Biomolecule PET based on one-pot/flow 68Ga-DOTA labeling

2015 Fiscal Year Final Research Report

• Project/Area Number: 25560410
• Research Category: Grant-in-Aid for Challenging Exploratory Research
• Allocation Type: Multi-year Fund
• Research Field: Biomolecular chemistry
• Research Institution: Institute of Physical and Chemical Research
• Principal Investigator: Tanaka Katsunori 国立研究開発法人理化学研究所, 田中生体機能合成化学研究室, 准主任研究員 (00403098)
• Project Period (FY): 2013-04-01 – 2016-03-31
• Keywords: 68Ga-DOTA / アザ電子環状反応 / 理研クリック反応 / アルデヒド / アミノ基 / ポジトロン / ペプチド / PET

Outline of Final Research Achievements

Convenient and general method for labeling of lysines of biomolecules was established. Azide-containing labels were initially conjugated with the unsaturated ester aldehyde containing the strained acetylenes, by the strain-promoted click reaction. The resulting probes were then treated with the peptides, proteins, antibodies, and even live cell surface in one-pot process, efficiently labeling these biomolecules by azaelectrocyclization (now called as RIKEN click reaction) under the mild conditions. The efficient one-pot procedure enabled the introduction of various labels, e.g., positron emitters, paramagnetic metals, and fluorescences, very rapidly onto the various biomolecules including the sensitive and precious materials which are available with only limited amount. Applicability of biologically important molecules towards diagnosis and therapy will be expanded significantly.

Free Research Field

有機合成化学、ケミカルバイオロジー