Drug Discovery Imaging Platform Unit

Unit Leader
Yasuyoshi WATANABE
(M.D., Ph.D.)
At the Drug Discovery Imaging Platform Unit, we are advancing in vivo pharmacokinetic research of marmosets (monkeys), mice and humans by utilizing molecular imaging technology focused on positron emission tomography (PET). Labeling technologies for molecular imaging probes guarantee in vivo observation time and improve tracing after metabolic breakdown. Also, with a view to clinical studies of microdoses, we aim to build new drug discovery processes, developing labeling and probes for drug candidate compounds, as well as utilizing mice-to-human streamlined molecular imaging techniques.
- Utilization of molecular imaging in drug development
- Development of molecular probes for evaluation of anti-dementia drug candidates
- Yashio, K., Katayama, Y., Takashima, T., Ishiguro, N., Doi, H., Suzuki, M., Wada, Y., Tamai, I., and Watanabe, Y.:
"Synthesis of [11C]uric acid, using [11C]phosgene, as a possible biomarker in PET imaging for diagnosis of gout."
Bioorg. Med. Chem. Lett., 22(1): 115-119, 2012. - Ozawa, M., Takahashi, K., Akazawa, K., Takashima, T., Nagata, H., Doi, H., Hosoya, T., Wada, Y., Cui, Y.L., Kataoka, Y., and Watanabe, Y.:
"Positron emission tomography imaging of aromatase in gastric parietal cells using [11C]Vorozole."
J. Nucl. Med., 52(12): 1964-1969, 2011. - Takashima, T., Hashizume, Y., Katayama, Y., Murai, M., Wada, Y., Maeda, K., Sugiyama, Y., and Watanabe, Y.:
"The involvement of organic anion transporting polypeptide in the hepatic uptake of telmisartan in rats: PET studies with 11C telmisartan."
Mol. Pharm., 8(5): 1789-1798, 2011. - Takashima, T., Yokoyama, C., Mizuma, H., Yamanaka, H., Wada, Y., Onoe, K., Nagata, H., Tazawa, S., Doi, H., Takahashi, K., Morita, M., Kanai, M., Shibasaki, M., Kusuhara, H., Sugiyama, Y., Onoe, H., and Watanabe, Y.:
"Developmental changes in P-glycoprotein function in the blood-brain barrier of non-human primates: PET study with R-[11C] verapamil and [11C] oseltamivir."
J. Nucl. Med., 52(6): 950-957, 2011. - 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-(11)C]vorozole, an efficient PET tracer targeting aromatase in the brain."
Bioorg. Med. Chem., 19(4): 1464-1470, 2011. - Yamashita, S., Takashima, T., Kataoka, M., Oh, H., Sakuma, S., Takahashi, M., Suzuki, N., Hayashinaka, E., Wada, Y., Cui, Y., and Watanabe, Y.:
"PET imaging of the gastrointestinal absorption of orally administered drugs in conscious and anesthetized rats."
J. Nucl. Med., 52(2): 249-56, 2011. - Kuboyama, T., Nakamura, M., Yoshino, M., Cui, Y.L., Sako, T., Wada, Y., Imanishi, T., Obika, S., Watanabe, Y., Suzuki, M., and Doi, H.:
"Stoichiometry-focused 18F-labeling of alkyne-substituted oligodeoxynucleotides using azido([18f]fluoromethyl)benzenes by Cu-catalyzed Huisgen reation."
Bioorg. Med. Chem., 19(1): 249-255, 2011 - Takashima, T., Nagata, H., Nakae, T., Cui, Y., Wada, Y., Kitamura, S., Doi, H., Suzuki, M., Maeda, K., Kusuhara, H., Sugiyama, Y., and Watanabe, Y.:
"PET studies using 15R-[11C]TIC-Me for the evaluation of hepatobiliary transport."
J. Pharmacol. Exp. Ther., 335(2): 314-323, 2010. - Tanaka, K., Minami, K., Tahara, T., Fujii, Y., Siwu, E.R., Nozaki, S., Onoe, H., Yokoi, S., Koyama, K., Watanabe, Y., and Fukase, K.:
"Electrocyclization-based labeling allows efficient in vivo imaging of cellular trafficking."
Chem. Med. Chem., 5(6): 841-845, 2010. - Takashima-Hirano, M., Shukuri, M., Takashima, T., Goto, M., Wada, Y., Watanabe, Y., Onoe, H., Doi, H., and Suzuki, M.:
"General Method for the (11)C-Labeling of 2-Arylpropionic Acids and Their Esters: Construction of a PET Tracer Library for a Study of Biological Events Involved in COXs Expression."
Chemistry, 16(14):4250-4258, 2010.
Principal Investigator
- Yasuyoshi WATANABE
- Unit Leader
Members
- Yasuhiro WADA
- Senior Scientist
- William Ewan HUME
- Senior Scientist
- Tadayuki TAKASHIMA
- Research Scientist
- Yasuko MATSUMOTO
- Research Scientist
- Keiji YASHIO
- Research Scientist
- Takashi OKAUCHI
- Research Associate