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Nucl Med Mol Imaging 2006;40(4 )218~227 |
9-(4-[18F]Fluoro-3-hydroxymethylbutyl)guanine ([18F]FHBG)ÀÇ ÇÕ¼º°ú Ç츣Æ佺 ´Ü¼ø ¹ÙÀÌ·¯½º Ƽ¹Ìµò Å°³ª¾ÆÁ¦ ÀÌÀÔ °£¾Ï ¼¼Æ÷ÁÖ¿¡¼ÀÇ ±âÃÊ ¿¬±¸ (Synthesis and Preliminary Evaluation of 9-(4-[18F]Fluoro-3-hydroxymethylbutyl) Guanine ([18F]FHBG) in HSV1-tk Gene Transduced Hepatoma Cell) |
Author |
¹®º´¼®1,ÀÌż·2,À̸í±Ù4,À̱³Ã¶1,¾È±¤ÀÏ1,Àü±Ç¼ö1,¿À¿ÁµÎ4,Áö´ëÀ±5,ÃÖâ¿î2,3,ÀÓ»ó¹«2,3,õ±âÁ¤1,2,3, |
Byung Seok Moon,M.S.1, Tae Sup Lee, Ph.D.2, Myoung Keun Lee, M.S.4,Kyo Chul Lee, Ph.D.1,Gwang Il An, Ph.D.1, Kwon Soo Chun, Ph.D.1, Ok Doo Awh, Ph.D.4, Dae Yoon Chi, Ph.D.5,Chang Woon Choi, M.D. & Ph.D.2,3, Sang Moo Lim, M.D. & Ph.D.2,3, and Gi Jeong Cheo |
Affiliation |
¿øÀÚ·ÂÀÇÇпø RI ¹× ¹æ»ç¼ºÀǾàÇ°°³¹ß½Ç1, ÇÙÀÇÇבּ¸½Ç2, ÇÙÀÇÇаú3, ¿¬¼¼´ëÇб³ ÀÓ»óº´¸®Çаú4,ÀÎÇÏ´ëÇб³ ÈÇаú5 1Laboratory of Radiopharmaceuticals, 2Laboratory of Nuclear Medicine, 3Department of Nuclear Medicine, Korea, Institute of Radiological and Medical Sciences, Seoul, Korea; 4Department of Medical Laboratory Science, Yonsei University, Wonju, Korea; 5Depart |
Abstract |
Purpose: The HSV1-tk reporter gene system is the most widely used system because of its advantage that direct
monitoring is possible without the introduction of a separate reporter gene in case of HSV1-tk suicide gene
therapy. In this study, we investigate the usefulness of the reporter probe (substrate), 9-(4-[18F]fluoro-3-
hydroxymethylbutyl)guanine ([18F]FHBG) for non-invasive reporter gene imaging using PET in HSV1-tk expressing
hepatoma model. Materials and Methods: Radiolabeled FHBG was prepared in 8 steps from a commercially
available triester. The labeling reaction was carried out by NCA nucleophilic substitution with K[18F]/K2.2.2. in
acetonitrile using N2-monomethoxytrityl-9-[4-(tosyl)-3-monomethoxytritylmethylbutyl]guanine as a precursor, followed
by deprotection with 1 N HCl. Preliminary biological properties of the probe were evaluated with MCA cells and
MCA-tk cells transduced with HSV1-tk reporter gene. In vitro uptake and release-out studies of [18F]FHBG were
performed, and was analyzed correlation between [18F]FHBG uptake ratio according to increasing numeric count of
MCA-tk cells and degree of gene expression. MicroPET scan image was obtained with MCA and MCA-tk tumor
bearing Balb/c-nude mouse model. Results: [18F]FHBG was purified by reverse phase semi-HPLC system and
collected at around 16-18 min. Radiochemical yield was about 20-25% (corrected for decay), radiochemical purity
was >95% and specific activity was around >55.5 GBq/¥ìmol. Specific accumulation of [18F]FHBG was observed in
HSV1-tk gene transduced MCA-tk cells but not in MCA cells, and consecutive 1 hour release-out results showed
more than 86% of uptaked [18F]FHBG was retained inside of cells. The uptake of [18F]FHBG was showed a highly
significant linear correlation (R2=0.995) with increasing percentage of MCA-tk numeric cell count. In microPET scan
images, remarkable difference of accumulation was observed for the two type of tumors. Conclusion: [18F]FHBG
appears to be a useful as non-invasive PET imaging substrate in HSV1-tk expressing hepatoma model. (Nucl Med
Mol Imaging 2006;40(4):218-227) |
Keyword |
[18F]FHBG, thymidine kinase, gene therapy, PET |
Full text Article |
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