title: Synthesis and biological evaluation of an 123I-labeled bicyclic nucleoside analogue (BCNA) as potential SPECT tracer for VZV-tk reporter gene imaging.
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): 4.2 microM). 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.
authors: Laboratory for Radiopharmacy, Katholieke Universiteit Leuven, Leuven, Belgium.
authors: Satish K
authors: SK
authors: Chitneni
authors: Christophe M
authors: CM
authors: Deroose
authors: Humphrey
authors: H
authors: Fonge
authors: Rik
authors: R
authors: Gijsbers
authors: Natalia
authors: N
authors: Dyubankova
authors: Jan
authors: J
authors: Balzarini
authors: Zeger
authors: Z
authors: Debyser
authors: Luc
authors: L
authors: Mortelmans
authors: Alfons M
authors: AM
authors: Verbruggen
authors: Guy M
authors: GM
authors: Bormans
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D001643:Bridged Bicyclo Compounds / Q000138:chemical synthesis / Q000494:pharmacology*; D002460:Cell Line / Q000187:drug effects; D017930:Genes, Reporter; D014645:Herpesvirus 3, Human / Q000187:drug effects* / Q000235:genetics; D006801:Humans; D007457:Iodine Radioisotopes; D007668:Kidney / Q000166:cytology / Q000196:embryology / Q000473:pathology; D008956:Models, Chemical; D009712:Nucleotides, Cyclic / Q000138:chemical synthesis / Q000494:pharmacology*; D049268:Positron-Emission Tomography; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000494:pharmacology*; D013937:Thymidine Kinase / Q000235:genetics / Q000378:metabolism
chemical_list: D000998:Antiviral Agents; D001643:Bridged Bicyclo Compounds; D007457:Iodine Radioisotopes; D009712:Nucleotides, Cyclic; D019275:Radiopharmaceuticals; D013937:Thymidine Kinase