| Budget Amount *help |
¥3,700,000 (Direct Cost: ¥3,700,000)
Fiscal Year 2000: ¥1,000,000 (Direct Cost: ¥1,000,000)
Fiscal Year 1999: ¥2,700,000 (Direct Cost: ¥2,700,000)
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| Research Abstract |
In the first year of this project, nine kinds of 4-fluorophenylalanine [Phe(4F)] containing peptides were synthesized. These peptides were accumulated into some kinds of tumor cells via specific oligopeptide transporter. This result suggests that Phe(4F)-containing peptides can be utilized for the diagnosis of cancer based on the positron emission tomography (PET). For this purpose, however, we have to newly develop a convenient method for the preparation of Phe(4F) labeled with ^<18>F.
In the second year, three kinds of p-boronophenylalanine (Bpa) containing peptides with serine, glutamic acid and lysine as C-terminal amino acid, respectively. These peptides are 300-fold more soluble in water than Bpa, and their accumulation into tumor cells are comparable to that of Bpa. The results suggest that Bpa-containing peptides may be good candidates for boron neutron capture therapy (BNCT) of cancer. From a viewpoint of necessity of Bpa as very valuable ^<10>B carrier, we developed a novel and secure method to prepare Bpa.
p-Boronophenylalaninol (Bpa-ol) reported by Kirihata et al.is also useful compound as a ^<10>B carrier. In the present study, we synthesized a hybrid compound between Bpa and Bpa-ol, and are currently undertaking the measurement of their accumulation into tumor cells as well as their tumor cell killing effect.
As a result of present study, we newly planned to elucidate nuclear magnetic resonance imaging method for the diagnosis of cancer using Phe(4F)- or Bpa-containing peptides that accumulate specifically into tumor cells.
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