title: Disclosing the CXCR4 expression in lymphoproliferative diseases by targeted molecular imaging.
abstract: 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 [(68)Ga]Pentixafor in mice bearing human lymphoma xenografts as an exemplary CXCR4-expressing tumor entity, we report on the first clinical applications of [(68)Ga]Pentixafor-Positron Emission Tomography as a powerful method for CXCR4 imaging in cancer patients. [(68)Ga]Pentixafor binds with high affinity and selectivity to human CXCR4 and exhibits a favorable dosimetry. [(68)Ga]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.
authors.affiliation: 1. Pharmaceutical Radiochemistry, Technische Universität München, Garching, Germany.
authors.forename: Hans Jürgen
authors.initials: HJ
authors.lastname: Wester
authors.affiliation: 2. III. Medical Department, Technische Universität München, Munich, Germany.
authors.forename: Ulrich
authors.initials: U
authors.lastname: Keller
authors.affiliation: 1. Pharmaceutical Radiochemistry, Technische Universität München, Garching, Germany.
authors.forename: Margret
authors.initials: M
authors.lastname: Schottelius
authors.affiliation: 3. Department of Nuclear Medicine, Technische Universität München, Munich, Germany.
authors.forename: Ambros
authors.initials: A
authors.lastname: Beer
authors.affiliation: 2. III. Medical Department, Technische Universität München, Munich, Germany.
authors.forename: Kathrin
authors.initials: K
authors.lastname: Philipp-Abbrederis
authors.affiliation: 1. Pharmaceutical Radiochemistry, Technische Universität München, Garching, Germany.
authors.forename: Frauke
authors.initials: F
authors.lastname: Hoffmann
authors.affiliation: 1. Pharmaceutical Radiochemistry, Technische Universität München, Garching, Germany.
authors.forename: Jakub
authors.initials: J
authors.lastname: Šimeček
authors.affiliation: 3. Department of Nuclear Medicine, Technische Universität München, Munich, Germany.
authors.forename: Carlos
authors.initials: C
authors.lastname: Gerngross
authors.affiliation: 4. Department of Nuclear Medicine, University Hospital Würzburg, Würzburg, Germany.
authors.forename: Michael
authors.initials: M
authors.lastname: Lassmann
authors.affiliation: 4. Department of Nuclear Medicine, University Hospital Würzburg, Würzburg, Germany.
authors.forename: Ken
authors.initials: K
authors.lastname: Herrmann
authors.affiliation: 5. Institute of Pathology, Helmholtz Zentrum München, Munich, Germany.
authors.forename: Natalia
authors.initials: N
authors.lastname: Pellegata
authors.affiliation: 6. Institute of Pathology, Universität Würzburg, Comprehensive Cancer Center Mainfranken, Würzburg, Germany.
authors.forename: Martina
authors.initials: M
authors.lastname: Rudelius
authors.affiliation: 7. Institute for Advanced Study, Department of Chemistry, Technische Universität München, Garching, Germany ; 8. Chemistry Department, Faculty of Science, King Abdulaziz University, Jeddah, Saudi Arabia.
authors.forename: Horst
authors.initials: H
authors.lastname: Kessler
authors.affiliation: 3. Department of Nuclear Medicine, Technische Universität München, Munich, Germany.
authors.forename: Markus
authors.initials: M
authors.lastname: Schwaiger
mesh_terms: D000818:Animals; D056831:Coordination Complexes / Q000138:chemical synthesis / Q000493:pharmacokinetics* / Q000494:pharmacology; D005260:Female; D006801:Humans; D019169:Jurkat Cells; D016403:Lymphoma, Large B-Cell, Diffuse / Q000000981:diagnostic imaging*; D008297:Male; D051379:Mice; D016513:Mice, SCID; D010456:Peptides, Cyclic / Q000138:chemical synthesis / Q000493:pharmacokinetics* / Q000494:pharmacology; D049268:Positron-Emission Tomography; D011485:Protein Binding; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics* / Q000494:pharmacology; D019718:Receptors, CXCR4 / Q000037:antagonists & inhibitors / Q000378:metabolism*; D014018:Tissue Distribution
chemical_list: C000597686:68Ga-pentixafor; D056831:Coordination Complexes; D010456:Peptides, Cyclic; D019275:Radiopharmaceuticals; D019718:Receptors, CXCR4
keywords: CXCR4; chemokine receptor; lymphoma, in vivo imaging; positron emission tomography
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