18F-Based Pretargeted PET Imaging Based on Bioorthogonal Diels-Alder Click Chemistry Academic Article uri icon

Overview

MeSH Major

  • Cyclooctanes
  • Fluorine Radioisotopes
  • Immunoconjugates
  • Pancreatic Neoplasms
  • Positron-Emission Tomography

abstract

  • A first-of-its-kind (18)F pretargeted PET imaging approach based on the bioorthogonal inverse electron demand Diels-Alder (IEDDA) reaction between tetrazine (Tz) and trans-cyclooctene (TCO) is presented. As proof-of-principle, a TCO-bearing immunoconjugate of the anti-CA19.9 antibody 5B1 and an Al[(18)F]NOTA-labeled tetrazine radioligand were harnessed for the visualization of CA19.9-expressing BxPC3 pancreatic cancer xenografts. Biodistribution and (18)F-PET imaging data clearly demonstrate that this methodology effectively delineates tumor mass with activity concentrations up to 6.4 %ID/g at 4 h after injection of the radioligand.

publication date

  • February 17, 2016

Research

keywords

  • Academic Article

Identity

Language

  • eng

PubMed Central ID

  • PMC4759614

Digital Object Identifier (DOI)

  • 10.1021/acs.bioconjchem.5b00504

PubMed ID

  • 26479967

Additional Document Info

start page

  • 298

end page

  • 301

volume

  • 27

number

  • 2