Radiosynthesis and evaluation of tumor cell-penetrating oligopeptides containing short-lived positron-emitt ing radionuclides

2016 Fiscal Year Final Research Report

• Project/Area Number: 26861031
• Research Category: Grant-in-Aid for Young Scientists (B)
• Allocation Type: Multi-year Fund
• Research Field: Radiation science
• Research Institution: National Institutes for Quantum and Radiological Science and Technology
• Principal Investigator: Hanyu Masayuki 国立研究開発法人量子科学技術研究開発機構, 放射線医学総合研究所 標識薬剤開発部, 研究員(任常) (80435552)
• Project Period (FY): 2014-04-01 – 2017-03-31
• Keywords: PETイメージング / オリゴペプチド / ピクテスペングラー反応

Outline of Final Research Achievements

A procedure for the synthesis of a carbon-11 labeled oligopeptide containing [1-11C]1,2,3,4-tetrahydro-beta-carboline-3-carboxylic acid ([1-11C]Tpi) from the corresponding Trp・HCl-containing peptides has been developed involving a Pictet-Spengler reaction with [11C]formaldehyde. The radiolabeling of a Trp・HCl-containing iRGD peptide using the Pictet-Spengler reaction was successful. Furthermore, the remote-controlled synthesis of a [1-11C]Tpi-containing iRGD (1) peptide was attempted using an automatic production system to generate [11C]CH3I. The radiochemical yield of the compound 1 at the end of synthesis was 4.2 ± 3.2 % (n=3), for a total synthesis time of about 35 min. The usefulness of our synthesis was demonstrated PET studies using the compound 1 for the mouse bearing MIAPaca-2 and BxPC-3, a small cell pancreatic cancer cell line. The BxPC-3 cell-to-muscle and MIAPaca-2 cell-to-muscle of 1 at 22 min were not retained.

Free Research Field

医歯薬学