Synthesis and biological evaluation of an 123I-labeled bicyclic nucleoside analogue (BCNA) as potential SPECT tracer for VZV-tk reporter gene imaging.
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.
Chitneni
Satish K
SK
Laboratory for Radiopharmacy, Katholieke Universiteit Leuven, Leuven, Belgium.
Deroose
Christophe M
CM
Fonge
Humphrey
H
Gijsbers
Rik
R
Dyubankova
Natalia
N
Balzarini
Jan
J
Debyser
Zeger
Z
Mortelmans
Luc
L
Verbruggen
Alfons M
AM
Bormans
Guy M
GM
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
D000998:Antiviral Agents; D001643:Bridged Bicyclo Compounds; D007457:Iodine Radioisotopes; D009712:Nucleotides, Cyclic; D019275:Radiopharmaceuticals; D013937:Thymidine Kinase