Tc-Labeled Cyclic RGD Peptides for Noninvasive Monitoring of Tumor Integrin αβ Expression
This report describes the biologic evaluations of [ 99m Tc(HYNIC-3P-RGD 2 )(tricine)(TPPTS)] ( 99m Tc-3P-RGD 2 : 6-hydrazinonicotinyl; 3P-RGD 2 = PEG 4 -E[PEG 4 -c(RGDfK)] 2 ; PEG 4 = 15-amino-4,7,10,13-tetraoxapentadecanoic acid; and TPPTS = trisodium triphenylpho-sphine-3,3′,3“-trisulfonate), [ 99...
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| Format: | Article |
| Language: | English |
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SAGE Publishing
2011-09-01
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| Series: | Molecular Imaging |
| Online Access: | https://doi.org/10.2310/7290.2011.00006 |
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| author | Yang Zhou Young-Seung Kim Sudipta Chakraborty Jiyun Shi Haijuan Gao Shuang Liu |
| author_facet | Yang Zhou Young-Seung Kim Sudipta Chakraborty Jiyun Shi Haijuan Gao Shuang Liu |
| author_sort | Yang Zhou |
| collection | DOAJ |
| description | This report describes the biologic evaluations of [ 99m Tc(HYNIC-3P-RGD 2 )(tricine)(TPPTS)] ( 99m Tc-3P-RGD 2 : 6-hydrazinonicotinyl; 3P-RGD 2 = PEG 4 -E[PEG 4 -c(RGDfK)] 2 ; PEG 4 = 15-amino-4,7,10,13-tetraoxapentadecanoic acid; and TPPTS = trisodium triphenylpho-sphine-3,3′,3“-trisulfonate), [ 99m Tc(HYNIC-3G-RGD 2 )(tricine)(TPPTS)] ( 99m Tc-3G-RGD 2 : 3G-RGD 2 = G 3 -E[G 3 -c(RGDfK)] 2 and G 3 = Gly-Gly-Gly), and 99m TcO(MAG 2 −3G-RGD 2 ) (MAG 2 = mercaptoacetylglycylglycyl) as radiotracers for noninvasive imaging of tumor integrin α v β 3 expression in five xenografted tumor-bearing models. Biodistribution and imaging studies were performed in athymic nude mice bearing U87MG, MDA-MB-435, A549, HT29, or PC-3 tumor xenografts. Immunochemistry was performed using the cultured primary tumor cells and xenografted tumor tissues. It was found that the radiotracer tumor uptake followed the trend U87MG > MDA-MB-435 ≈ HT29 ≈ A549 > PC-3. The total integrin β 3 expression levels followed the general trend: U87MG > MDA-MB-435 ≈ A549~HT29 > PC-3. There is a linear relationship between the radiotracer injected dose per gram tumor uptake and the total integrin β 3 expression levels. On the basis of these, it was concluded that radiotracer tumor uptake is contributed by integrin α V β 3 expressed on tumor cells and activated endothelial cells of the tumor neovasculature. 99m Tc-3P-RGD 2 has the capability to monitor integrin α v β 3 expression in a noninvasive fashion. |
| format | Article |
| id | doaj-art-2443fa329ded458c9abc5210e008449e |
| institution | Kabale University |
| issn | 1536-0121 |
| language | English |
| publishDate | 2011-09-01 |
| publisher | SAGE Publishing |
| record_format | Article |
| series | Molecular Imaging |
| spelling | doaj-art-2443fa329ded458c9abc5210e008449e2025-02-03T10:08:13ZengSAGE PublishingMolecular Imaging1536-01212011-09-011010.2310/7290.2011.0000610.2310_7290.2011.00006Tc-Labeled Cyclic RGD Peptides for Noninvasive Monitoring of Tumor Integrin αβ ExpressionYang ZhouYoung-Seung KimSudipta ChakrabortyJiyun ShiHaijuan GaoShuang LiuThis report describes the biologic evaluations of [ 99m Tc(HYNIC-3P-RGD 2 )(tricine)(TPPTS)] ( 99m Tc-3P-RGD 2 : 6-hydrazinonicotinyl; 3P-RGD 2 = PEG 4 -E[PEG 4 -c(RGDfK)] 2 ; PEG 4 = 15-amino-4,7,10,13-tetraoxapentadecanoic acid; and TPPTS = trisodium triphenylpho-sphine-3,3′,3“-trisulfonate), [ 99m Tc(HYNIC-3G-RGD 2 )(tricine)(TPPTS)] ( 99m Tc-3G-RGD 2 : 3G-RGD 2 = G 3 -E[G 3 -c(RGDfK)] 2 and G 3 = Gly-Gly-Gly), and 99m TcO(MAG 2 −3G-RGD 2 ) (MAG 2 = mercaptoacetylglycylglycyl) as radiotracers for noninvasive imaging of tumor integrin α v β 3 expression in five xenografted tumor-bearing models. Biodistribution and imaging studies were performed in athymic nude mice bearing U87MG, MDA-MB-435, A549, HT29, or PC-3 tumor xenografts. Immunochemistry was performed using the cultured primary tumor cells and xenografted tumor tissues. It was found that the radiotracer tumor uptake followed the trend U87MG > MDA-MB-435 ≈ HT29 ≈ A549 > PC-3. The total integrin β 3 expression levels followed the general trend: U87MG > MDA-MB-435 ≈ A549~HT29 > PC-3. There is a linear relationship between the radiotracer injected dose per gram tumor uptake and the total integrin β 3 expression levels. On the basis of these, it was concluded that radiotracer tumor uptake is contributed by integrin α V β 3 expressed on tumor cells and activated endothelial cells of the tumor neovasculature. 99m Tc-3P-RGD 2 has the capability to monitor integrin α v β 3 expression in a noninvasive fashion.https://doi.org/10.2310/7290.2011.00006 |
| spellingShingle | Yang Zhou Young-Seung Kim Sudipta Chakraborty Jiyun Shi Haijuan Gao Shuang Liu Tc-Labeled Cyclic RGD Peptides for Noninvasive Monitoring of Tumor Integrin αβ Expression Molecular Imaging |
| title | Tc-Labeled Cyclic RGD Peptides for Noninvasive Monitoring of Tumor Integrin αβ Expression |
| title_full | Tc-Labeled Cyclic RGD Peptides for Noninvasive Monitoring of Tumor Integrin αβ Expression |
| title_fullStr | Tc-Labeled Cyclic RGD Peptides for Noninvasive Monitoring of Tumor Integrin αβ Expression |
| title_full_unstemmed | Tc-Labeled Cyclic RGD Peptides for Noninvasive Monitoring of Tumor Integrin αβ Expression |
| title_short | Tc-Labeled Cyclic RGD Peptides for Noninvasive Monitoring of Tumor Integrin αβ Expression |
| title_sort | tc labeled cyclic rgd peptides for noninvasive monitoring of tumor integrin αβ expression |
| url | https://doi.org/10.2310/7290.2011.00006 |
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