Synthesis of 2′-deoxy-2′-[18F]fluoro-5-bromo-1- β-D-arabinofuranosyluracil ([18F]-FBAU) and 2′-deoxy- 2′-[18F]fluoro-5-chloro-1-β-D-arabinofuranosyl-uracil ([18F]-FCAU), and their biological evaluation as markers for gene expression

Mian M. Alauddin; Antranic Shahinian; Ryan Park; Michel Tohme; John D. Fissekis; Peter S. Conti

doi:10.1016/j.nucmedbio.2003.12.008

Synthesis of 2′-deoxy-2′-[¹⁸F]fluoro-5-bromo-1- β-D-arabinofuranosyluracil ([¹⁸F]-FBAU) and 2′-deoxy- 2′-[¹⁸F]fluoro-5-chloro-1-β-D-arabinofuranosyl-uracil ([¹⁸F]-FCAU), and their biological evaluation as markers for gene expression

Mian M. Alauddin
, Antranic Shahinian
, Ryan Park
, Michel Tohme
, John D. Fissekis
, Peter S. Conti

Cancer Systems Imaging

Research output: Contribution to journal › Article › peer-review

34 Scopus citations

Abstract

[¹⁸F]-FBAU and [¹⁸F]-FCAU have been synthesized and evaluated in vivo as markers for HSV1-tk gene expression. At 2 hours, uptake of [¹⁸F]-FBAU and [¹⁸F]-FCAU in HSV1-tk-positive tumors was 7.9-fold and 6.0-fold higher than the control tumors, respectively. Micro-PET images also showed very high uptake in HSV-tk tumors. Compared to [ ¹⁴C]-FMAU, total uptake of [¹⁸F]-FBAU and [ ¹⁸F]-FCAU was similar in tk-positive cells, but the uptake ratio (tk+/wild) was higher. [¹⁸F]-FBAU and [¹⁸F]-FCAU appear to be potential PET imaging agents for gene expression.

Original language	English (US)
Pages (from-to)	399-405
Number of pages	7
Journal	Nuclear Medicine and Biology
Volume	31
Issue number	4
DOIs	https://doi.org/10.1016/j.nucmedbio.2003.12.008
State	Published - May 2004

Keywords

FBAU
FCAU
FMAU
Gene expression
HSV-tk
PET

ASJC Scopus subject areas

Molecular Medicine
Radiology Nuclear Medicine and imaging
Cancer Research

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10.1016/j.nucmedbio.2003.12.008

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Alauddin, M. M., Shahinian, A., Park, R., Tohme, M., Fissekis, J. D., & Conti, P. S. (2004). Synthesis of 2′-deoxy-2′-[¹⁸F]fluoro-5-bromo-1- β-D-arabinofuranosyluracil ([¹⁸F]-FBAU) and 2′-deoxy- 2′-[¹⁸F]fluoro-5-chloro-1-β-D-arabinofuranosyl-uracil ([¹⁸F]-FCAU), and their biological evaluation as markers for gene expression. Nuclear Medicine and Biology, 31(4), 399-405. https://doi.org/10.1016/j.nucmedbio.2003.12.008

Synthesis of 2′-deoxy-2′-[¹⁸F]fluoro-5-bromo-1- β-D-arabinofuranosyluracil ([¹⁸F]-FBAU) and 2′-deoxy- 2′-[¹⁸F]fluoro-5-chloro-1-β-D-arabinofuranosyl-uracil ([¹⁸F]-FCAU), and their biological evaluation as markers for gene expression. / Alauddin, Mian M.; Shahinian, Antranic; Park, Ryan et al.
In: Nuclear Medicine and Biology, Vol. 31, No. 4, 05.2004, p. 399-405.

Research output: Contribution to journal › Article › peer-review

Alauddin, MM, Shahinian, A, Park, R, Tohme, M, Fissekis, JD & Conti, PS 2004, 'Synthesis of 2′-deoxy-2′-[¹⁸F]fluoro-5-bromo-1- β-D-arabinofuranosyluracil ([¹⁸F]-FBAU) and 2′-deoxy- 2′-[¹⁸F]fluoro-5-chloro-1-β-D-arabinofuranosyl-uracil ([¹⁸F]-FCAU), and their biological evaluation as markers for gene expression', Nuclear Medicine and Biology, vol. 31, no. 4, pp. 399-405. https://doi.org/10.1016/j.nucmedbio.2003.12.008

Alauddin MM, Shahinian A, Park R, Tohme M, Fissekis JD, Conti PS. Synthesis of 2′-deoxy-2′-[¹⁸F]fluoro-5-bromo-1- β-D-arabinofuranosyluracil ([¹⁸F]-FBAU) and 2′-deoxy- 2′-[¹⁸F]fluoro-5-chloro-1-β-D-arabinofuranosyl-uracil ([¹⁸F]-FCAU), and their biological evaluation as markers for gene expression. Nuclear Medicine and Biology. 2004 May;31(4):399-405. doi: 10.1016/j.nucmedbio.2003.12.008

Alauddin, Mian M. ; Shahinian, Antranic ; Park, Ryan et al. / Synthesis of 2′-deoxy-2′-[¹⁸F]fluoro-5-bromo-1- β-D-arabinofuranosyluracil ([¹⁸F]-FBAU) and 2′-deoxy- 2′-[¹⁸F]fluoro-5-chloro-1-β-D-arabinofuranosyl-uracil ([¹⁸F]-FCAU), and their biological evaluation as markers for gene expression. In: Nuclear Medicine and Biology. 2004 ; Vol. 31, No. 4. pp. 399-405.

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title = "Synthesis of 2′-deoxy-2′-[18F]fluoro-5-bromo-1- β-D-arabinofuranosyluracil ([18F]-FBAU) and 2′-deoxy- 2′-[18F]fluoro-5-chloro-1-β-D-arabinofuranosyl-uracil ([18F]-FCAU), and their biological evaluation as markers for gene expression",

abstract = "[18F]-FBAU and [18F]-FCAU have been synthesized and evaluated in vivo as markers for HSV1-tk gene expression. At 2 hours, uptake of [18F]-FBAU and [18F]-FCAU in HSV1-tk-positive tumors was 7.9-fold and 6.0-fold higher than the control tumors, respectively. Micro-PET images also showed very high uptake in HSV-tk tumors. Compared to [ 14C]-FMAU, total uptake of [18F]-FBAU and [ 18F]-FCAU was similar in tk-positive cells, but the uptake ratio (tk+/wild) was higher. [18F]-FBAU and [18F]-FCAU appear to be potential PET imaging agents for gene expression.",

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author = "Alauddin, \{Mian M.\} and Antranic Shahinian and Ryan Park and Michel Tohme and Fissekis, \{John D.\} and Conti, \{Peter S.\}",

note = "Funding Information: This work was supported in part by National Cancer Institute Grant CA 72896. ",

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AU - Alauddin, Mian M.

AU - Shahinian, Antranic

AU - Park, Ryan

AU - Tohme, Michel

AU - Fissekis, John D.

AU - Conti, Peter S.

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AB - [18F]-FBAU and [18F]-FCAU have been synthesized and evaluated in vivo as markers for HSV1-tk gene expression. At 2 hours, uptake of [18F]-FBAU and [18F]-FCAU in HSV1-tk-positive tumors was 7.9-fold and 6.0-fold higher than the control tumors, respectively. Micro-PET images also showed very high uptake in HSV-tk tumors. Compared to [ 14C]-FMAU, total uptake of [18F]-FBAU and [ 18F]-FCAU was similar in tk-positive cells, but the uptake ratio (tk+/wild) was higher. [18F]-FBAU and [18F]-FCAU appear to be potential PET imaging agents for gene expression.

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