top > Div. of Biomolecular Chemistry  > Dept. of Organic and 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. Kagechika Prof
T. Hirano Assoc Prof
S. Mori Assist Prof
Y. Yuasa Assist Prof

Research Theme

  1. Medicinal Chemistry of Retinoid
    Retinoids are specific modulators of cell proliferation, differentiation, and morphogenesis in vertebrates. The pleiotropic activities of retinoids are mediated by binding to and activating two classes of nuclear receptors, RARs and RXRs. We are developing novel synthetic RAR and RXR agonists/antagonists. Among them, an RAR agonist, Am80 (tamibarotene) was approved as a drug for relapsed acute promyelocytic leukemia (APL) in Japan (2005).
  2. Medicinal Chemistry of Nuclear Receptors
    Nuclear receptors are ligand-inducible transcription factors that regulate the expression of their target genes. Nuclear receptors have become one of the most significant molecular targets for drug discovery in the fields of cancer, metabolic syndrome, autoimmune diseases, and so on. We are developing novel synthetic ligands for various nuclear receptors, including nuclear orphan receptors whose specific ligands are unknown.
  3. Development of Novel Functional Fluorescent Molecules for Elucidation of Intracellular Signal Transduction Pathways
    Functional fluorescent molecules are useful in many fields of scientific research, including analytical chemistry or cell biology. We are developing novel fluoresecent molecules, whose fluorescence properties can be changed by binding to or reacting with ions, small molecules, or enzymes, enable us to estimate the concentration or activity of the targets.
  4. Aromatic Architecture Based on the Steric Properties of N-Methylated Amides
    The amide bond often plays a key role in functions such as molecular recognition maps or biological activities. We found that most secondary amides, such as acetanilide and benzanilide, exist in the trans structure, while the corresponding N-methylated compounds exist in cis form in the crystals and predominantly in cis form in various solvents. We are developing armatic amides and related molecules with unique structures or conformational behaviors, and applying themin thefield of medicinal chemistry and materials science.


  1. Yokoo, H.; Ohsaki, A.; Kagechika, H.; Hirano, T. Unique properties of 1, 5-naphthyridin-2(1H)-one derivatives as environmental-polarity-sensitive fluorescent dyes. Eur. J. Org. Chem. 2018, 679-687 .
  2. Mori, S.; Hirano T.; Takaguchi, A.; Fujiwara, T.; Okazaki, Y.; Kagechika, H. Selective Reagent for Detection of N-ε-Monomethylation of a Peptide Lysine Residue through SNAr Reaction. Eur. J. Org. Chem. 2017, 3606-3611 .
  3. Ishigami-Yuasa, M.; Watanabe, Y.; Mori, T.; Masuno, H.; Fujii, S.; Kikuchi, E.; Uchida, S.; Kagechika,H. Development of WNK signaling inhibitors as a new class of antihypertensive drugs. Bioorg. Med. Chem. 2017, 25, 3845-3852 .
  4. Yoshizaki, Y.; Mori, T.; Ishigami-Yuasa, M.; Kikuchi, E.; Takahashi, D.; Zeniya, M.; Nomura, N.; Mori, Y.; Araki, Y.; Ando, F.; Mandai, S.; Kasagi, Y.; Arai, Y.; Sasaki, E.; Yoshida, S.; Kagechika, H.; Rai, T.; Uchida, S.; Sohara, E. Drug-Repositioning Screening for Keap1-Nrf2 Binding Inhibitors using Fluorescence Correlation Spectroscopy. Sci. Rep. 2017, 7, 3945 .
  5. Perri, M.; Caroleo, Nannan M. C.; Gallelli, L. L.; De Sarro, G.; Kagechika, H.; Cione,E. 9-cis Retinoic acid modulates myotrophin expression and its miR in physiological and pathophysiological cell models. Exp. Cell Res. 2017, 354, 25-30 .
  6. Okamoto-Uchida, Y.; Yu, R.; Miyamura, N.; Arima, N.; Ishigami-Yuasa, M.; Kagechika, H.; Yoshida, S.; Hosoya, T.; Nawa, M.; Kasama, T.; Asaoka, Y.; Alois, R. W.; Elling, U.; Penninger, J. M.; Nishina, S.; Azuma, N.; Nishina, H. The mevalonate pathway regulates primitive streak formation via protein farnesylation. Sci. Rep. 2016, 6, 37697 .
  7. Hirano, T.; Noji, Y.; Shiraishi, T.; Ishigami-Yuasa, M.; Kagechika,H. Development of an "OFF-ON-OFF" fluorescent pH sensor suitable for the study of intracellular pH. Tetrahedron 2016, 72, 4925-4930 .
  8. Persaud, S. D.; Park, S. W.; Ishigami-Yuasa, M.; Koyano-Nakagawa, N.; Kagechika, H.; Wei, L.-N. All trans-retinoic acid analogs promote cancer cell apoptosis through non-genomic Crabp1 mediating ERK1/2 phosphorylation. Sci. Rep.,2016, 6, 22396 .
  9. Kikuchi, E.; Mori, T.; Zeniya, M.; Isobe, K.; Ishigami-Yuasa, M.; Fujii, S.; Kagechika, H.; Ishihara, T.; Mizushima, T.; Sasaki, S.; Sohara, E.; Rai, T.; Uchida, S. Discovery of Novel SPAK Inhibitors That Block WNK Kinase Signaling to Cation Chloride Transporters. J. Am. Soc. Nephrol. 2015, 26 (7), 1525-1536 .
  10. Fujii, S.; Shimizu, A.; Takeda, N.; Oguchi, K.; Katsurai, T.; Shirakawa, H.; Komai, M.; Kagechika, H. Systematic synthesis and anti-inflammatory activity of ω-carboxylated menaquinone derivatives - Investigations on identified and putative vitamin K2 metabolites - Bioorg. Med. Chem. 2015, 23, 2344-2352 .