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RIKEN Center for Sustainable Resource Science Drug Discovery Chemistry Platform Unit

Unit Leader: Hiroo Koyama (Ph.D.)

Research Summary

Hiroo  Koyama(Ph.D.)

The main focus of our unit is to identify small molecule drug candidates suitable for animal safety studies and subsequent human clinical trials. Our dedicated scientists conduct lead compound generation, and multi-dimensional lead compound optimization on potency to target receptor/enzyme, PKPD profiles, and off-target activities through SAR development. By capitalizing on RIKEN's available expertise in X-ray crystal structure analysis, in-silico modeling studies, and HTS, we strive to expedite the drug discovery process by rational drug design. Our current therapeutic targets include rare genetic diseases and hard-to-treat cancers.

Main Research Fields

  • Chemistry

Related Research Fields

  • Medicine, Dentistry & Pharmacy


  • Drug discovery
  • Medicinal chemistry
  • Pharmacokinetics optimization

Selected Publications

  • 1. Shibata, N.; Cho, N.; Koyama, H.; Naito, N.
    "Development of a degrader against oncogenic fusion protein FGFR3-TACC3"
    Bioorg. Med. Chem. Lett., 60. 128584. (2022)
  • 2. Cho, N.; Kikuzato, K.; Futamura, Y.; Shimuzu, T.; Hayase, H.; Kamisaka, K.; Takaya, D.; Yuki, H.; Honma, T.; Niikura, M.; Kobayashi, F.; Watanabe, N.; Osada, H.; Koyama, H.
    "New antimalarials identified by a cell-based phenotypic approach: Structure-activity relationships of 2,3,4,9-tetrahydro-1H-b-carboline derivatives possessing 2-((coumarin-5-yl)oxy)alkanoyl moiety"
    Bioorg. Med. Chem., 66, 116830. (2022)
  • 3.Koda Y.; Sato S.; Yamamoto H.; Niwa H; Watanabe C.; Sato T; Watanabe H.; Nakamura K.; Tanaka A.; Shirouzu M.; Honma T.; Fukami T.; Koyama H.; Umehara T.
    "In silico design and synthesis of tranylcypromine-derived LSD1 inhibitors with improved hERG and microsomal stability profiles."
    ACS Med. Chem. Lett., 13, 848. (2022)
  • 4. Yamamoto, H.; Sakai, N.; Ohte, S.; Sato, T.; Sekimata, K.; Matsumoto, T.; Nakamura, K.; Watanabe, H.; Mishima-Tsumagari, C.; Takaka, A.; Hashizume, Y.; Honma, T.; Katagiri, T.; Miyazono, K.; Tomoda, H.; Shirouzu, M.; Koyama, H.
    "Novel bicyclic pyrazoles as potent ALK2 (R206H) inhibitors for the treatment of fibrodysplasia ossificans progressive"
    Bioorg. Med. Chem. Lett., 28, 127858. (2021)
  • 5. Nara, T.; Nakagawa, Y.; Tsuganezawa, K.; Yuki, H.; Sekimata, K.; Koyama, H.; Ogawa, N.; Honma, T.; Shirouzu, M.; Fukami, T.; Matsuo, Y.; Inaoka, D. K.; Kita, Y.; Tanaka, A.
    "The ubiquinone synthesis pathway is a promising drug target for Chagas disease"
    PLoS ONE, 16(2), e0243855. (2021)
  • 6.Sekimata, K.; Sato, T.; Sakai, N.
    "ALK2: A Therapeutic Target for Fibrodysplasia Ossificans Progressiva and Diffuse Intrinsic Pontine Glioma."
    Chem. Pharm. Bull., 68(3) 194-200. (2020)
  • 7. Shirai, F.; Mizutani, A.; Yashiroda, Y.; Tsumura, T.; Kano, Y.; Muramatsu, Y.; Chikada, T.; Yuki, H.; Niwa, H.; Sato, S.; Washizuka, K.; Koda, Y.; Mazaki, Y.; Jan, M-K.; Yoshida, H.; Nagamori, A.; Okue, M.; Watanabe, T.; Kitamura, K.; Shitara, E.; Honma, T.; Umehara, T.; Shirouzu, M.; Fukami, T.; Seimiya, H.; Yoshida, M.; Koyama, H.
    "Design and Discovery of an Orally Efficacious Spiroindolinone-based Tankyrase Inhibitor for the Treatment of Colon Cancer."
    J. Med. Chem., 63, 4183-4204. (2020)
  • 8.Sekimata, K.; Sato, T.; Sakai, N.; Watanabe, H.; Mishima-Tsumagari, C.; Taguri, T.; Matsumoto, T.; Fujii, Y.; Handa, N.; Honma, T.; Tanaka, A.; Shirouzu, M.; Yokoyama, S.; Miyazono, K.; Hashizume, Y.; Koyama, H.
    "Bis-Heteroaryl Pyrazoles: Identification of Orally Bioavailable Inhibitors of Activin Receptor-Like Kinase-2 (R206H)."
    Chem. Pharm. Bull., 67, 224–235. (2019)
  • 9. Shirai, F.; Tsumura, T.; Yashiroda, Y.; Yuki, H.; Niwa, H.; Sato, S.; Chikada, T.; Koda, Y.; Washizuka, K.; Yoshimoto, N.; Abe, M.; Onuki, T.; Mazaki, Y.; Hirama, C.; Fukami, T.; Watanabe, H.; Honma, T.; Umehara, T.; Shirouzu, M.; Okue, M.; Kano, Y.; Watanabe, T.; Kitamura, K.; Shitara, E.; Muramatsu, Y.; Yoshida, H.; Mizutani, A.; Seimiya, H.; Yoshida, M; Koyama, H.
    "Discovery of Novel Spiroindoline Derivatives as Selective Tankyrase Inhibitors."
    J. Med. Chem., 62(7), 3407-3427. (2019)
  • 10. Tsuganezawa, K.; Sekimata, K.; Nakagawa, Y.; Utata, R.; Nakamura, K.; Ogawa, N.; Koyama, H.; Shirouzu, M.; Fukami, T.; Kita, K.; Tanaka, A.
    "Identification of small molecule inhibitors of human COQ7."
    Bioog. Med. Chem. , https://doi.org/10.1016/j.bmc.2019.115182. (2019)

Related Links

Lab Members

Principal investigator

Hiroo Koyama
Unit Leader

Core members

Fumiyuki Shirai
Senior Research Scientist
Nobuo Cho
Senior Research Scientist
Junichi Kazami
Senior Technical Scientist
Katsuhiko Sekimata
Research Scientist
Yasuko Koda
Research Scientist
Hirokazu Kubota
Research Scientist
Hirofumi Yamamoto
Research Scientist
Ko Kikuzato
Senior Technical Staff
Rie Osaki
Technical Staff I
Takuya Tashiro
Visiting Scientist
Fumiko Kyotani
Research Part-time Worker II
Chieko Shida

Contact Information

Main Research Building room 628
2-1 Hirosawa
Wako, Saitama
351-0198 Japan

Email: hiroo.koyama [at] riken.jp