Title: Synthesis and biological evaluation of an (123)I-labeled bicyclic nucleoside analogue (BCNA) as potential SPECT tracer for VZV-tk reporter gene imaging
Authors: Chitneni, Satish Kumar
Deroose, Christophe
Fonge, Humphrey
Gijsbers, Rik
Dyubankova, Natalia
Balzarini, Jan
Debyser, Zeger
Mortelmans, Luc
Verbruggen, Alfons
Bormans, Guy # ×
Issue Date: Jun-2007
Publisher: Pergamon Press
Series Title: Bioorganic & Medicinal Chemistry Letters vol:17 issue:12 pages:3458-3462
Abstract: An iodine-123 labeled bicyclic nucleoside analogue ([(123)I]-4) has been synthesized and evaluated as a potential single photon emission tomography (SPECT) reporter probe for the non-invasive imaging of expression of the varicella zoster virus thymidine kinase (VZV-tk) reporter gene. In vitro enzymatic assays revealed that the non-radioactive mono-iodo derivative 4 has good affinity for VZV-TK (IC(50): 4.2muM). Biodistribution of [(123)I]-4 was examined in normal mice. Evaluation of [(123)I]-4 in HEK-293T cells showed 1.74-fold higher accumulation in VZV-TK-expressing cells compared to control cells.
ISSN: 0960-894X
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
Medicinal Chemistry (Rega Institute)
Molecular Virology and Gene Therapy
Nuclear Medicine & Molecular Imaging
× corresponding author
# (joint) last author

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