Journal
THERANOSTICS
Volume 5, Issue 6, Pages 618-630Publisher
IVYSPRING INT PUBL
DOI: 10.7150/thno.11251
Keywords
CXCR4; chemokine receptor; positron emission tomography; lymphoma; in vivo imaging
Categories
Funding
- Deutsche Forschungsgemeinschaft [SFB824, Z1/4, A5/7/8, B5/8, C3]
- DFG [KE 222/7-1, DJCLS R11/18]
- Center of Integrated Protein Science Munic (CIPSM)
- King Abdulaziz University KAU [HiCi/25-3-1432]
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Chemokine ligand-receptor interactions play a pivotal role in cell attraction and cellular trafficking, both in normal tissue homeostasis and in disease. In cancer, chemokine receptor-4 (CXCR4) expression is an adverse prognostic factor. Early clinical studies suggest that targeting CXCR4 with suitable high-affinity antagonists might be a novel means for therapy. In addition to the preclinical evaluation of [Ga-68]Pentixafor in mice bearing human lymphoma xenografts as an exemplary CXCR4-expressing tumor entity, we report on the first clinical applications of [Ga-68]Pentixafor-Positron Emission Tomography as a powerful method for CXCR4 imaging in cancer patients. [Ga-68]Pentixafor binds with high affinity and selectivity to human CXCR4 and exhibits a favorable dosimetry. [Ga-68]Pentixafor-PET provides images with excellent specificity and contrast. This non-invasive imaging technology for quantitative assessment of CXCR4 expression allows to further elucidate the role of CXCR4/CXCL12 ligand interaction in the pathogenesis and treatment of cancer, cardiovascular diseases and autoimmune and inflammatory disorders.
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