PET of tumor CXCR4 expression with 4-18F-T140.

ABSTRACT:

Unlabelled

Expression of the chemokine receptor CXCR4 by cancers has been shown to correlate with tumor aggressiveness and poor prognosis and may also contribute to metastatic seeding of organs that express its ligand SDF-1. However, fully optimized PET agents for determining CXCR4 expression by tumor cells in vivo are not yet available. This study aims to develop a stable, (18)F-labeled peptide that enables in vivo quantification of CXCR4 in cancer.

Methods

4-F-benzoyl-TN14003 (4-F-T140), a short peptide antagonist of CXCR4 with 1-(4,4-dimethyl-2,6-dioxocyclohexylidene)ethyl protecting groups on the ε-amino groups of the lysine residues, was labeled with (18)F-fluoride via N-succinimidyl-4-(18)F-fluorobenzoate conjugation, followed by deprotection to give 4-(18)F-T140 that

SUBMITTER: Jacobson O 

PROVIDER: S-EPMC3629977 | biostudies-literature | 2010 Nov

REPOSITORIES: biostudies-literature