top > Div. of Biomolecular Chemistry > Dept. of Medicinal Chemistry

  • Div. of Biomedical Materials
  • Div. of Biofunctional Restoration
  • Div. of Medical Devices
  • Div. of Biomolecular Chemistry
  • Medical and Dental Device Technology Incubation Center
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H. Tamamura Prof
K. Tsuji Assist Prof
T. Kobayakawa Assist Prof

Research Theme

  1. Development of peptidomimetics and drug discovery templates.
    Peptidomimetics for the development of peptide-lead drugs and drug-discovery templates for conformational restriction, which enable pharmacophores of bioactive compounds (ex. peptides) to be suitably disposed in three-dimensional space, are being developed. Drug discovery for the chemotherapy is being performed based on targeting several receptors, enzymes, etc.
  2. Development of HIV inhibitors and AIDS vaccines.
    Using peptide chemistry and medicinal chemistry approaches, HIV inhibitors and antigens for AIDS vaccine are being developed.
  3. Development of bioprobes and chemical biology.
    Development of bioprobes that specifically recognize each receptor or enzyme for research on chemical biology is going on.
  4. Development of applications of zinc finger protein for gene therapy and nano technology.
    Utilizing the DNA sequence-specific recognition of zinc finger proteins, technologies for DNA recombination, modifications, and DNA labeling are being developed.


  1. Wataru Nomura, Taisuke Koseki, Nami Ohashi, Takaaki Mizuguchi & Hirokazu Tamamura Trivalent Lignds for CXCR4 Bearing Polyproline Linkers Show Specific Recognition for Cells with Increased CXCR4 Expression. Org. Biomol. Chem., 13, 8734-8739 (2015)
  2. Takaaki Mizuguchi, Nami Ohashi, Wataru Nomura, Mao Komoriya, Chie Hashimoto, Naoki Yamamoto, Tsutomu Murakami & Hirokazu Tamamura Anti-HIV Screening for Cell-Penetrating Peptides Using Chloroquine and Identification of Anti-HIV Peptides Derived from Matrix Proteins. Bioorg. Med. Chem., 23(15),4423-4427 (2015)
  3. Wataru Nomura, Nami Ohashi, Atsumi Mori & Hirokazu Tamamura An In-cell Fluorogenic Tag-probe System for Protein Dynamics Imaging Enabled by Cell-Penetrating Peptides. Bioconjugate Chem., 26(6),1080-1085 (2015)
  4. Takuya Kobayakawa, Tetsuo Narumi & Hirokazu Tamamura Remote Stereoinduction in the Organocuprate-Mediated Allylic Alkylation of Allylic gem-Dichlorides: Highly Diastereoselective Synthesis of (Z)-Chloroalkene Dipeptide Isosteres. Org. Lett.,17(10),2302-2305(2015)
  1. Nami Ohashi, Wataru Nomura, Natsuki Minato & Hirokazu Tamamura Screening for Protein Kinase C Ligands Using Fluorescence Resonance Energy Transfer. Chem. Pharm. Bull.,62(10), 1019-1025 (2014)
  2. Maryna Masyuk, Aisha Abduelmula, Gabriela Morosan-Puopolo, Veysel Odemis, Rizwan Rehimi, Nargis Khalida, Faisal Yusuf, Jurgen Engele, Hirokazu Tamamura, Carsten Theiss & Beate Brand-Saberi Retrograde Migration of Pectoral Girdle Muscle Precursors Depends on CXCR4/SDF-1 Signaling. Histochem. Cell. Biol.,142(5), 473-488 (2014)
  3. Jun Yamamoto, Nami Maeda, Chiaki Komiya, Tomohiro Tanaka, Masaya Denda, Koji Ebisuno, Wataru Nomura, Hirokazu Tamamura, Youichi Sato, Aiko Yamauchi, Akira Shigenaga & Akira Otaka Development of a Fluoride-responsive Amide Bond Cleavage Device that is Potentially Applicable to a Traceable Linker. Tetrahedron, 70(34), 5122-5127 (2014)
  4. Hikaru Takano, Tetsuo Narumi, Nami Ohashi, Akinobu Suzuki, Toshiaki Furuta, Wataru Nomura & Hirokazu Tamamura Development of the 8-Aza-3-bromo-7-hydroxycoumarin-4-ylmethyl Group as a New Entry of Photolabile Protecting Groups. Tetrahedron, 70(29), 4400-4404 (2014)
  5. Jun Yamamoto, Masaya Denda, Nami Maeda, Miku Kita, Chiaki Komiya, Tomohiro Tanaka, Wataru Nomura, Hirokazu Tamamura, Youichi Sato, Aiko Yamauchi, Akira Shigenaga & Akira Otaka Development of a Traceable Linker Containing a Thiol-responsive Amino Acid for the Enrichment and Selective Labelling of Target Proteins. Org. Biomol. Chem., 12(23), 3821-3826 (2014)
  6. Tetsuo Narumi, Seiji Tsuzuki & Hirokazu Tamamura Imidazolium Salt-Catalyzed Friedel-Crafts-Type Conjugate Addition of Indoles: Analysis of Indole/Imidazolium Complex by High Level ab Initio Calculations. Asian J. Org. Chem., 3(4), 497-503 (2014)
  7. Tetsuo Narumi, Hikaru Takano, Nami Ohashi, Akinobu Suzuki, Toshiaki Furuta & Hirokazu Tamamura Isostere-Based Design of 8-Azacoumarin-Type Photolabile Protecting Groups: A Hydrophilicity Increasing Strategy for Coumarin-4-ylmethyls. Org. Lett., 16(4), 1184-1187 (2014)
Until 2013
  1. Chie Hashimoto, Tetsuo Narumi, Hiroyuki Otsuki, Yuki Hirota, Hiroshi Arai, Kazuhisa Yoshimura, Shigeyoshi Harada, Nami Ohashi, Wataru Nomura, Tomoyuki Miura, Tatsuhiko Igarashi, Shuzo Matsushita & Hirokazu Tamamura A CD4 Mimic as an HIV Entry Inhibitor: Pharmacokinetics. Bioorg. Med. Chem., 21(24), 7884-7889 (2013)
  2. Chie Hashimoto, Wataru Nomura, Tetsuo Narumi, Masayuki Fujino, Toru Nakahara, Naoki Yamamoto, Tsutomu Murakami & Hirokazu Tamamura CXCR4-derived Synthetic Peptides Inducing Anti-HIV-1 Antibodies. Bioorg. Med. Chem., 21(22), 6878-6885 (2013)
  3. Hiroyuki Otsuki, Takayuki Hishiki, Tomoyuki Miura, Chie Hashimoto, Tetsuo Narumi, Hirokazu Tamamura, Kazuhisa Yoshimura, Shuzo Matsushita & Tatsuhiko Igarashi Generation of a Replication-competent Simian-human Immunodeficiency Virus, the Neutralisation Sensitivity of Which can be Enhanced in the Presence of a Small Molecule CD4 Mimic. J. Gen.Virol., 94(12), 2710-2716 (2013)
  4. Chie Hashimoto, Wataru Nomura, Tetsuo Narumi, Masayuki Fujino, Hiroshi Tsutsumi, Masaki Haseyama, Naoki Yamamoto, Tsutomu Murakami & Hirokazu Tamamura Anti-HIV-1 Peptide Derivatives Based on the HIV-1 Co-receptor CXCR4. ChemMedChem, 8(10), 1668-1672 (2013)
  5. Wataru Nomura, Haruo Aikawa, Nami Ohashi, Emiko Urano, Mathieu Metifiot, Masayuki Fujino, Kasthuraiah Maddali, Taro Ozaki, Ami Nozue, Tetsuo Narumi, Chie Hashimoto, Tomohiro Tanaka, Yves Pommier, Naoki Yamamoto, Jun Komano, Tsutomu Murakami & Hirokazu Tamamura Cell-Permeable Stapled Peptides Based on HIV-1 Integrase Inhibitors Derived from HIV-1 Gene Products. ACS Chem. Biol., 8(10), 2235-2244 (2013)
  6. Wataru Nomura, Chie Hashimoto, Takaharu Suzuki, Nami Ohashi, Masayuki Fujino, Tsutomu Murakami, Naoki Yamamoto & Hirokazu Tamamura Multimerized CHR-derived Peptides as HIV-1 Fusion Inhibitors. Bioorg. Med. Chem., 21(15), 4452-4458 (2013)
  7. Tetsuo Narumi, Hiroshi Arai, Kazuhisa Yoshimura, Shigeyoshi Harada, Yuki Hirota, Nami Ohashi, Chie Hashimoto, Wataru Nomura, Shuzo Matsushita & Hirokazu Tamamura CD4 Mimics as HIV Entry Inhibitors: Lead Optimization Studies of the Aromatic Substituents. Bioorg. Med. Chem., 21(9), 2518?2526 (2013)
  8. Tetsuo Narumi, Haruo Aikawa, Tomohiro Tanaka, Chie Hashimoto, Nami Ohashi, Wataru Nomura, Takuya Kobayakawa, Hikaru Takano, Yuki Hirota, Tsutomu Murakami, Naoki Yamamoto & Hirokazu Tamamura Low Molecular Weight CXCR4 Ligands with Variable Spacers. ChemMedChem, 8(1), 118-124 (2013)
  9. Tetsuo Narumi, Takuya Kobayakawa, Haruo Aikawa, Shunsuke Seike & Hirokazu Tamamura Stereoselective Formation ofTrisubstituted (Z)-Chloroalkenes Adjacent to a Tertiary Carbon Stereogenic Center by Organocuprate-Mediated Reduction/Alkylation. Org. Lett., 14(17), 4490-4493 (2012)
  10. Tetsuo Narumi, Tomohiro Tanaka, Chie Hashimoto, Wataru Nomura, Haruo Aikawa, Akira Sohma, Kyoko Itotani, Miyako Kawamata, Tsutomu Murakami, Naoki Yamamoto & Hirokazu Tamamura Pharmacophore-based Small Molecule CXCR4 Ligands. Bioorg. Med. Chem. Lett., 22(12), 4169-4172 (2012)
  11. Chie Hashimoto, Wataru Nomura, Aki Ohya, Emiko Urano, Kosuke Miyauchi, Tetsuo Narumi, Haruo Aikawa, Jun A. Komano, Naoki Yamamoto & Hirokazu Tamamura Evaluation of a Synthetic C34 Trimer of HIV-1 gp41 as AIDS Vaccines. Bioorg. Med. Chem., 20(10), 3287?3291 (2012)
  12. Wataru Nomura, Akemi Masuda, Kenji Ohba, Arisa Urabe, Nobutoshi Ito, Akihide Ryo, Naoki Yamamoto & Hirokazu Tamamura Effects of DNA Binding of Zinc Finger and Linkers for Domain Fusion on Catalytic Activity of Sequence-Specific Chimeric Recombinases Determined by a Facile Fluorescent System. Biochemistry, 51(7), 1510?1517 (2012)
  13. Tetsuo Narumi, Mao Komoriya, Chie Hashimoto, Honggui Wu, Wataru Nomura, Shintaro Suzuki, Tomohiro Tanaka, Joe Chiba, Naoki Yamamoto, Tsutomu Murakami & Hirokazu Tamamura Conjugation of Cell-penetrating Peptides Leads to Identification of Anti-HIV Peptides from Matrix Proteins. Bioorg. Med. Chem., 20(4), 1468-1474 (2012)
  14. Wataru Nomura, Chie Hashimoto, Aki Ohya, Kosuke Miyauchi, Emiko Urano, Tomohiro Tanaka, Tetsuo Narumi, Toru Nakahara, Jun A. Komano, Naoki Yamamoto & Hirokazu Tamamura Synthetic C34 Trimer of HIV-1 gp41 Shows Significant Increase of Inhibition Potency. ChemMedChem, 7(2), 205?208 and 546 (2012)
  15. Tetsuo Narumi, Hiroshi Arai, Kazuhisa Yoshimura, Shigeyoshi Harada, Wataru Nomura, Shuzo Matsushita & Hirokazu Tamamura Small Molecular CD4 Mimics as HIV Entry Inhibitors. Bioorg. Med. Chem., 19(22), 6735?6742 (2011)
  16. Wataru Nomura, Nami Ohashi, Yoshiaki Okuda, Tetsuo Narumi, Teikichi Ikura, Nobutoshi Ito & Hirokazu Tamamura Fluorescence-Quenching Screening of Protein Kinase C Ligands with an Environmentally Sensitive Fluorophore. Bioconjugate Chem., 22(5), 923-930 (2011)
  17. Tomohiro Tanaka, Tetsuo Narumi, Taro Ozaki, Akira Sohma, Nami Ohashi, Chie Hashimoto, Kyoko Itotani, Wataru Nomura, Tsutomu Murakami, Naoki Yamamoto & Hirokazu Tamamura Azamacrocyclic-metal Complexes as CXCR4 Antagonists. ChemMedChem, 6(5), 834?839 (2011)
  18. Hiroshi Tsutsumi, Seiichiro Abe, Tomoaki Mino, Wataru Nomura & Hirokazu Tamamura Intense Blue Fluorescence in a Leucine Zipper Assembly. ChemBioChem, 12(5), 691?694 (2011)
  19. Nami Ohashi, Wataru Nomura, Tetsuo Narumi, Nancy E. Lewin, Kyoko Itotani, Peter M. Blumberg & Hirokazu Tamamura Fluorescent-responsive Synthetic C1b Domains of Protein Kinase Cδ as Reporters of Specific High Affinity Ligand Binding. Bioconjugate Chem., 22(1), 82?87 (2011)
  20. Wataru Nomura, Tetsuo Narumi, Nami Ohashi, Yuki Serizawa, Nancy E. Lewin, Peter M. Blumberg, Toshiaki Furuta & Hirokazu Tamamura Synthetic Caged DAG-lactones for Photochemically-controlled Activation of Protein Kinase C. ChemBioChem, 12(4), 535?539 (2011)
  21. Tomohiro Tanaka, Wataru Nomura, Tetsuo Narumi, Akemi Masuda & Hirokazu Tamamura Bivalent Ligands of CXCR4 with Rigid Linkers for Elucidation of Dimerization State in Cells. J. Am. Chem. Soc. (Commun.), 132(45), 15899?15901 (2010)
  22. Hiroshi Tsutsumi, Wataru Nomura, Seiichiro Abe, Tomoaki Mino, Akemi Masuda, Nami Ohashi, Tomohiro Tanaka, Kenji Ohba, Naoki Yamamoto, Kazunari Akiyoshi & Hirokazu Tamamura Fluorogenically Active Leucine Zipper Peptides as New Tag-Probe Pairs for Protein Imaging in Living Cells. Angew. Chem., Int. Ed., 48(48), 9164-9166 (2009)