RIKEN Center for Sustainable Resource Science Drug Discovery Chemistry Platform Unit
Unit Leader: Hiroo Koyama (Ph.D.)
Research Summary
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
Keywords
- Drug discovery
- Medicinal chemistry
- Pharmacokinetics optimization
Selected Publications
- 1.Koda, Y.; Kikuzato, K.; Mikuni, J.; Tanaka, A.; Yuki, H.; Honma, T.; Tomabechi, Y.; Kukimoto-Niino, M.; Shirouzu, M.; Shirai,F.; Koyama, H.:
“Identification of pyrrolo[2,3-d]pyrimidines as potent HCK and FLT3-ITD dual inhibitors”
Bioorg. Med. Chem. 2017, 27, 4994-4998. - 2.Yuki, H.; Kikuzato, K.; Koda, H.; Mikuni, J.; Tomabechi, Y.; Kukimoto-Niino, M.; Tanaka, A.; Shirai, F.; Shirouzu, M.; Koyama, H.; Honma, T.:
“Activity cliff for 7-substituted pyrrolo-pyrimidine inhibitors of HCK explained in terms of predicted basicity of the amine nitrogen”
Bioorg. Med. Chem. 2017, 25, 4259-4264. - 3.Saito,Y.; Yuki, H.; Kuratani, M.; Hashizume, Y.; Takagi, S.; Honma, T.; Tanaka, A.; Shirouzu, M.; Mikuni, M.; Handa, N,; Ogahara, I.; Sone, A.; Najima, Y,; Tomabechi, Y.; Wakiyama, M.; Uchida, N,; Tomizawa-Murasawa, M.; Kaneko, A.; Tanaka, S.; Suzuki, N.; Kajita, H.; Aoki, Y.; Ohara, O.; Shultz, Leonard D.; Fukami, T.; Goto, T.; Taniguchi, S.; Yokoyama, S.; Ishikawa, F.:
“A Pyrrolo-Pyrimidine Derivative Targets Human Primary AML Stem Cells in Vivo”
Sci. Transl.Med. 2013, 5, 181ra52. - 4.Tashiro, T.; Nakagawa, R.; Shigeura, T.; Watarai, H.; Taniguchi, M.; Mori, K.:
“RCAI-61 and related 6-modified analogs of KRN7000: their synthesis and bioactivity for mouse lymphocytes to produce interferon- in vivo”
Bioorg. Med. Chem. 2013, 21, 3066-3079. - 5.Shiozaki, M.; Tashiro, T.; Koshino, H.; Shigeura, T.; Watarai, H.; Taniguchi, M.; Mori, K.:
“Synthesis and biological activity of hydroxylated analogs of RCAI-80”
Tetrahedron 2013, 69, 9710-9725. - 6.Tashiro, T,; Shigeura, T.; Shiozaki, M.; Watarai, H.; Taniguchi, M.; Mori, K.:
“RCAI-133, an N-methylated analogue of KRN7000, activates mouse natural killer T cells to produce Th2-biased cytokines”
MedChemComm 2013, 4, 949-955. - 7.Shiozaki,, M.; Tashiro, T.; Koshino, H.; Shigeura, T.; Watarai, H.; Taniguchi, M.; Mori, K.:
“Synthesis and biological activity of hydroxylated analogues of KRN7000 (-galactosylceramide)”
Carbohydr. Res., 2013, 370, 46–66.
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
- Kenichi Washizuka
- Research Scientist
- Hirofumi Yamamoto
- Research Scientist
- Ko Kikuzato
- Technical Scientist
- Rie Osaki
- Technical Staff I
- Takuya Tashiro
- Visiting Scientist
- Fumiko Kyotani
- Part-time Worker
- Chieko Shida
- Assistant
Contact Information
Main Research Building room 628
2-1 Hirosawa
Wako, Saitama
351-0198 Japan
Email: hiroo.koyama [at] riken.jp