Centers & Labs

RIKEN Center for Life Science Technologies

Drug Discovery Chemistry Platform Unit

Unit Leader: Hiroo Koyama (Ph.D.)
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 Field


Related Research Fields

Medicine, dentistry, and pharmacy

Research Subjects

  • Small molecule drug discovery through medicinal chemistry

Selected Publications

Papers with an asterisk(*) are based on research conducted outside of RIKEN.
  1. * Koyama, H.; Miller, D. J.; Boueres, J. K.;
    (2R)-2-Ethylchromane-2-carboxylic Acids: Discovery of Novel PPARα/γ Dual Agonists as Antihyperglycemic and Antihyperlipidemic Agents
    J. Med. Chem. 2004, 47, 3255-3263
  2. * Koyama, H.; Boueres, J. K.; Han, W.;
    5-Aryl thiazolidine-2, 4-dione as Selective PPARγ Agonists
    Bioorg. Med. Chem. Lett. 2003, 13, 1801-1803
  3. * Koyama, H.; Boueres, J. K.; Miller, D. J.;
    "(2R)-2-Methylchromane-2-carboxylic Acids: Discovery of Selective PPARαAgonists as Hypolipidemic Agents
    Bioorg. Med. Chem. Lett. 2005, 15(14), 3347-3351

Lab Members

Principal Investigator

Hiroo Koyama
Unit Leader

Core Members

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