Evaluation of agonist and antagonist radioligands for somatostatin receptor imaging of breast cancer using positron emission tomography.

ABSTRACT:

Background

The somatostatin receptor subtype 2 (sstr2) is expressed on a majority of luminal breast cancers, however SPECT and scintigraphy imaging with agonistic sstr2 probes has been sub-optimal. High affinity antagonists can access more binding sites on the cell surface, resulting in higher tumor uptake and improved sensitivity. We compared the tumor uptake and biodistribution of the antagonist ⁶⁸Ga-NODAGA-JR11 with two agonists ⁶⁸Ga-DOTA-Tyr³-octreotide (⁶⁸Ga-DOTATOC) and ⁶⁸Ga-DOTA-Tyr³-octreotate (⁶⁸Ga-DOTATATE), in the human, sstr2-positive, luminal breast cancer model: ZR-75-1.

Results

Peptides were assayed for binding affinity using a filtration-based competitive assay to sstr2. ^nat

SUBMITTER: Dude I 

PROVIDER: S-EPMC5824694 | biostudies-literature | 2017

REPOSITORIES: biostudies-literature