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2'-Deoxy-2'-[ 18 F]fluoro-5-fluoro-1-β-D-arabinofuranosyluracil

2'-Deoxy-2'-[ 18 F]fluoro-5-fluoro-1-β-D-arabinofuranosyluracil

The MICAD Research Team

PMID: 20641657

Abstract:

Herpes simplex virus type-1 thymidine kinase (HSV1-tk) can be used as a suicide gene for gene therapy. As of today, animal studies using HSV1-tk gene and ganciclovir (1) have brought some success in treating malignant tumors with suicide gene therapy; however, clinical results showed that such methods did not provide sufficient gene delivery to the tumor human cells for therapy (2).
HSV1-tk can phosphorylate a wide range of nucleoside analogs (e.g. acycloguanosines and 2'-deoxyfuranosyluracil nucleoside derivatives) that are not phosphorylated efficiently by the native enzyme (3). The presence of fluorine in the 2'-arabino position in a furanosyluracil nucleoside results in enhanced monophosphorylation by HSV-tk type 1 and type 2 compared with the host thymidine kinase.
In vivo imaging methods are essential tools for monitoring the gene expression as an indicator of gene delivery and for quantifying the level of HSV1-tk enzyme activity after gene transfer (4-6). Several probes for positron emission tomography (PET) of HSV1 -tk gene have been studied so far. Among them, [18F]FMAU, [18F]FHPG (7), [18F]FHBG and [18F]FIAU. [124I]FIAU appears to be superior to the acycloguanosine derivatives FHPG and FHBG in some cell lines (8) with respect to total uptake and the uptake ratio (tk-positive to wild type), although it is susceptible to deiodination in vivo. 2'-deoxy-2'-fluoro-5-fluoro-1-α-D-arabinofuranosyluracil ([18F]FFAU) may offer an advantage over [124I]FIAU and other 5-substituted analogs for imaging gene expression, and is currently under investigation (9).

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP59277893-A	Acycloguanosine		59277-89-3	Price

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