[18F]RPS-544: A PET tracer for imaging the chemokine receptor CXCR4 Academic Article uri icon

Overview

MeSH Major

  • Dendritic Cells
  • Nerve Tissue Proteins
  • TCF Transcription Factors

abstract

  • Here we present, to the best of our knowledge, the first high affinity [18F]-labeled tracer, suitable for in vivo PET imaging of CXCR4. [18F]RPS-544 displayed high affinity for CXCR4 and good tumor uptake with a maximum uptake at 1 h p.i.. CXCR4 dependent uptake was demonstrated using bilateral tumors with differential CXCR4 expression as well as pharmacological blockade using the known CXCR4 antagonist, AMD-3100. Tissue contrast as judged by tumor to normal tissue ratios was positive in several key tissues. The structural and pharmacological similarities between [18F]RPS-544 and the approved drug AMD-3465, combined with the ease of synthesis and high molar activity (>185 GBq/μmol) achieved during radiosynthesis could lead to accelerated translation into the clinic.

publication date

  • May 2018

Research

keywords

  • Academic Article

Identity

Language

  • eng

Digital Object Identifier (DOI)

  • 10.1016/j.nucmedbio.2018.01.004

PubMed ID

  • 29544122

Additional Document Info

start page

  • 37

end page

  • 44

volume

  • 60