Molecular Imaging Medicinal Chemistry Laboratory
Team Leader
Masaaki SUZUKI (D.Sci.)
Our laboratory aims to develop novel methodologies in in vivo molecular science necessary to the promotion of exploratory studies for drug candidates, particularly focusing on imaging the dynamic behavior of designed compounds in vital systems using positron emission tomography (PET). Some of our specific research goals include (1) the development of rapid chemical reactions, particularly rapid C-methylations and fluoromethylations through carbon-carbon bond formations to incorporate short-lived 11C radio-nuclides into organic molecules to elaborate metabolically stable PET tracers in addition to the 18F incorporation. (2) Design and synthesis of specific molecular probes for targeting important biological phenomena and serious diseases. (3) The application of the rapid reactions to the synthesis of high-definition PET tracers and (4) efficient chemical synthesis of highly polished drugs candidates. (5) Extensive collaboration with an instrument company to accurize and micronize the synthetic apparatuses and enhance safety. The novel method of methylation offers a number of benefits. The C-11CH3 group is metabolically highly stable, thus the resulting image is very reliable. As well, the methyl group possesses the minimum carbon substituent and is non-polar, allowing high variation from the lead compound with minimal change in functions (bioactivities), permitting tracer design within a predictable range. The rapid C-[11C]methylation and C-[18F]fluoromethylation compensate each other correspondent with research purposes.
- Development of new rapid chemical reactions for the synthesis of high-definition PET tracers
- Design and synthesis of specific molecular probes for targeting important biological phenomena and serious diseases
- Development of new photoaffinity labeling methods and the detection of candidate target proteins
- Development of microreactor for the application of rapid C-[11C]methylation and C-[18F]fluoromethylation
- March 9,2010
- Labeling of antipyretic and analgesic drugs enables successful visualization inside the body
- R. Noyori and M. Suzuki.:
"Organic Synthesis of the Prostaglandins: Advancing Biology"
Science, 259, 44-45 (1993) - M. Suzuki, K. Kato, R. Noyori, Yu. Watanabe, H. Takechi, K. Matsumura, B. Langstrom , and Y. Watanabe.:
"(15R)-16-m-Tolyl-17,18,19,20-tetranorisocarbacyclin: A Stable Ligand with High Binding Affinity and specificity for a Prostacyclin Receptor in the Central Nervous System"
Angew. Chem., Int. Ed. Engl., 35, 334-336 (1996). - M. Suzuki, H. Doi, M. Bjorkman, Y. Andersson, B. Langstrom, Y. Watanabe, and R. Noyori.:
"Rapid Coupling of Methyl Iodide with Aryltributylstannanes Mediated by Palladium(0) Complexes: A General Protocol for the Systhesis of 11CH3-Labeled PET Tracers"
Chem. Eur. J, 3, 2039-2042 (1997) - M. Suzuki, H. Doi, T. Hosoya, B. Långström, Y. Watanabe.:
"Rapid Methylation on Carbon Frameworks Leading to the Synthesis of a PET Tracer Capable of Imaging a Novel CNS-Type Prostacyclin Receptor in Living Human Brain"
Trends in Analytical Chemistry, 23, 595-607 (2004). - H. Doi, I. Ban, A. Nonoyama, K. Sumi, C. Kuang, T. Hosoya, H. Tsukada, M. Suzuki.:
"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 C-11CH3 and C-18FCH2 Containing PET Tracers"
Chem. Eur. J., 15 ,4165-4171(2009). - Masaaki Suzuki, Kengo Sumi, Hiroko Koyama, Siqin, Takamitsu Hosoya, Misato Takashima, Hisashi doi.:
"Pd(0)-Mediated Rapid Coupling between Methy Iodide and Hetero-Arylstannanes: an Efficient and General Method for the Incorporation of a Positron-Emitting 11C Radionuclide into Heteroaromatic Frameworks"
Chemistry a European Journal 15,12489-12495(2009). - Takaaki Ikemoto, Takamitsu Hosoya, Kumi Takata, Hiroshi Aoyama, Hirotaka Onoe, Masaaki Suzuki, Makoto Endo.:
"Functional role of NSP-like 1 protein in membrane translocation of glucose transporter 4"
Diabetes,58,2802-2812(2009). - Misato Takashima-Hirano, Miho Shukuri, Tadayuki Takashima, Miki Goto, Yasuhiro Wada,Yasuyoshi Watanabe, Hirotaka Onoe, Hisashi Doi, Masaaki Suzuki.:
"General Method for 11C-Labeling of 2-Arylpropionic Acids and Their Esters:Construction of a PET Tracer Library for a Study of Biological Events Involved in COXs Expression"
Chem. Eur. J., 16, 4250-4258 (2010). - Misato Takashima-Hirano, Tadayuki Takashima, Yumiko Katayama, Yasuhiro Wada, Yuichi Sugiyama, Yasuyoshi Watanabe, Hisashi Doi, Masaaki Suzuki.:
"Efficient Sequential Synthesis of PET Probes of the COX-2 Inhibitor [11C]celecoxib and Its Major Metabolite [11C]SC-62807 and In Vivo PET Evaluation"
19, 2997-3004 (2011). - Masaaki Suzuki, Hiroko Koyama, Misato Takashima-Hirano, Hisashi Doi.:
"Pd0-Mediated Rapid C-[11C]Methylation and C-[18F]Fluoromethylation: Revolutionary Advanced Methods for General Incorporation of Short-Lived Positron-Emitting 11C and 18F Radionuclides in an Organic Framework"
In Tech., Positron Emission Tomography - Current Clinical and Research Aspects, Chapter5, 115-152 (2012)
Principal Investigator
- Masaaki SUZUKI
- Team Leader
Members
- Hideki ISHII
- Deputy Team Leader
- Ryosuke IJUIN
- Research Scientist
- Zhouen ZHANG
- Research Scientist
- Daiki OZAKI
- Research Associate
- Tasuku HAKETA
- Research Associate
- Aya MAWATARI
- Technical Staff I
- Emi SEKITO
- Technical Staff I