University of Delaware OEIP
University of Delaware

Highly Reactive Trans-Cyclooctenes For Radiochemical Labeling

Technology #ud16-22

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Researchers
Dr. Joseph Fox
Research in the Fox group centers on the development of new types of chemical reactions, the application of these new reactions to the synthesis of naturally occurring and designed molecules with biological function, and in the use of design concepts in organic synthesis for applications in biology and materials science
External Link (www1.udel.edu)
Dr. Zibo Li
Yu Liu
Michael Taylor
Dennis Svatunek
Katarina Rohlfing
Mengzhe Wang
Zhanhong Wu
Managed By
Yops Brad
Director, Technology Transfer Center 3028310147
Patent Protection

Conformationally strained trans-cycloalkenes for radiolabeling

PCT Patent Application WO 2017106253 A1
Publications
Conformationally Strained trans-Cyclooctene (sTCO) Enables the Rapid Construction of 18F-PET Probes via Tetrazine Ligation
Theranostics, 2016, Vol. 6, Issue 6, 887-895

Technology Description:

Positron emission tomography (PET) is a non-invasive technique to track radiolabeled biomolecules in vivo. F-18 is the most commonly used radionuclides and there is a high demand for methods that efficiently introduce F-18 to biological macromolecules. Researchers at the University of Delaware have developed a second generation F-18 labeling system based on a conformational strained trans-cyclooctene (sTCO). An improvement in the existing technology, the biorthogonal reaction between tetrazines and trans-cyclooctenes is a method for the rapid construction of F-18 probes for PET imaging. Hence these tetrazine ligations employing F18-sTCO can serve as a powerful and general platform for the rapid construction of peptide or protein derived PET agents.

Benefits:

  • Broad ranged, can be used to label all biomolecules. 
  • 100x faster than the current methods of F18 induction into the biomolecule. 
  •  The radiolabeled-peptides constructed by this method display better pharmacokinetic properties

Uses/Users:

  • In-vivo biomolecule imaging 
  • Probe construction 
  • Pre-targeted imaging 
  • Radiation therapy 
  • Potential use in drug labeling and targeted drug delivery