 玉村啓和, 玉村啓和

    日本薬学会関東支部大会講演要旨集   54th   2010

  • HIV侵入の動的超分子機構を模倣した立体構造特異的人工抗原分子の創製

    野村渉, 中原徹, 橋本知恵, 相馬晃, 田中智博, 鳴海哲夫, 玉村啓和, 大庭賢二, 山本直樹

    反応と合成の進歩シンポジウム講演要旨集   36th   2010

  • HIV-1コレセプターCXCR4を基にした人工設計型抗原分子の開発

    橋本知恵, 橋本知恵, 堤浩, 田中智博, 中原徹, 中原徹, 野村渉, 大庭賢二, 村上努, 山本直樹, 玉村啓和, 玉村啓和

    日本薬学会年会要旨集   129th ( 2 )   2009

  • HIV-1コレセプターCXCR4を基にした人工設計型抗原分子の開発

    橋本知恵, 橋本知恵, 野村渉, 田中智博, 中原徹, 中原徹, 鳴海哲夫, 大庭賢二, 村上努, 山本直樹, 玉村啓和, 玉村啓和

    日本薬理学会関東部会プログラム・要旨集   120th   2009

  • HIV-gp41の三量体構造に特異的な中和抗体を誘導する人工抗原ペプチド

    大矢亜紀, 中原徹, 中原徹, 野村渉, 大庭賢二, 田中智博, 橋本知恵, 橋本知恵, 鳴海哲夫, 村上努, 山本直樹, 玉村啓和, 玉村啓和

    メディシナルケミストリーシンポジウム講演要旨集   28th   2009

  • HIV-1第二受容体CXCR4を基にした合成抗原分子の開発

    橋本知恵, 橋本知恵, 野村渉, 田中智博, 鳴海哲夫, 大庭賢二, 山本直樹, 玉村啓和, 玉村啓和

    メディシナルケミストリーシンポジウム講演要旨集   28th   2009

  • CXCR4特異的蛍光プローブの開発と薬剤スクリーニングへの応用

    田中智博, 野村渉, 田部泰明, 田部泰明, 鳴海哲夫, 糸谷恭子, 大庭賢二, 山本直樹, 玉村啓和, 玉村啓和

    日本薬理学会関東部会プログラム・要旨集   120th   2009

  • 蛍光性CXCR4特異的リガンドの開発:スクリーニング及びイメージングへの展開

    田中智博, 野村渉, 田部泰章, 田部泰章, 堤浩, 糸谷恭子, 大庭賢二, 村上努, 山本直樹, 玉村啓和, 玉村啓和

    日本薬学会年会要旨集   129th ( 2 )   2009

  • 蛍光標識PKCおよび光制御型ケージドジアシルグリセロール誘導体の合成と機能評価

    大橋南美, 芹澤雄樹, 野村渉, 堤浩, 松本洋典, 奥田善章, 田中智博, 古田寿昭, 玉村啓和

    反応と合成の進歩シンポジウム講演要旨集   34th   190 - 191   2008.10

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  • 新規pharmacophoreを有するCXCR4アンタゴニストの構造活性相関研究

    TANAKA TOMOHIRO, TABE YASUAKI, OHASHI NAMI, HASEYAMA MASAKI, TSUTSUMI HIROSHI, NOMURA WATARU, ITOYA KYOKO, ESAKA AI, OISHI SHIN'YA, FUJII NOBUTAKA, WANG Z, PEIPER S C, EVANS B, TAMAMURA HIROKAZU

    日本薬学会年会要旨集   128th ( 2 )   84   2008.3

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  • 蛍光性アンタゴニストを用いたCXCR4のイメージングと阻害剤のスクリーニング法の確立

    田部泰章, 野村渉, 堤浩, 田中智博, 大庭賢二, 駒野淳, 山本直樹, 藤井信孝, 玉村啓和

    日本化学会講演予稿集   88th ( 2 )   2008

  • 標的タンパク質を特異的に蛍光検出する新規タグ‐プローブシステムの開発

    堤浩, 大橋南美, 田中智博, 田部泰章, 阿部清一朗, 蓑友明, 玉村啓和

    反応と合成の進歩シンポジウム講演要旨集   33rd   306 - 307   2007.10

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  • Stereoselective synthesis of peptidomimetics based on acid-catalyzed ring-opening of beta-aziridinyl-alpha, beta-enoates

    H. Tamamura, T. Tanaka, H. Tsutsumi, K. Nemoto, S. Mizokami, N. Ohashi

    BIOPOLYMERS   88 ( 4 )   580 - 580   2007

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  • Development of chemokine receptor CXCR4 antagonists using bio-mimetic strategy

    H. Tamamura, T. Tanaka, H. Tsutsumi, N. Ohashi, K. Hiramatsu, T. Araki, A. Ojida, I. Hamachi, Z. Wang, S. C. Pelper, J. O. Trent, S. Ueda, S. Oishi, N. Fujii

    BIOPOLYMERS   88 ( 4 )   577 - 577   2007

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Presentations

  • Development of Novel Carrier Molecules Based on CADY Peptide for Boron Neutron Capture Therapy

    Shiori Nakajo, Masashi Ueda, Hiroki Ueda, Minoru Suzuki, Tomohiro Tanaka

    28th Korean Peptide Protein Society (KPPS) Symposium  2025.6.24 

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    Event date: 2025.6.23 - 2025.6.25

    Presentation type:Poster presentation  

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  • ホウ素中性子捕捉療法のためのカチオン性 キャリア分子の創出 Invited

    田中智博

    2024年日本化学会中国四国支部大会 岡山大会  2024.11.16 

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    Event date: 2024.11.16 - 2024.11.17

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  • 静電的相互作用を利用したBSHキャリア分子の創製研究 Invited

    田中智博

    第20回日本中性子捕捉療法学会学術大会  2024.7.26 

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    Event date: 2024.7.26 - 2024.7.27

    Presentation type:Oral presentation (invited, special)  

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  • BSHの細胞内送達のための新規CADY誘導体の合成と評価

    中上栞里, 上田真史, 田中智博, 上田大貴, 鈴木実

    第20回日本中性子捕捉療法学会学術大会  2024.7.26 

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    Event date: 2024.7.26 - 2024.7.27

    Presentation type:Poster presentation  

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  • ホウ素中性子線捕捉療法に資するナノ粒子型10B薬剤の開発

    田中 智博, 上田 大貴, 鈴木 実, 櫻井 良憲, 上田 真史, 青木 伸

    第62回日本薬学会・日本薬剤師会・日本病院薬剤師会 中国四国支部学術大会  2023.10.29 

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    Event date: 2023.10.28 - 2023.10.29

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  • 大環状ポリアミン型のホウ素中性子捕捉療法(BNCT)用含ホウ素薬剤の設計と合成

    青木伸, 上田大貴, 田中智博, 鈴木実, 櫻井良憲

    第39回メディシナルケミストリーシンポジウム  2022.11.23 

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    Event date: 2022.11.23 - 2022.11.25

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  • Design and Synthesis of Boron-Containing Macrocyclic Polyamines as Boron Neutron Capture Therapy (BNCT) Agents Invited

    International Congress on Pure & Applied Chemistry Kona Kitabalu  2022.11.25 

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    Event date: 2022.11.22 - 2022.11.27

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  • ホウ素中性子捕捉療法のためのDNA標的型ホウ素薬剤の開発

    上田大貴, 鈴木実, 櫻井良憲, 田中智博, 青木伸

    第18回日本中性子捕捉療法学会学術大会  2022.10.18 

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    Event date: 2022.10.17 - 2022.10.18

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Awards

  • 奨励賞

    2024.11   日本薬学会中四国支部   がんの診断および治療に資する機能性分子の創製研究

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Research Projects

  • グルコース輸送体を標的とするBNCT用ホウ素クラスターキャリア分子の創製

    Grant number:20K05755  2020.04 - 2023.03

    日本学術振興会  科学研究費助成事業  基盤研究(C)

    田中 智博

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    Grant amount:\4420000 ( Direct expense: \3400000 、 Indirect expense:\1020000 )

    本研究課題の主要な目的はホウ素中性子線補足療法に用いられるホウ素クラスターであるBSH(Sodium Borocaptate)を効率的にがん細胞内に取り込ませるための手法の確立にある。昨年度、我々は細胞内に効率的に取り込ませるための補助剤としてポリエチレンイミンやポリリジンなどのカチオン性ポリマーが有効である事を見出した。種々の検討の結果、カチオン性ポリマーがアニオン性分子であるBSHと静電的相互作用を介してナノ粒子を形成し、がん細胞内への移行を促進していると考えられた。しかしながら、その細胞内取り込み機構については以前不明であったため、本年度はA549細胞やHela-S3細胞を用いてその機構についての解析を行った。具体的には、ナノ粒子の主要な取り込み経路として知られるエンドサイトーシスに着目し、種々のエンドサイトーシス阻害剤を用いた取り込み阻害実験を行った。
    その結果、メチル-β-シクロデキストリンやdynasoreにより前処理した細胞ではナノ粒子の取り込み量の低下が見られたため、ナノ粒子はカベオラ依存性エンドサイトーシス及びクラスリン依存性エンドサイトーシスによって取り込まれることが明らかとなった。一方で、これらの阻害剤の存在下においてもBSH単独よりも高い細胞内取り込み量を示したため、ナノ粒子の取り込みには複数の経路が関与していることが示唆された。そのため、蛍光基修飾されたカチオン性ポリマーを用いて解析を行ったが、現在のところ有益な結果は得られていない。

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  • Development of signal amplification probes for detection of Copper (II) ions Using 11B NMR/MRI

    Grant number:16K18915  2016.04 - 2018.03

    Japan Society for the Promotion of Science  Grants-in-Aid for Scientific Research  Grant-in-Aid for Young Scientists (B)

    Tanaka Tomohiro

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    Grant amount:\2730000 ( Direct expense: \2100000 、 Indirect expense:\630000 )

    Biorelevant metals have been known to play an important role for bio-organism. Specifically, Cu2+ ion is closely correlated with certain types of physiological and pathological events. Therefore, the development of a noninvasive methodology for detecting Cu2+ is important for understanding its biological role and relationship with disease. Herein, we report on the development of a Cu2+‐specific 11B NMR/MRI probe. The method is based on the rapid complete deboronation reaction of nido-o-carborane containing a chelator unit by Cu2+ under physiological conditions.

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  • Design and Synthesis of Helical Moving Rotaxane Molecules Having Chiral Axis

    Grant number:25893259  2013.08 - 2015.03

    Japan Society for the Promotion of Science  Grants-in-Aid for Scientific Research  Grant-in-Aid for Research Activity Start-up

    TANAKA tomohiro

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    Grant amount:\2730000 ( Direct expense: \2100000 、 Indirect expense:\630000 )

    In organism, various biomolecules was intricately interacted as machines and expressed its functions. A rotaxane is a mechanically-interlocked molecular architecture consisting of a dumbbell shaped molecule, which is threaded through a macrocycle. A series of rotaxanes, whose ring can be moved by external stimuli are called molecular shuttles, are attracting growing attention as basic structures of molecular machines. To date, most of the reported molecular machines function in organic solvents, and there are few example of water soluble molecular shuttle. Our interest is to design and synthesize bimolecular mimicry molecular shuttles.
    In this work, we successfully synthesized a rotaxane that consists an axis having an azobenzen unit and Zn2+-cyclen station, and the a-CyD ring. NMR, UV-VIS, and CD experiments of this rotaxane and its derivatives having some functionalities on the ring such as kinase substrate and thiol.

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