Centers & Labs

RIKEN Center for Life Science Technologies

Chemical Biology Team

Director: Takamitsu Hosoya (Ph.D.)
Takamitsu  Hosoya(Ph.D.)

In order to achieve the promotion of human live science and drug discovery, it is necessary to develop new methods and tools realized by the innovative chemistries. Through the researches under collaboration with a number of scientists of different disciplines, we are looking to face with significant challenges including development of useful PET probes for in vivo imaging of target molecules, nobel strategies for efficient PET probe synthesis, chemical tools and methods that facilitate chemical biology researches, and development of efficient synthetic methods of valuable compounds.

Main Research Field


Related Research Fields

Medicine, dentistry, and pharmacy

Research Subjects

  • Development of world’s first strategies for efficient PET probe synthesis
  • Development of practical PET probes specific for target molecules
  • Development of sequence specific chemical modification methods for biomolecular probe synthesis
  • Development of novel synthetic methods of valuable compounds

Selected Publications

  1. Niwa, T., Ochiai, H., Watanabe, Y., and Hosoya, T.:
    "Ni/Cu-Catalyzed Defluoroborylation of Fluoroarenes for Diverse C–F Bond Functionalization"
    J. Am. Chem. Soc. 137 (45), 14313-8 (2015).
  2. Takahashi, K., Hosoya, T., Onoe, K., Doi, H., Nagata, H., Hiramatsu, T., Li, X. L., Watanabe, Y., Wada, Y., Takashima, T., Suzuki, M., Onoe, H., and Watanabe, Y.:
    "[11C]Cetrozole: an Improved C-[11C]Methylated PET Probe for Aromatase Imaging in the Brain."
    J. Nucl. Med. 55 (5), 852-7 (2014).
  3. Suzuki, M., Doi, H., Koyama, H., Zhang, Z., Hosoya, T., Onoe, H., and Watanabe, Y.:
    "Pd0-Mediated Rapid Cross-Coupling Reactions, the Rapid C-[11C]Methylations, Revolutionarily Advancing the Syntheses of Short-Lived PET Molecular Probes."
    Chem. Rec. 14 (3), 516-41 (2014).
  4. Miyajima, M., Kusuhara, H., Takahashi, K., Takashima, T., Hosoya, T., Watanabe, Y., and Sugiyama, Y.:
    "Investigation of the effect of active efflux at the blood-brain barrier on the distribution of nonsteroidal aromatase inhibitors in the central nervous system."
    J. Pharm. Sci. 102 (9), 3309-19 (2013).
  5. Koyama, H., Zhang, Z., Ijuin, R., Siqin, Son, J., Hatta, Y., Ohta, M., Wakao, M., Hosoya, T., Doi H., and Suzuki, M.:
    "Pd0-mediated rapid coupling of methyl iodide with excess amounts of benzyl- and cinnamylboronic acid esters: efficient method for incorporation of positron-emitting 11C radionuclide into organic frameworks by coupling between two sp3-hybridized carbons"
    RSC Adv. 3 (24), 9391-401 (2013).
  6. Ozawa, M., Takahashi, K., Akazawa, K. H., Takashima, T., Nagata, H., Doi, H., Hosoya, T., Wada, Y., Cui, Y., Kataoka, Y., and Watanabe, Y.:
    "PET of aromatase in gastric parietal cells using 11C-vorozole."
    J. Nucl. Med. 52 (12), 1964-9 (2011).
  7. Takahashi, K., Onoe, K., Doi, H., Nagata, H., Yamagishi, G., Hosoya, T., Tamura, Y., Wada, Y., Yamanaka, H., Yokoyama, C., Mizuma, H., Takashima, T., Bergstro¨m, M., Onoe, H., La°ngstro¨m, B., and Watanabe, Y.:
    "Increase in hypothalamic aromatase in macaque monkeys treated with anabolic-androgenic steroids: PET study with [11C]vorozole."
    Neuroreport 22 (7), 326–30 (2011).
  8. Takahashi, K., Yamagishi, G., Hiramatsu, T., Hosoya, A., Onoe, K., Doi, H., Nagata, H., Wada, Y., Onoe, H., Watanabe, Y., and Hosoya, T.:
    "Practical synthesis of precursor of [N-methyl-11C]vorozole, an efficient PET tracer targeting aromatase in the brain."
    Bioorg. Med. Chem. 19 (4), 1464–70 (2011).
  9. Ikemoto, T., Hosoya, T., Takata, K., Aoyama, H., Hiramatsu, T., Onoe, H., Suzuki, M., and Endo, M.:
    "Functional role of NSP-like 1 protein in membrane translocation of glucose transporter 4."
    Diabetes 58 (12), 2802–12 (2009).
  10. Doi, H., Ban, I., Nonoyama, A., Sumi, K., Kuang, C., Hosoya, T., Tsukada, H., and Suzuki, M.:
    "Palladium(0)-Mediated Rapid Methylation and Fluoromethylation on Carbon Frameworks by Reacting Methyl and Fluoromethyl Iodide with Aryl and Alkenyl Boronic Acid Esters: Useful for the Synthesis of [11C]CH3-C and [18F]FCH2-C-Containing PET Tracers (PET = Positron Emission Tomography)."
    Chem. Eur. J. 15 (16), 4165–71 (2009).

Lab Members

Principal Investigator

Takamitsu Hosoya

Core Members

Takashi Niwa
Deputy Team Leader
Hiroo Koyama
Senior Scientist
Zhouen Zhang
Research Scientist
Yuto Sumida
Research Scientist
Hidenori Ochiai
Special Postdoctoral Researcher
Yuta Uetake
Postdoctoral Researcher
Motoyuki Isoda
Postdoctoral Researcher
Tomoe Sumida
Technical Staff I
Yasuko Kawai

Contact information

6-7-3 Minatojima-minamimachi, Chuo-ku
Kobe, Hyogo
650-0047, Japan

Email: takamitsu.hosoya [at]

Related links

Recent research results

May 19, 2017: RIKEN RESEARCH
Making stepping stones to drugs
March 18, 2016: RIKEN RESEARCH
Breaking bonds for probes and drugs