4.7 Article

The efficiency of 18F labelling of a prostate specific membrane antigen ligand via strain-promoted azide-alkyne reaction: reaction speed versus hydrophilicity

Journal

CHEMICAL COMMUNICATIONS
Volume 54, Issue 56, Pages 7810-7813

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/c8cc03999b

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Funding

  1. UNC Chapel Hill Department of Radiology and BRIC
  2. NSF [CHE-1565646]
  3. Science and Technology Program of Guangzhou, China [201804010448]
  4. UNC-CH

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Here we report the F-18 labeling of a prostate specific membrane antigen (PSMA) ligand via a strain promoted oxa-dibenzocyclooctyne (ODIBO)- or bicyclo[6.1.0]nonyne (BCN)-azide reaction. Although ODIBO reacts with azide 20 fold faster than BCN, in vivo PET imaging suggests that F-18-BCN-azide-PSMA demonstrated much higher tumor uptake and a much higher tumor to background contrast.

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