2000 Fiscal Year Final Research Report Summary
Synthetic Study of Peptides Accumulating into Tumor Cells for the Diagnosis and Treatment of Cancer.
| Project/Area Number |
11680593
|
|---|
| Research Category |
Grant-in-Aid for Scientific Research (C)
|
| Allocation Type | Single-year Grants |
|---|
| Section | 一般 |
|---|
| Research Field |
Bioorganic chemistry
|
|---|
| Research Institution | Kinki University |
|---|
Principal Investigator |
WAKAMIYA Tateaki School of Science and Engineering, Kinki University, Professor, 理工学部, 教授 (10028243)
|
|---|
| Project Period (FY) |
1999 – 2000
|
| Keywords | 4-Fluorophenylalanine / Oligopeptide Transporter / Cancer / p-Boronophenylalanine / Peptides Accumulating into Tumor Cells / Positron Emission Tomography / Boron Neutron Capture Theraph / Nuclear Magnetic Resonance Imaging Method |
|---|
| 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.
|
