Synthesis and pre-clinical evaluation of a new class of high-affinity ¹⁸F-labeled PSMA ligands for detection of prostate cancer by PET imaging.

ABSTRACT:

Purpose

Current clinical imaging of PSMA-positive prostate cancer by positron emission tomography (PET) mainly features ⁶⁸Ga-labeled tracers, notably [⁶⁸Ga]Ga-PSMA-HBED-CC. The longer half-life of fluorine-18 offers significant advantages over Ga-68, clinically and logistically. We aimed to develop high-affinity PSMA inhibitors labeled with fluorine-18 as alternative tracers for prostate cancer.

Methods

Six triazolylphenyl ureas and their alkyne precursors were synthesized from the Glu-urea-Lys PSMA binding moiety. PSMA affinity was determined in a competitive binding assay using LNCaP cells. The [¹⁸F]triazoles were isolated following a Cu(I)-catalyzed click reaction between the alkynes and [¹⁸F]fluoroethylazide. The ¹⁸F

SUBMITTER: Kelly J 

PROVIDER: S-EPMC5323493 | biostudies-literature | 2017 Apr

REPOSITORIES: biostudies-literature