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RIKEN Center for Biosystems Dynamics Research Drug Discovery Structural Biology Platform Unit

Unit Leader: Mikako Shirouzu (Ph.D.)

Research Summary

Mikako  Shirouzu(Ph.D.)

RIKEN Program for Drug Discovery and Medical Technology (DMP) is developing new candidate drugs and technologies for drug discovery and medical treatment. As part of the activities, our unit carries out protein sample preparation, evaluation of candidate compounds in vitro and in a cell-based manner, and structural analysis of their complexes to improve monoclonal antibody drugs, vaccines, and candidate small molecular drugs. Our activities as experts of protein science and cell biology are indispensable for the rational drug development promoted by DMP.

Main Research Fields

  • Biological Sciences

Related Research Fields

  • Medicine, Dentistry & Pharmacy


  • Antigen preparation
  • Protein preparation
  • X-ray crystallography
  • In vitro compound evaluation
  • Cell-based compound evaluation

Selected Publications

  • 1.Koda, Y., Kikuzato, K., Mikuni, J., Tanaka, A., Yuki, H., Honma, T., Tomabechi, Y., Kukimoto-Niino, M., Shirouzu, M., Shirai, F. and Koyama, H.:
    “Identification of pyrrolo[2,3-d]pyrimidines as potent HCK and FLT3-ITD dual inhibitors”
    Bioorganic & Medicinal Chemistry Letters 27(22), 4944-4998. (2017).
  • 2.Shoji, S, Hanada, K., Ohsawa, N. and Shirouzu, M.:
    “Central catalytic domain of BRAP (RNF52) recognizes the types of ubiquitin chains and utilizes oligo-ubiquitin for ubiquitylation”
    Biochemical Journal 474(18), 3207-3226. (2017)
  • 3.Yuki, H, Kikuzato, K., Koda, Y., Mikuni, J., Tomabechi, Y., Kukizato-Niino, M., Tanaka, A., Shirai, F., Shirouzu, M., Koyama, H. and Honma, T.:
    “Activity cliff for 7-substituted pyrrolo-pyrimidine inhibitors of HCK explained in terms of predicted basicity of the amine nitrogen”
    Bioorganic & Medicinal Chemistry 25(16), 4259-4264. (2017).
  • 4.Amano, Y., Kikuchi, M., Sato, S., Yokoyama, S., Umehara, T., Umezawa, N. and Higuchi, T.:
    “Development and crystallographic evaluation of histone H3 peptide with N-terminal serine substitution as a potent inhibitor of lysine-specific demethylase 1”
    Bioorganic & Medicinal Chemistry 25(9), 2617-2624. (2017).
  • 5.Takemoto, Y., Ito, A., Niwa, H., Okumura, M., Fujiwara, T., Hirano, T., Handa, N., Umehara, T., Sonoda, T., Ogawa K., Tariq, M., Nishino, N., Dan, S., Kagechika, H., Yamori, T., Yokoyama, S. and Yoshida, M.:
    “Identification of Cyproheptadine as an Inhibitor of SET Domain Containing Lysine Methyltransferase 7/9 (Set7/9) That Regulates Estrogen-Dependent Transcription.”
    Journal of Medicinal Chemistry 59(8), 3650-3660. (2016).

Related Links

Lab Members

Principal investigator

Mikako Shirouzu
Unit Leader

Contact Information

C316 3F Central Research Building,
1-7-22 Suehiro-cho, Tsurumi-ku,
Yokohama, Kanagawa
230-0045, Japan
Tel: +81-(0)45-503-9202
Fax: +81-(0)45-503-9264

Email: mikako.shirouzu [at] riken.jp